BDBM496512 NAU-LAT-8502cac5-8
BDBM496632 CVD-0005286 NAU-LAT-64f4b287-4
BDBM496633 NAU-LAT-64f4b287-5 CVD-0005287
Latrunculin A LatA BDBM65515 LAT-A 76343-93-6
US20240058459, Compound Sunitinib-ester amide linker (AVT-4517) BDBM652295
- Amano, Y; Umezawa, N; Sato, S; Watanabe, H; Umehara, T; Higuchi, T Activation of lysine-specific demethylase 1 inhibitor peptide by redox-controlled cleavage of a traceless linker. Bioorg Med Chem 25: 1227-1234 (2017)
- Kok, ZY; Stoddart, LA; Mistry, SJ; Mocking, TAM; Vischer, HF; Leurs, R; Hill, SJ; Mistry, SN; Kellam, B Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H J Med Chem 65: 8258-8288 (2022)
- Augustyn, E; Finke, K; Zur, AA; Hansen, L; Heeren, N; Chien, HC; Lin, L; Giacomini, KM; Colas, C; Schlessinger, A; Thomas, AA LAT-1 activity of meta-substituted phenylalanine and tyrosine analogs. Bioorg Med Chem Lett 26: 2616-2621 (2016)
- Zhang, H; Gomika Udugamasooriya, D Linker optimization and activity validation of a cell surface vimentin targeted homo-dimeric peptoid antagonist for lung cancer stem cells. Bioorg Med Chem 97: (2024)
- Nomura, W; Aikawa, H; Taketomi, S; Tanabe, M; Mizuguchi, T; Tamamura, H Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands. Bioorg Med Chem 23: 6967-73 (2015)
- Awalt, JK; Nguyen, ATN; Fyfe, TJ; Thai, BS; White, PJ; Christopoulos, A; Jörg, M; May, LT; Scammells, PJ Examining the Role of the Linker in Bitopic J Med Chem 65: 9076-9095 (2022)
- Cheng, S; Li, M; Feng, Y; Liu, T; He, L; Xu, M; Ma, L; Li, X Glycan-Modified Peptides for Dual Inhibition of Human Immunodeficiency Virus Entry into Dendritic Cells and T Cells. J Med Chem 67: 4225-4233
- Zheng, S; Zhang, K; Zhang, X; Xiao, Y; Wang, T; Jiang, S Development of Inhibitors Targeting the V-Domain Ig Suppressor of T Cell Activation Signal Pathway. J Med Chem 65: 11900-11912 (2022)
- Li, Y; Qu, J; Jiang, L; Peng, X; Wu, K; Chen, M; Peng, Y; Cao, X Application and challenges of nitrogen heterocycles in PROTAC linker. Eur J Med Chem 273:
- You, W; Steegborn, C Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin. ACS Med Chem Lett 11: 2285-2289 (2020)
- Eckroat, TJ; Green, KD; Reed, RA; Bornstein, JJ; Garneau-Tsodikova, S Investigation of the role of linker moieties in bifunctional tacrine hybrids. Bioorg Med Chem 21: 3614-23 (2013)
- Argade, A; Bhamidipati, S; Li, H; Carroll, D; Clough, J; Keim, H; Sylvain, C; Rossi, AB; Coquilla, C; Issakani, SD; Masuda, ES; Payan, DG; Singh, R Application of cultured human mast cells (CHMC) for the design and structure-activity relationship of IgE-mediated mast cell activation inhibitors. Bioorg Med Chem Lett 25: 2117-21 (2015)
- Ye, X; Gaucher, JF; Hu, H; Wang, L; Broussy, S Dimer Peptide Ligands of Vascular Endothelial Growth Factor: Optimizing Linker Length for High Affinity and Antiangiogenic Activity. J Med Chem 66: 9753-9765 (2023)
- Basagni, F; Ortega, JA; Bertozzi, SM; Armirotti, A; Summa, M; Bertorelli, R; Bartolini, M; Mellor, IR; Bedeschi, M; Bottegoni, G; Lembo, V; Minarini, A; Cavalli, A; Rosini, M Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties. Eur J Med Chem 261:
- Goon, S; Shiu Chen Liu, C; Ghosh Dastidar, U; Paul, B; Mukherjee, S; Sarkar, HS; Desai, M; Jana, R; Pal, S; Sreedevi, NV; Ganguly, D; Talukdar, A Exploring the Structural Attributes of Yoda1 for the Development of New-Generation Piezo1 Agonist Yaddle1 as a Vaccine Adjuvant Targeting Optimal T Cell Activation. J Med Chem 67: 8225-8246
- Grant, PS; Kahlcke, N; Govindpani, K; Hunter, M; MacDonald, C; Brimble, MA; Glass, M; Furkert, DP Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes. Bioorg Med Chem Lett 29: (2019)
- PUGLIOLI, S; FAVALLI, N; BASSI, G; GALBIATI, A; ZANA, A; CAZZAMALLI, S; NERI, D HIGH-AFFINITY LIGANDS OF FIBROBLAST ACTIVATION PROTEIN FOR TARGETED DELIVERY APPLICATIONS US Patent US20250177582 (2025)
- Sudoł, S; Kucwaj-Brysz, K; Kurczab, R; Wilczyńska, N; Jastrzębska-Więsek, M; Satała, G; Latacz, G; Głuch-Lutwin, M; Mordyl, B; Żesławska, E; Nitek, W; Partyka, A; Buzun, K; Doroz-Płonka, A; Wesołowska, A; Bielawska, A; Handzlik, J Chlorine substituents and linker topology as factors of 5-HT Eur J Med Chem 203: (2020)
- Nguyen, C; Blanco, J; Mazaleyrat, JP; Krust, B; Callebaut, C; Jacotot, E; Hovanessian, AG; Wakselman, M Specific and irreversible cyclopeptide inhibitors of dipeptidyl peptidase IV activity of the T-cell activation antigen CD26. J Med Chem 41: 2100-10 (1998)
- Dyniewicz, J; Lipinski, PF; Kosson, P; Lesniak, A; Bochynska-Czyz, M; Muchowska, A; Tourwé, D; Ballet, S; Misicka, A; Lipkowski, AW Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds. ACS Med Chem Lett 8: 73-77 (2017)
- Beinat, C; Banister, SD; van Prehn, S; Doddareddy, MR; Hibbs, D; Sako, M; Chebib, M; Tran, T; Al-Muhtasib, N; Xiao, Y; Kassiou, M Consequences of linker length alteration of thea7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333. Bioorg Med Chem Lett 22: 2380-4 (2012)
- Thach, TT; Lee, CK; Park, HW; Lee, SJ; Lee, SJ Syringaresinol induces mitochondrial biogenesis through activation of PPARß pathway in skeletal muscle cells. Bioorg Med Chem Lett 26: 3978-83 (2016)
- Goulet, S; Poupart, MA; Gillard, J; Poirier, M; Kukolj, G; Beaulieu, PL Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization. Bioorg Med Chem Lett 20: 196-200 (2010)
- Bach, P; Nilsson, K; Svensson, T; Bauer, U; Hammerland, LG; Peterson, A; Wållberg, A; Osterlund, K; Karis, D; Boije, M; Wensbo, D Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5). Bioorg Med Chem Lett 16: 4788-91 (2006)
- Göransson, O; McBride, A; Hawley, SA; Ross, FA; Shpiro, N; Foretz, M; Viollet, B; Hardie, DG; Sakamoto, K Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase. J Biol Chem 282: 32549-60 (2007)
- Tremblay, ML; Pike, K; Perez Quintero, LA Enhancing CD8+ T cells for adoptive T cell therapy by inhibiting PTPN1 (PTP1B) and PTPN2 (TC-PTP) US Patent US11597739 (2023)
- Plunk, MA; Alaniz, A; Olademehin, OP; Ellington, TL; Shuford, KL; Kane, RR Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation. ACS Med Chem Lett 11: 141-146 (2020)
- Chung, S; Parker, JB; Bianchet, M; Amzel, LM; Stivers, JT Impact of linker strain and flexibility in the design of a fragment-based inhibitor. Nat Chem Biol 5: 407-13 (2009)
- Conejo-García, A; Báñez-Coronel, M; Sánchez-Martín, RM; Rodríguez-González, A; Ramos, A; Ramírez de Molina, A; Espinosa, A; Gallo, MA; Campos, JM; Lacal, JC Influence of the linker in bispyridium compounds on the inhibition of human choline kinase. J Med Chem 47: 5433-40 (2004)
- Corte, JR; Fang, T; Osuna, H; Pinto, DJ; Rossi, KA; Myers, JE; Sheriff, S; Lou, Z; Zheng, JJ; Harper, TW; Bozarth, JM; Wu, Y; Luettgen, JM; Seiffert, DA; Decicco, CP; Wexler, RR; Quan, ML Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker. J Med Chem 60: 1060-1075 (2017)
- Chen, W; Guo, N; Qi, M; Dai, H; Hong, M; Guan, L; Huan, X; Song, S; He, J; Wang, Y; Xi, Y; Yang, X; Shen, Y; Su, Y; Sun, Y; Gao, Y; Chen, Y; Ding, J; Tang, Y; Ren, G; Miao, Z; Li, J Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy. Eur J Med Chem 138: 514-531 (2017)
- Wang, T; Wang, K; Zhang, Y; Zhang, K; Cai, S; Jiang, S; Xiao, Y; Zhang, X Novel Benzimidazoles as Potent Small-Molecule Inhibitors and Degraders of V-Domain Ig Suppressor of T-Cell Activation (VISTA). J Med Chem 66: 11881-11892 (2023)
- PubChem, PC Late stage assay provider counterscreen for TLR9 inhibitors: Luminescence-based assay to identify inhibitors of TLR9-dependent cell activation using RAW264.7 cells PubChem Bioassay (2013)
- Lin, TA; McIntyre, KW; Das, J; Liu, C; O'Day, KD; Penhallow, B; Hung, CY; Whitney, GS; Shuster, DJ; Yang, X; Townsend, R; Postelnek, J; Spergel, SH; Lin, J; Moquin, RV; Furch, JA; Kamath, AV; Zhang, H; Marathe, PH; Perez-Villar, JJ; Doweyko, A; Killar, L; Dodd, JH; Barrish, JC; Wityak, J; Kanner, SB Selective Itk inhibitors block T-cell activation and murine lung inflammation. Biochemistry 43: 11056-62
- Liu, R; Peng, L; Han, H; Lam, KS Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells. Biopolymers 84: 595-604 (2006)
- Plescia, J; Hédou, D; Pousse, ME; Labarre, A; Dufresne, C; Mittermaier, A; Moitessier, N Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications. Eur J Med Chem 240: (2022)
- Okuzumi, T; Fiedler, D; Zhang, C; Gray, DC; Aizenstein, B; Hoffman, R; Shokat, KM Inhibitor hijacking of Akt activation. Nat Chem Biol 5: 484-93 (2009)
- Pujala, B; Panpatil, D; Bernales, S; Belmar, S; Ureta Díaz, GA Inhibitors of fibroblast activation protein US Patent US11504364 (2022)
- Chen, Q; Wang, A; Covelli, DJ; Bhattacharjee, A; Wang, Q; Orth-He, EL; Rao, SD; Huang, HC; Ball, DP; Hsiao, JC; Bachovchin, DA Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation. J Med Chem 66: 2589-2607 (2023)
- Schmees, N; Wortmann, L; Kirchhoff, D; Nguyen, TT; Werbeck, N; Bömer, U; Petersen, K; Kober, C; Lechner, C; Kosemund, D; Offringa, R; Grees, M; Bader, B Substituted aminoquinolones as DGKalpha inhibitors for immune activation US Patent US11998539 (2024)
- Schmees, N; Roehn, U; Kirchhoff, D; Petersen, K; Grees, M; Werbeck, N; Bader, B; Offringa, R; Link, C Substituted aminothiazoles as DGKzeta inhibitors for immune activation US Patent US11964953 (2024)
- Poongavanam, V; Atilaw, Y; Siegel, S; Giese, A; Lehmann, L; Meibom, D; Erdelyi, M; Kihlberg, J Linker-Dependent Folding Rationalizes PROTAC Cell Permeability. J Med Chem 65: 13029-13040 (2022)
- Suebsuwong, C; Pinkas, DM; Ray, SS; Bufton, JC; Dai, B; Bullock, AN; Degterev, A; Cuny, GD Activation loop targeting strategy for design of receptor-interacting protein kinase 2 (RIPK2) inhibitors. Bioorg Med Chem Lett 28: 577-583 (2018)
- Sauerberg, P; Jeppesen, L; Olesen, PH; Sheardown, MJ; Fink-Jensen, A; Rasmussen, T; Rimvall, K; Shannon, HE; Bymaster, FP; DeLapp, NW; Calligaro, DO; Ward, JS; Whitesitt, CA; Thomsen, C Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation. Bioorg Med Chem Lett 8: 2897-902 (1999)
- Hou, X; Vandermeers, A; Gourlet, P; Vandermeers-Piret, MC; Robberecht, P Structural requirements for the occupancy of rat brain PACAP receptors and adenylate cyclase activation. Neuropharmacology 33: 1189-95 (1994)
- Chen, T; Ning, M; Ye, Y; Wang, K; Leng, Y; Shen, J Design, synthesis and structure-activity relationship studies of GPR40 agonists containing amide linker. Eur J Med Chem 152: 175-194 (2018)
- Chen, S; Chen, Z; Lu, L; Zhao, Y; Zhou, R; Xie, Q; Shu, Y; Lin, J; Yu, X; Wang, Y Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy. Eur J Med Chem 255: (2023)
- Jukič, M; Ilaš, J; Brvar, M; Kikelj, D; Cesar, J; Anderluh, M Linker-switch approach towards new ATP binding site inhibitors of DNA gyrase B. Eur J Med Chem 125: 500-514 (2017)
- Bourgault, S; Vaudry, D; Ségalas-Milazzo, I; Guilhaudis, L; Couvineau, A; Laburthe, M; Vaudry, H; Fournier, A Molecular and conformational determinants of pituitary adenylate cyclase-activating polypeptide (PACAP) for activation of the PAC1 receptor. J Med Chem 52: 3308-16 (2009)
- Isozaki, K; Li, J; Okada, K; Nishimura, H; Matsushima, A; Nose, T; Costa, T; Shimohigashi, Y Spare interactions of highly potent [Arg(14),Lys(15)]nociceptin for cooperative induction of ORL1 receptor activation. Bioorg Med Chem 17: 7904-8 (2009)
- Fulton, BS; Knapp, BL; Bidlack, JM; Neumeyer, JL Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors. Bioorg Med Chem Lett 20: 1507-9 (2010)
- Marek, L; Hamacher, A; Hansen, FK; Kuna, K; Gohlke, H; Kassack, MU; Kurz, T Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells. J Med Chem 56: 427-36 (2013)
- Liu, S; Guo, P; Wang, K; Zhang, S; Li, Y; Shen, J; Mei, L; Ye, Y; Zhang, Q; Yang, H General Pharmacological Activation Mechanism of K J Med Chem 65: 10285-10299 (2022)
- Abdelsamie, AS; Bey, E; Hanke, N; Empting, M; Hartmann, RW; Frotscher, M Inhibition of 17ß-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker. Eur J Med Chem 82: 394-406 (2014)
- Asai, D; Inoue, N; Sugiyama, M; Fujita, T; Matsuyama, Y; Liu, X; Matsushima, A; Nose, T; Costa, T; Shimohigashi, Y Direct evidence of edge-to-face CH/π interaction for PAR-1 thrombin receptor activation. Bioorg Med Chem 51: (2021)
- Cooper, AG; MacDonald, C; Glass, M; Hook, S; Tyndall, JDA; Vernall, AJ Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment. Eur J Med Chem 145: 770-789 (2018)
- Xu, X; Chang, X; Huang, J; Zhang, D; Wang, M; Jing, T; Zhuang, Y; Kou, J; Qiu, Z; Wang, J; Li, Z; Bian, J Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles. Eur J Med Chem 236: (2022)
- Thiele, NA; Kärkkäinen, J; Sloan, KB; Rautio, J; Huttunen, KM Secondary carbamate linker can facilitate the sustained release of dopamine from brain-targeted prodrug. Bioorg Med Chem Lett 28: 2856-2860 (2018)
- Yang, J; Guo, H; Padilla, RS; Berwick, M; Miao, Y Replacement of the Lys linker with an Arg linker resulting in improved melanoma uptake and reduced renal uptake of Tc-99m-labeled Arg-Gly-Asp-conjugated alpha-melanocyte stimulating hormone hybrid peptide. Bioorg Med Chem 18: 6695-700 (2010)
- Larson, P; Kucaba, TA; Xiong, Z; Olin, M; Griffith, TS; Ferguson, DM Design and Synthesis of N1-Modified Imidazoquinoline Agonists for Selective Activation of Toll-like Receptors 7 and 8. ACS Med Chem Lett 8: 1148-1152 (2017)
- Gobec, M; Mlinaric-Rašcan, I; Dolenc, MS; Jakopin, Ž Structural requirements of acylated Gly-l-Ala-d-Glu analogs for activation of the innate immune receptor NOD2. Eur J Med Chem 116: 1-12 (2016)
- Appendino, G; Minassi, A; Morello, AS; De Petrocellis, L; Di Marzo, V N-Acylvanillamides: development of an expeditious synthesis and discovery of new acyl templates for powerful activation of the vanilloid receptor. J Med Chem 45: 3739-45 (2002)
- Rajak, H; Kumar, P; Parmar, P; Thakur, BS; Veerasamy, R; Sharma, PC; Sharma, AK; Gupta, AK; Dangi, JS Appraisal of GABA and PABA as linker: design and synthesis of novel benzamide based histone deacetylase inhibitors. Eur J Med Chem 53: 390-7 (2012)
- Moussa, IA; Banister, SD; Akladios, FN; Chua, SW; Kassiou, M Effects of linker elongation in a series of N-(2-benzofuranylmethyl)-N'-(methoxyphenylalkyl)piperazines¿? receptor ligands. Bioorg Med Chem Lett 21: 5707-10 (2011)
- Wang, MS; Wang, ZZ; Li, ZL; Gong, Y; Duan, CX; Cheng, QH; Huang, W; Yang, GF Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy. J Med Chem 66: 611-626 (2023)
- Heo, JH; Seo, HN; Choe, YJ; Kim, S; Oh, CR; Kim, YD; Rhim, H; Choo, DJ; Kim, J; Lee, JY T-type Ca2+ channel blockers suppress the growth of human cancer cells. Bioorg Med Chem Lett 18: 3899-901 (2008)
- Suto, MJ; Gupta, V; Mathew, B; Zhang, W; Pallero, MA; Murphy-Ullrich, JE Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β. ACS Med Chem Lett 11: 1130-1136 (2020)
- McClure, KF; Darout, E; Guimarães, CR; DeNinno, MP; Mascitti, V; Munchhof, MJ; Robinson, RP; Kohrt, J; Harris, AR; Moore, DE; Li, B; Samp, L; Lefker, BA; Futatsugi, K; Kung, D; Bonin, PD; Cornelius, P; Wang, R; Salter, E; Hornby, S; Kalgutkar, AS; Chen, Y Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response. J Med Chem 54: 1948-52 (2011)
- Chen, IJ; Chen, HL; Demetriou, M Lateral compartmentalization of T cell receptor versus CD45 by galectin-N-glycan binding and microfilaments coordinate basal and activation signaling. J Biol Chem 282: 35361-72 (2007)
- Jing, Q; Li, H; Roman, LJ; Martásek, P; Poulos, TL; Silverman, RB An Accessible Chiral Linker to Enhance Potency and Selectivity of Neuronal Nitric Oxide Synthase Inhibitors. ACS Med Chem Lett 5: 56-60 (2014)
- Qin, D; Sullivan, R; Berkowitz, WF; Bittman, R; Rotenberg, SA Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry. J Med Chem 43: 1413-7 (2000)
- Lopez-Tapia, F; Brotherton-Pleiss, C; Yue, P; Murakami, H; Costa Araujo, AC; Reis Dos Santos, B; Ichinotsubo, E; Rabkin, A; Shah, R; Lantz, M; Chen, S; Tius, MA; Turkson, J Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors. ACS Med Chem Lett 9: 250-255 (2018)
- Jia, F; Lei, H; Chen, Y; Li, T; Xing, L; Cao, Z; Zhai, X Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors. Bioorg Med Chem 28: (2020)
- Brooks, CD; Summers, JB Modulators of leukotriene biosynthesis and receptor activation. J Med Chem 39: 2629-54 (1996)
- Stanford, SM; Krishnamurthy, D; Falk, MD; Messina, R; Debnath, B; Li, S; Liu, T; Kazemi, R; Dahl, R; He, Y; Yu, X; Chan, AC; Zhang, ZY; Barrios, AM; Woods, VL; Neamati, N; Bottini, N Discovery of a novel series of inhibitors of lymphoid tyrosine phosphatase with activity in human T cells. J Med Chem 54: 1640-54 (2011)
- Waibel, M; De Angelis, M; Stossi, F; Kieser, KJ; Carlson, KE; Katzenellenbogen, BS; Katzenellenbogen, JA Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta. Eur J Med Chem 44: 3412-24 (2009)
- Matsuda, H; Kogami, Y; Nakamura, S; Sugiyama, T; Ueno, T; Yoshikawa, M Structural requirements of flavonoids for the adipogenesis of 3T3-L1 cells. Bioorg Med Chem 19: 2835-41 (2011)
- Bachovchin, WW; Lai, H; Wu, W RADIOFLUORINATED AGENTS FOR PET IMAGING SELECTIVELY TARGETING FIBROBLAST ACTIVATION PROTEIN US Patent US20240366807 (2024)
- Tietze, R; Löber, S; Hübner, H; Gmeiner, P; Kuwert, T; Prante, O Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker. Bioorg Med Chem Lett 18: 983-8 (2008)
- Zeng, LF; Jiang, XH; Sanchez, T; Zhang, HS; Dayam, R; Neamati, N; Long, YQ Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: effects of the phenyl substituent and the linker orientation. Bioorg Med Chem 16: 7777-87 (2008)
- Clark, CG; Rossi, KA; Corte, JR; Fang, T; Smallheer, JM; De Lucca, I; Nirschl, DS; Orwat, MJ; Pinto, DJP; Hu, Z; Wang, Y; Yang, W; Jeon, Y; Ewing, WR; Myers, JE; Sheriff, S; Lou, Z; Bozarth, JM; Wu, Y; Rendina, A; Harper, T; Zheng, J; Xin, B; Xiang, Q; Luettgen, JM; Seiffert, DA; Wexler, RR; Lam, PYS Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability. Bioorg Med Chem Lett 29: (2019)
- DiMauro, EF; Newcomb, J; Nunes, JJ; Bemis, JE; Boucher, C; Chai, L; Chaffee, SC; Deak, HL; Epstein, LF; Faust, T; Gallant, P; Gore, A; Gu, Y; Henkle, B; Hsieh, F; Huang, X; Kim, JL; Lee, JH; Martin, MW; McGowan, DC; Metz, D; Mohn, D; Morgenstern, KA; Oliveira-dos-Santos, A; Patel, VF; Powers, D; Rose, PE; Schneider, S; Tomlinson, SA; Tudor, YY; Turci, SM; Welcher, AA; Zhao, H; Zhu, L; Zhu, X Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation. J Med Chem 51: 1681-94 (2008)
- Dobenecker, MW; Park, JS; Marcello, J; McCabe, MT; Gregory, R; Knight, SD; Rioja, I; Bassil, AK; Prinjha, RK; Tarakhovsky, A Signaling function of PRC2 is essential for TCR-driven T cell responses. J Exp Med 215: 1101-1113
- Dai, XJ; Zhao, LJ; Yang, LH; Guo, T; Xue, LP; Ren, HM; Yin, ZL; Xiong, XP; Zhou, Y; Ji, SK; Liu, HM; Liu, HM; Liu, Y; Zheng, YC Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells. J Med Chem 66: 3896-3916 (2023)
- Sun, H; Liu, L; Lu, J; Bai, L; Li, X; Nikolovska-Coleska, Z; McEachern, D; Yang, CY; Qiu, S; Yi, H; Sun, D; Wang, S Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity. J Med Chem 54: 3306-18 (2011)
- Gu, SX; Qiao, H; Zhu, YY; Shu, QC; Liu, H; Ju, XL; De Clercq, E; Balzarini, J; Pannecouque, C A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. Bioorg Med Chem 23: 6587-93 (2015)
- Lachance, N; Guiral, S; Huang, Z; Leclerc, JP; Li, CS; Oballa, RM; Ramtohul, YK; Wang, H; Wu, J; Zhang, L Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series. Bioorg Med Chem Lett 22: 623-7 (2011)
- Loaiza, PR; Löber, S; Hübner, H; Gmeiner, P Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker. Bioorg Med Chem 17: 5482-7 (2009)
- Bobesh, KA; Renuka, J; Srilakshmi, RR; Yellanki, S; Kulkarni, P; Yogeeswari, P; Sriram, D Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors. Bioorg Med Chem 24: 42-52 (2016)
- Johnson, SM; Connelly, S; Wilson, IA; Kelly, JW Toward optimization of the linker substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies. J Med Chem 51: 6348-58 (2008)
- Lee, KH; Petruncio, G; Shim, A; Burdick, M; Zhang, Z; Shim, YM; Noble, SM; Paige, M Effect of Modifier Structure on the Activation of Leukotriene A J Med Chem 62: 10605-10616 (2019)
- Khan, PM; Correa, RG; Divlianska, DB; Peddibhotla, S; Sessions, EH; Magnuson, G; Brown, B; Suyama, E; Yuan, H; Mangravita-Novo, A; Vicchiarelli, M; Su, Y; Vasile, S; Smith, LH; Diaz, PW; Reed, JC; Roth, GP Identification of Inhibitors of NOD1-Induced Nuclear Factor-¿B Activation. ACS Med Chem Lett 2: 780-785 (2011)
- Pelish, HE; Peterson, JR; Salvarezza, SB; Rodriguez-Boulan, E; Chen, JL; Stamnes, M; Macia, E; Feng, Y; Shair, MD; Kirchhausen, T Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro. Nat Chem Biol 2: 39-46 (2006)
- Mandabi, A; Ganin, H; Meijler, MM Synergistic activation of quorum sensing in Vibrio harveyi. Bioorg Med Chem Lett 25: 3966-9 (2015)
- Macchia, B; Balsamo, A; Breschi, MC; Lapucci, A; Lucacchini, A; Macchia, F; Manera, C; Martinelli, A; Martini, C; Martinotti, E Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors. J Med Chem 35: 1009-18 (1992)
- Pismataro, MC; Horenstein, NA; Stokes, C; Quadri, M; De Amici, M; Papke, RL; Dallanoce, C Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation. Eur J Med Chem 205: (2020)
- Duvall, B; Zimmermann, SC; Gao, RD; Thomas, AG; Kalčic, F; Veeravalli, V; Elgogary, A; Rais, R; Rojas, C; Le, A; Slusher, BS; Tsukamoto, T Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker. Bioorg Med Chem 28: (2020)
- Simoni, D; Gebbia, N; Invidiata, FP; Eleopra, M; Marchetti, P; Rondanin, R; Baruchello, R; Provera, S; Marchioro, C; Tolomeo, M; Marinelli, L; Limongelli, V; Novellino, E; Kwaasi, A; Dunford, J; Buccheri, S; Caccamo, N; Dieli, F Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. J Med Chem 51: 6800-7 (2008)
- Zhou, YD; Kim, YP; Mohammed, KA; Jones, DK; Muhammad, I; Dunbar, DC; Nagle, DG Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells. J Nat Prod 68: 947-50 (2005)
- Gentili, F; Ghelfi, F; Giannella, M; Piergentili, A; Pigini, M; Quaglia, W; Vesprini, C; Crassous, PA; Paris, H; Carrieri, A alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype. J Med Chem 47: 6160-73 (2004)
- Nakamura, M; Kajita, D; Matsumoto, Y; Hashimoto, Y Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker. Bioorg Med Chem 21: 7381-91 (2013)
- Makadia, P; Shah, SR; Pingali, H; Zaware, P; Patel, D; Pola, S; Thube, B; Priyadarshini, P; Suthar, D; Shah, M; Giri, S; Trivedi, C; Jain, M; Patel, P; Bahekar, R Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists. Bioorg Med Chem 19: 771-82 (2011)
- Liu, F; Hakami, RM; Dyas, B; Bahta, M; Lountos, GT; Waugh, DS; Ulrich, RG; Burke, TR A rapid oxime linker-based library approach to identification of bivalent inhibitors of the Yersinia pestis protein-tyrosine phosphatase, YopH. Bioorg Med Chem Lett 20: 2813-6 (2010)
- Koura, M; Yamaguchi, Y; Kurobuchi, S; Sumida, H; Watanabe, Y; Enomoto, T; Matsuda, T; Okuda, A; Koshizawa, T; Matsumoto, Y; Shibuya, K Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency andß-selectivity of liver X receptor agonist. Bioorg Med Chem 24: 3436-46 (2016)
- Yu, JY; Cheng, HJ; Wu, HR; Wu, WS; Lu, JW; Cheng, TJ; Wu, YT; Fang, JM Structure-based design of bacterial transglycosylase inhibitors incorporating biphenyl, amine linker and 2-alkoxy-3-phosphorylpropanoate moieties. Eur J Med Chem 150: 729-741 (2018)
- Kasuga, J; Oyama, T; Hirakawa, Y; Makishima, M; Morikawa, K; Hashimoto, Y; Miyachi, H Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: effect of introduction of fluorine at the linker part. Bioorg Med Chem Lett 18: 4525-8 (2008)
- Deck, LM; Hunsaker, LA; Vander Jagt, TA; Whalen, LJ; Royer, RE; Vander Jagt, DL Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin. Eur J Med Chem 143: 854-865 (2018)
- Venukadasula, PK; Owusu, BY; Bansal, N; Ross, LJ; Hobrath, JV; Bao, D; Truss, JW; Stackhouse, M; Messick, TE; Klampfer, L; Galemmo, RA Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation. ACS Med Chem Lett 7: 177-81 (2016)
- Teng, M; Young, DW; Tan, Z The Pursuit of Enzyme Activation: A Snapshot of the Gold Rush. J Med Chem 65: 14289-14304 (2022)
- Maximov, PY; Fernandes, DJ; McDaniel, RE; Myers, CB; Curpan, RF; Jordan, VC Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells. J Med Chem 57: 4569-83 (2014)
- Lu, Q; Gouda, NA; Quan, G; Nada, H; Elkamhawy, A; Lee, D; Lee, CH; Cho, J; Lee, K Novel cudraisoflavone J derivatives as potent neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/HO-1 signaling. Eur J Med Chem 242: (2022)
- Clarke, CA; Lugar, III, CW; Morphy, JR; Richardson, TI; Rudyk, H; Sapmaz, S; Stites, RE; Vaught, GM Compounds useful for inhibiting RORγt US Patent US11008336 (2021)
- Lugar, III, CW; Morphy, JR; Richardson, TI; Rudyk, HC; Sapmaz, S; Stites, RE Compounds useful for inhibiting ROR-gamma-t US Patent US10603320 (2020)
- Sabnis, RW Factor XI Activation Inhibitors for Treating Thromboses, Embolism, Hypercoagulability, or Fibrotic Changes. ACS Med Chem Lett 13: 1548-1549 (2022)
- Sabnis, RW Factor XI Activation Inhibitors for Treating Thrombosis, Embolisms, Hypercoagulability, and Fibrotic Changes. ACS Med Chem Lett 13: 530-531 (2022)
- Kalin, JH; Butler, KV; Akimova, T; Hancock, WW; Kozikowski, AP Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells. J Med Chem 55: 639-51 (2012)
- Venkatesh, R; Ramaiah, MJ; Gaikwad, HK; Janardhan, S; Bantu, R; Nagarapu, L; Sastry, GN; Ganesh, AR; Bhadra, M Luotonin-A based quinazolinones cause apoptosis and senescence via HDAC inhibition and activation of tumor suppressor proteins in HeLa cells. Eur J Med Chem 94: 87-101 (2015)
- Oishi, S; Misu, R; Tomita, K; Setsuda, S; Masuda, R; Ohno, H; Naniwa, Y; Ieda, N; Inoue, N; Ohkura, S; Uenoyama, Y; Tsukamura, H; Maeda, K; Hirasawa, A; Tsujimoto, G; Fujii, N Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands. ACS Med Chem Lett 2: 53-57 (2011)
- Nomura, DK; Blankman, JL; Simon, GM; Fujioka, K; Issa, RS; Ward, AM; Cravatt, BF; Casida, JE Activation of the endocannabinoid system by organophosphorus nerve agents. Nat Chem Biol 4: 373-8 (2008)
- Zhang, Q; Yan, L; Zhang, L; Yu, J; Han, Z; Liu, H; Gu, J; Wang, K; Wang, J; Chen, F; Zhao, R; Yan, Y; Jiang, C; You, Q; Wang, L Allosteric Activation of Protein Phosphatase 5 with Small Molecules. J Med Chem 67: 15080-15097
- Casey, RJ; Desaulniers, JP; Hojfeldt, JW; Mapp, AK Expanding the repertoire of small molecule transcriptional activation domains. Bioorg Med Chem 17: 1034-43 (2009)
- Blois, J; Yuan, H; Smith, A; Pacold, ME; Weissleder, R; Cantley, LC; Josephson, L Slow self-activation enhances the potency of viridin prodrugs. J Med Chem 51: 4699-707 (2008)
- Rhim, H; Lee, YS; Park, SJ; Chung, BY; Lee, JY Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett 15: 283-6 (2004)
- Carreras, CW; Siani, MA; Santi, DV; Dillon, SB Stable expression of a synthetic gene for the human motilin receptor: use in an aequorin-based receptor activation assay. Anal Biochem 300: 146-51 (2002)
- Zhou, D; Chu, W; Rothfuss, J; Zeng, C; Xu, J; Jones, L; Welch, MJ; Mach, RH Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis. Bioorg Med Chem Lett 16: 5041-6 (2006)
- Zhu, W; Liu, C; Xi, K; Li, A; Shen, LA; Li, Y; Jia, M; He, Y; Chen, G; Liu, C; Chen, Y; Chen, K; Sun, F; Zhang, D; Duan, C; Wang, H; Wang, D; Zhao, Y; Meng, X; Zhu, D Discovery of Novel 1-Phenylpiperidine Urea-Containing Derivatives Inhibiting β-Catenin/BCL9 Interaction and Exerting Antitumor Efficacy through the Activation of Antigen Presentation of cDC1 Cells. J Med Chem 67: 12485-12520
- Willems, S; Morstein, J; Hinnah, K; Trauner, D; Merk, D A Photohormone for Light-Dependent Control of PPARα in Live Cells. J Med Chem 64: 10393-10402 (2021)
- Spiegel, D; Murelli, R; Zhang, A Chimeric small molecules for the recruitment of antibodies to cancer cells US Patent US9296708 (2016)
- Kakuta, H; Koiso, Y; Nagasawa, K; Hashimoto, Y Fluorescent bioprobes for visualization of puromycin-sensitive aminopeptidase in living cells. Bioorg Med Chem Lett 13: 83-6 (2002)
- Hill, JE; Linder, MK; Davies, KS; Sawada, GA; Morgan, J; Ohulchanskyy, TY; Detty, MR Selenorhodamine photosensitizers for photodynamic therapy of P-glycoprotein-expressing cancer cells. J Med Chem 57: 8622-34 (2014)
- Kargbo, RB Thiazole Derivatives as Inhibitors for the Treatment of Cancer Cells Resistant. ACS Med Chem Lett 9: 169-170 (2018)
- Xu, C; Han, Y; Xu, S; Wang, R; Yue, M; Tian, Y; Li, X; Zhao, Y; Gong, P Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker. Eur J Med Chem 186: (2020)
- Yang, J; Li, Z; Li, H; Liu, C; Wang, N; Shi, W; Liao, C; Cai, X; Huang, W; Qian, H Design, synthesis and structure-activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker. Bioorg Med Chem 25: 2445-2450 (2017)
- Tanaka, A; Hattori, K; Taniguchi, K; Okitsu, O; Tabuchi, S; Nishio, M; Nagakura, Y; Maeda, N; Murai, H; Seki, J Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. Bioorg Med Chem Lett 16: 4861-4 (2006)
- Ho, SS; Go, ML Restraining the flexibility of the central linker in terameprocol results in constrained analogs with improved growth inhibitory activity. Bioorg Med Chem Lett 23: 6127-33 (2013)
- Li, L; Okumu, A; Dellos-Nolan, S; Li, Z; Karmahapatra, S; English, A; Yalowich, JC; Wozniak, DJ; Mitton-Fry, MJ Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety. Bioorg Med Chem Lett 28: 2477-2480 (2018)
- Maresso, AW; Wu, R; Kern, JW; Zhang, R; Janik, D; Missiakas, DM; Duban, ME; Joachimiak, A; Schneewind, O Activation of inhibitors by sortase triggers irreversible modification of the active site. J Biol Chem 282: 23129-39 (2007)
- Bowler, JM; Hervert, KL; Kearley, ML; Miller, BG Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose. ACS Med Chem Lett 4: 580-4 (2013)
- Tang, J; Do, HT; Huber, AD; Casey, MC; Kirby, KA; Wilson, DJ; Kankanala, J; Parniak, MA; Sarafianos, SG; Wang, Z Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker. Eur J Med Chem 166: 390-399 (2019)
- Schoepf, AM; Salcher, S; Obexer, P; Gust, R Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells. Eur J Med Chem 195: (2020)
- Brimacombe, KR; Walsh, MJ; Liu, L; Vásquez-Valdivieso, MG; Morgan, HP; McNae, I; Fothergill-Gilmore, LA; Michels, PA; Auld, DS; Simeonov, A; Walkinshaw, MD; Shen, M; Boxer, MB Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase. ACS Med Chem Lett 5: 12-7 (2014)
- Oboh, E; Schubert, TJ; Teixeira, JE; Stebbins, EE; Miller, P; Philo, E; Thakellapalli, H; Campbell, SD; Griggs, DW; Huston, CD; Meyers, MJ Optimization of the Urea Linker of Triazolopyridazine MMV665917 Results in a New Anticryptosporidial Lead with Improved Potency and Predicted hERG Safety Margin. J Med Chem 64: 11729-11745 (2021)
- Kabasawa, M; Furuta, M; Ibayashi, Y; Kanemaru, K; Kohatsu, H; Kuramochi, F; Yamatoya, K; Nakata, K; Nakamura, Y; Tomoshige, S; Ohgane, K; Furuyama, Y; Takasawa, R; Kobayashi, S; Sugawara, F; Ikekita, M; Kuramochi, K Plakevulin A induces apoptosis and suppresses IL-6-induced STAT3 activation in HL60 cells. Bioorg Med Chem Lett 110:
- Fortin, S; Charest-Morin, X; Turcotte, V; Lauvaux, C; Lacroix, J; Côté, MF; Gobeil, S; C-Gaudreault, R Activation of Phenyl 4-(2-Oxo-3-alkylimidazolidin-1-yl)benzenesulfonates Prodrugs by CYP1A1 as New Antimitotics Targeting Breast Cancer Cells. J Med Chem 60: 4963-4982 (2017)
- Yang, JS; Lee, C; Cho, M; Kim, H; Kim, JH; Choi, S; Oh, SJ; Kang, JS; Jeong, JH; Kim, HJ; Han, G Discovery of Orally Available Runt-Related Transcription Factor 3 (RUNX3) Modulators for Anticancer Chemotherapy by Epigenetic Activation and Protein Stabilization. J Med Chem 58: 3512-21 (2015)
- Thomas, MG; De Rycker, M; Ajakane, M; Albrecht, S; Álvarez-Pedraglio, AI; Boesche, M; Brand, S; Campbell, L; Cantizani-Perez, J; Cleghorn, LAT; Copley, RCB; Crouch, SD; Daugan, A; Drewes, G; Ferrer, S; Ghidelli-Disse, S; Gonzalez, S; Gresham, SL; Hill, AP; Hindley, SJ; Lowe, RM; MacKenzie, CJ; MacLean, L; Manthri, S; Martin, F; Miguel-Siles, J; Nguyen, VL; Norval, S; Osuna-Cabello, M; Woodland, A; Patterson, S; Pena, I; Quesada-Campos, MT; Reid, IH; Revill, C; Riley, J; Ruiz-Gomez, JR; Shishikura, Y; Simeons, FRC; Smith, A; Smith, VC; Spinks, D; Stojanovski, L; Thomas, J; Thompson, S; Underwood, T; Gray, DW; Fiandor, JM; Gilbert, IH; Wyatt, PG; Read, KD; Miles, TJ J Med Chem 62: 1180-1202 (2019)
- ChEMBL_2539527 Activation of PKC in human J-Lat 10.6 cells infected with latent HIV-1 assessed as reversal of HIV-1 latency by measuring increase of GFP-positive cells at 1 to 10000 nM incubated for 24 hrs by flow cytometry
- ChEMBL_2539528 Activation of PKC in human J-Lat 6.3 cells infected with latent HIV-1 assessed as reversal of HIV-1 latency by measuring increase of GFP-positive cells at 1 to 10000 nM incubated for 24 hrs by flow cytometry
- ChEMBL_1659718 (CHEMBL4009330) Activation of BTN3A1 in human Vgamma9Vdelta2 T cells assessed as induction of T effector cells mediated K562 cell lysis preincubated with K562 cells for 2 hrs followed by T effector cell addition measured after 4 hrs
- ChEMBL_861795 (CHEMBL2173388) Inhibition of SYK-mediated LAT phosphorylation
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- ChEMBL_92286 (CHEMBL705832) Inhibition of AP-1 (activator protein-1) mediated transcriptional activation in Jurkat T-cells
- ChEMBL_2185245 (CHEMBL5097327) Activation of ERK5 in MEF cells
- ChEMBL_2220399 (CHEMBL5133733) Activation of Nrf2 in HEK293T cells
- ChEMBL_1895070 (CHEMBL4397105) Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry
- ChEMBL_1711133 (CHEMBL4121182) Binding affinity to butyrophilin 3A1 in human Vgamma9/Vdelta2 T-cells assessed as activation of Vgamma9/Vdelta2 T-cells by upregulation of CD69 and CD25 after 18 hrs
- ChEMBL_2480574 Inhibition of PD-1/PD-L1 interaction in human Jurkat T cells co-cultured with CHO/TCRAct/PDL1 cells assessed as restoration of T cell activation measured for 6 hrs by luminescence based immune checkpoint blockade assay
- ChEMBL_2428279 Activation of IL-2 in human Jurkat cells incubated for 24 hrs by ELISA
- ChEMBL_1719033 (CHEMBL4134033) Activation of BTN3A1 in human PBMC-derived Vgamma9Vdelta2 T cells assessed as induction of interferon gamma production in response to K562 cells preincubated for 4 hrs with K562 cells followed by 11 days incubation post compound wash out with subsequent coculturing with Vgamma9Vdelta2 T cells for 20 hrs by ELISA
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- ChEMBL_2375095 Activation of human TRPV1 expressed in HEK293F cells
- ChEMBL_729862 (CHEMBL1695216) Activation of CCR5 in human PBMC cells
- ChEMBL_2489289 Inhibition of interaction of human PD-1 expressed in human Jurkat T cells co-expressing Luc/human PD-L1 expressed in CHO-K1 cells assessed as activation of NFAT-mediated luciferase activity pretreated compound with CHO-K1 cells for 2 hrs followed by co-treatment with human Jurkat T cells for 6 hrs by Bio-Glo Luciferase assay
- ChEMBL_2431626 Agonist activity at mouse PIEZO1 transfected in HEK293-T-REx cells assessed as activation of intracellular Ca2+ level
- ChEMBL_1438621 (CHEMBL3386726) Inhibition of Lyp in antiCD3-antibody-stimulated human Jurkat T cells assessed as activation of TCR-mediated and IL-2 promoter driven NFAT/AP1 transcriptional activation incubated for 1 hr by dual luciferase reporter gene assay
- ChEMBL_79561 (CHEMBL689508) Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)
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- ChEMBL_1520985 (CHEMBL3624289) Activation of human Kv7.4 expressed in CHOK1 cells
- ChEMBL_1520990 (CHEMBL3624294) Activation of rat Kv7.4 expressed in CHOK1 cells
- ChEMBL_1980320 (CHEMBL4613582) Activation of caspase 9 in human SMMC7721 cells
- ChEMBL_1980321 (CHEMBL4613583) Activation of caspase 3 in human SMMC7721 cells
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- ChEMBL_363879 (CHEMBL863210) Activation of human PEPT1 expressed in MDCK cells
- ChEMBL_491086 (CHEMBL982109) Inhibition of STAT6 activation in FW4 reporter cells
- ChEMBL_1996622 (CHEMBL4630517) Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay
- ChEMBL_2024433 (CHEMBL4678246) Allosteric inhibition of MALT1-mediated T cell activation in human Jurkat cells assessed as decrease in PMA induced IL2 activation preincubated for 1 hr followed by addition of PMA measured after 5.5 hrs by luciferase reporter gene assay
- ChEMBL_304388 (CHEMBL830038) Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_2110972 (CHEMBL4819822) Inhibition of PD-1/PD-L1 interaction in CHO cells expressing PD-Ll/TCR cocultured with human Jurkat cells expressing PD-1 assessed as activation of effector Jurkat T cells incubated for 6 hrs by luciferase reporter gene assay
- ChEMBL_2320945 Activation of STING pathway in mouse 293T-mSTING cells incubated for 48 hrs by QUANTI-Luc assay
- ChEMBL_1996626 (CHEMBL4630521) Activation of human PPAR-delta LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay
- ChEMBL_2329803 Activation of PKM2 (unknown origin) incubated for 30 mins
- ChEMBL_2322375 Activation of STING signalling pathway in human THP1-Dual cells assessed as increase in IRF-luciferase activation incubated for 24 hrs by QUANTI-luc assay
- ChEMBL_1808777 (CHEMBL4308136) Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 15 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA
- ChEMBL_1808778 (CHEMBL4308137) Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 60 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA
- ChEMBL_1808779 (CHEMBL4308138) Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA
- ChEMBL_1492951 (CHEMBL3528877) Activation of human PXR expressed in human LS174T cells
- ChEMBL_1520984 (CHEMBL3624288) Activation of human Kv7.2/7.3 expressed in CHOK1 cells
- ChEMBL_1520988 (CHEMBL3624292) Activation of human Kv7.1/KCNE1 expressed in CHOK1 cells
- ChEMBL_2347836 Activation of wildtype CFTR (unknown origin) expressed in CHO cells
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- ChEMBL_2432609 Inhibition of NLRP3 inflammasome activation in mouse J774.A1 cells
- ChEMBL_437579 (CHEMBL906015) Inhibition of human GR transcriptional activation by HepTAT cells
- ChEMBL_2325352 Inhibition of PD-1/PD-L1 interaction in human Jurkat T cells cocultured with artificial antigen presenting cells assessed as increase in TCR-mediated Jurkat T cells activation by measuring increase in luciferase signal incubated for 6 hrs by Bio-Glo reagent based luciferase assay
- ChEMBL_1863314 (CHEMBL4364170) Inhibition of MALT1-mediated T cell activation in human Jurkat cells assessed in decrease in PMA/ionomycin-induced IL2 production
- ChEMBL_479059 (CHEMBL921666) Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
- ChEMBL_2069837 (CHEMBL4725090) Activation of human PPARalpha transfected in human Cos7 cells incubated for overnight by luciferase reporter gene assay
- ChEMBL_2288536 Inhibition of thapsigargin-induced XBP1-luciferase activation in human HeLa cells incubated for 24 hrs by luciferase assay
- ChEMBL_2320944 Activation of STING pathway in human 293T-hSTING-R232 cells incubated for 48 hrs by QUANTI-Luc assay
- ChEMBL_2350533 Inhibition of CDC42 activation in human MDA-MB-231 cells treated for 24 hrs by Western blot analysis
- ChEMBL_2463383 Activation of ATF4 ( unknown origin) expressed in human H4 cells incubated for 24 hrs by reporter gene assay
- ChEMBL_2494223 Activation of Cisd2 (unknown origin) transfected in HEK293 cells incubated for 24 hrs by one-glo luciferase assay
- ChEMBL_1659697 (CHEMBL4009309) Activation of BTN3A1 in human Vgamma9Vdelta2 T cells assessed as induction of interleukin 2 stimulated cell proliferation treated for 72 hrs measured on day 11 post last treatment by flow cytometry
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- ChEMBL_304416 (CHEMBL831821) Effective concentration required for the activation of human C202A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304417 (CHEMBL831822) Effective concentration required for the activation of human C296A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304418 (CHEMBL831823) Effective concentration required for the activation of human D204A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304419 (CHEMBL832637) Effective concentration required for the activation of human D204E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304420 (CHEMBL832638) Effective concentration required for the activation of human D204N mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304421 (CHEMBL832639) Effective concentration required for the activation of human D208A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304422 (CHEMBL832640) Effective concentration required for the activation of human D289A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304423 (CHEMBL832641) Effective concentration required for the activation of human D300A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304424 (CHEMBL832642) Effective concentration required for the activation of human E209A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304425 (CHEMBL832643) Effective concentration required for the activation of human E209D mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304426 (CHEMBL832644) Effective concentration required for the activation of human E209Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304427 (CHEMBL832645) Effective concentration required for the activation of human E209R mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304428 (CHEMBL832646) Effective concentration required for the activation of human F131A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304429 (CHEMBL831974) Effective concentration required for the activation of human F226A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304430 (CHEMBL832804) Effective concentration required for the activation of human H132A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304431 (CHEMBL832331) Effective concentration required for the activation of human H277A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304432 (CHEMBL832332) Effective concentration required for the activation of human K125A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304433 (CHEMBL832333) Effective concentration required for the activation of human K196A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304434 (CHEMBL832334) Effective concentration required for the activation of human K198A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304435 (CHEMBL832335) Effective concentration required for the activation of human K280A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304436 (CHEMBL832336) Effective concentration required for the activation of human Q307A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304437 (CHEMBL832485) Effective concentration required for the activation of human R128A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304438 (CHEMBL832486) Effective concentration required for the activation of human R195A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304439 (CHEMBL832487) Effective concentration required for the activation of human R212A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304440 (CHEMBL832488) Effective concentration required for the activation of human R285A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304441 (CHEMBL832489) Effective concentration required for the activation of human R287A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304442 (CHEMBL832490) Effective concentration required for the activation of human R287E mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304443 (CHEMBL832491) Effective concentration required for the activation of human R287K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304444 (CHEMBL832492) Effective concentration required for the activation of human R287Q mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304445 (CHEMBL832493) Effective concentration required for the activation of human R301A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304446 (CHEMBL832494) Effective concentration required for the activation of human R310A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304447 (CHEMBL832495) Effective concentration required for the activation of human R310K mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304448 (CHEMBL832496) Effective concentration required for the activation of human S314A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304449 (CHEMBL832497) Effective concentration required for the activation of human S314T mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304450 (CHEMBL832498) Effective concentration required for the activation of human S317A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304451 (CHEMBL832499) Effective concentration required for the activation of human T221A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304452 (CHEMBL832500) Effective concentration required for the activation of human T222A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_304453 (CHEMBL832501) Effective concentration required for the activation of human Y136A mutant strain P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate
- ChEMBL_1744139 (CHEMBL4178649) Inhibition of Mycobacterium tuberculosis LAT using L-lysine as substrate by spectroscopic method
- ChEMBL_1891570 (CHEMBL4393397) Activation of human ERbeta assessed as induction of transcriptional activation incubated for 24 hrs by luciferase reporter gene assay
- ChEBML_159871 Inhibition of transcriptional activation in cells expressing progesterone receptor isoform B
- ChEMBL_481746 (CHEMBL1002847) Inhibition of hypoxia-induced HIF1 activation in human U251 cells
- ChEMBL_44515 (CHEMBL658539) The effective concentration in CV-1 cells for glucocorticoid response element activation (GRE).
- ChEMBL_2322374 Activation of STING signalling pathway in human THP1-Dual cells assessed as increase in NF-kappaB-SEAP activation incubated for 24 hrs by QUANTI-Blue reagent based assay
- ChEMBL_2132495 (CHEMBL4842010) Inhibition of PD-1/PD-L1 interaction in human Jurkat T cells expressing PD-1 cocultured with CHO cells expressing PD-Ll/TCR assessed as activation of Jurkat cells by luciferase reporter gene assay
- ChEMBL_1866554 (CHEMBL4367529) Activation of BTN3A1 in human PBMC-derived Vgamma9/Vdelta2 T cells assessed as induction of IL2-stimulated IFNgamma production measured after 48 hrs by ELISA
- ChEBML_214535 Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEBML_214854 Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEBML_208244 Activation of plasminogen
- ChEMBL_1978686 (CHEMBL4611821) Activation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter assay relative to control
- ChEMBL_2208081 (CHEMBL5121030) Activation of GIRK1/2 channel (unknown origin) expressed in HEK293 cells incubated for 6 mins by thallium flux assay
- ChEMBL_2208083 (CHEMBL5121032) Activation of GIRK1/4 channel (unknown origin) expressed in HEK293 cells incubated for 6 mins by thallium flux assay
- ChEMBL_2217813 (CHEMBL5130945) Activation of human EAAT2 overexpressed in MDCK cells assessed as glutamate reuptake incubated for 5 mins by LCMS assay
- ChEMBL_28876 (CHEMBL645946) Concentration required to inhibit activator protein-1(AP-1) mediated transcriptional activation in human Jurkat T-cells
- ChEMBL_1869951 (CHEMBL4371118) Activation of delta opioid receptor (unknown origin) expressed in CHO cells
- ChEMBL_1869952 (CHEMBL4371119) Activation of mu opioid receptor (unknown origin) expressed in CHO cells
- ChEMBL_1869953 (CHEMBL4371120) Activation of kappa opioid receptor (unknown origin) expressed in CHO cells
- ChEMBL_1877274 (CHEMBL4378668) Activation of human utrophin-1 in iDMD cells by HTRF assay
- ChEMBL_2347841 Activation of wildtype CFTR G551D mutant (unknown origin) expressed in CHO cells
- ChEMBL_44511 (CHEMBL658535) Inhibition of transcriptional activation in CV-1 cells expressing glucocorticoid receptor
- ChEMBL_604755 (CHEMBL1072549) Inhibition of CXCR3 in human T cells
- ChEMBL_604756 (CHEMBL1072550) Inhibition of CXCR4 in human T cells
- ChEMBL_2291623 Activation of cGAMP-STING signaling pathway in human THP-1 cells assessed as increase in ISRE activation by measuring luciferase activation in presence of cGAMP by luciferase reporter gene assay
- ChEMBL_304486 (CHEMBL832866) Effective concentration required for the activation of wild-type P2Y1 receptors expressed in COS-7 cells for the accumulation of inositol phosphate is determined in separate experiment
- ChEMBL_2364914 Activation of CPT-1 in digitonin-permeabilized human MCF7 cells preincubated for 2 hrs followed by digitonin addition for 6 mins by liquid scintillation method
- ChEMBL_741337 (CHEMBL1764806) Inhibition of staurosporine induced activation of caspase 3 activation in human Hela cells assessed as hydrolysis of Z-DEVD-R110 substrate by microplate fluorescence assay
- ChEMBL_1334655 (CHEMBL3239855) Activation of human VR1 expressed in HEK293 cells assessed as stimulation of Ca2+ influx
- ChEMBL_214533 (CHEMBL819370) Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214534 (CHEMBL819371) Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214535 (CHEMBL819372) Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214851 (CHEMBL824693) Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_214854 (CHEMBL821469) Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_142870 (CHEMBL750065) Compound was evaluated for concentration-dependent and oscillatory increase in [Ca2+], caused by activation of hNK3 receptors in CHO cells
- ChEMBL_2266440 Activation of human 3X-HA N-tagged OTR expressed in CHO-K1 cells incubated for 10 mins by cell Western assay
- ChEMBL_2266441 Activation of human 3X-HA N-tagged AVP1a expressed in CHO-K1 cells incubated for 10 mins by cell Western assay
- ChEMBL_2266442 Activation of human 3X-HA N-tagged AVP1b expressed in CHO-K1 cells incubated for 10 mins by cell Western assay
- Procaspase-3 Activation Assay Procaspase-3 activation assay; activation of procaspase-3 to caspase-3.
- Procaspase-7 Activation Assay Procaspase-7 activation assay; activation of procaspase-7 to caspase-7.
- ChEMBL_1559131 (CHEMBL3771552) Activation of human GLP1R expressed in HEK293 cells preincubated for 30 mins followed by addition of cAMP-d2 conjugate/cryptate conjugate incubated for 60 mins by fluorescence analysis
- ChEBML_76081 Binding affinity of compound towards H+/K+ ATPase for activation was determined
- ChEMBL_104281 (CHEMBL711716) Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat
- ChEMBL_104282 (CHEMBL711717) Concentration for half maximal activation of metabotropic glutamate mGluR5b in rat
- ChEMBL_104458 (CHEMBL712801) Concentration for half maximal activation of metabotropic glutamate mGluR6 in rat
- ChEMBL_104478 (CHEMBL712460) Concentration for half maximal activation of metabotropic glutamate mGluR7 in human
- ChEMBL_104481 (CHEMBL879748) Concentration for half maximal activation of metabotropic glutamate mGluR7 in rat
- ChEMBL_104621 (CHEMBL715569) Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
- ChEMBL_105571 (CHEMBL709768) Concentration for half maximal activation of metabotropic glutamate mGluR1b in human
- ChEMBL_105576 (CHEMBL709773) Concentration for half maximal activation of metabotropic glutamate mGluR1b in human
- ChEMBL_105717 (CHEMBL719084) Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat
- ChEMBL_105718 (CHEMBL719085) Concentration for half maximal activation of metabotropic glutamate mGluR1b in rat
- ChEMBL_105719 (CHEMBL719086) Concentration for half maximal activation of metabotropic glutamate mGluR1c in rat
- ChEMBL_105896 (CHEMBL717757) Concentration for half maximal activation of metabotropic glutamate mGluR2 in human
- ChEMBL_106064 (CHEMBL718229) Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat
- ChEMBL_106389 (CHEMBL717244) Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat
- ChEMBL_106552 (CHEMBL884506) Concentration for half maximal activation of metabotropic glutamate mGluR4a in human
- ChEMBL_106690 (CHEMBL714671) Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat
- ChEMBL_106717 (CHEMBL715723) Concentration for half maximal activation of metabotropic glutamate mGluR5a in human
- ChEMBL_205636 (CHEMBL813244) Tested for the inhibition of prostromelysin activation with no preincubation period
- ChEMBL_2206399 (CHEMBL5119107) Activation of human EAAT2 transfected in COS7 cells assessed as glutamate uptake
- ChEMBL_2206405 (CHEMBL5119113) Activation of human EAAT2 transfected in Glial cells assessed as glutamate uptake
- ChEMBL_2217850 (CHEMBL5130982) Activation of human EAAT2 expressed in COS cells assessed as glutamate uptake
- ChEMBL_453027 (CHEMBL902174) Activation of Nurr1 expressed in MN9D cells by luciferase reporter gene assay
- ChEMBL_459402 (CHEMBL926562) Inhibition of HIF1 activation in human T47D cells by TK-luciferase assay
- ChEMBL_612957 (CHEMBL1070909) Activation of KCNQ2/KCNQ3 expressed in CHO cells by isotopic efflux assay
- ChEMBL_765690 (CHEMBL1827135) Inhibition of SREBP2 activation expressed in CHO-K1 cells by densitometric analysis
- ChEMBL_940482 (CHEMBL2329609) Inhibition of c-MET activation (unknown origin) expressed in human HCT116 cells
- ChEMBL_1891572 (CHEMBL4393399) Activation of human ERbeta assessed as induction of transcriptional activation incubated for 24 hrs in presence of 50 uM H2O2 by luciferase reporter gene assay
- ChEMBL_1891573 (CHEMBL4393400) Activation of human ERbeta assessed as induction of transcriptional activation incubated for 24 hrs in presence of 100 uM H2O2 by luciferase reporter gene assay
- ChEMBL_2355761 Inhibition of human NOX4 in T-REx-293 cells
- ChEBML_1769782 Activation of human PXR
- ChEMBL_2286625 Activation of human PXR
- ChEMBL_354582 (CHEMBL865109) Activation of glucokinase
- ChEMBL_477125 (CHEMBL940160) Activation of TRPA1
- ChEMBL_573968 (CHEMBL1062958) Activation of PPARgamma
- ChEMBL_575546 (CHEMBL1035543) Activation of glucokinase
- ChEMBL_632337 (CHEMBL1112965) Activation of PXR
- ChEMBL_839534 (CHEMBL2090341) Activation of PXR
- ChEMBL_857730 (CHEMBL2168757) Activation of PXR
- ChEMBL_861572 (CHEMBL2174513) Activation of SIRT1
- ChEMBL_878388 (CHEMBL2186894) Activation of PXR
- ChEMBL_337605 (CHEMBL861567) Inhibition of TGFbeta R1 induced transcriptional activation of p3TP-Lux in mink Mv1Lu lung cells
- ChEMBL_458019 (CHEMBL924288) Activation of Drosophila melanogaster ryanodine receptor in Sf9 cells assessed as induction of calcium mobilization
- ChEMBL_572154 (CHEMBL1028510) Activation of ryanodine receptor 1 in mouse C2C12 cells assessed as induction of calcium mobilization
- ChEMBL_572155 (CHEMBL1028511) Activation of ryanodine receptor 2 in rat PC12 cells assessed as induction of calcium mobilization
- ChEMBL_842220 (CHEMBL2091725) Activation of rat TRPA1 expressed in HEK293 cells assessed as stimulation of intracellular Ca2+ levels
- ChEMBL_842223 (CHEMBL2091728) Activation of rat TRPM8 expressed in HEK293 cells assessed as stimulation of intracellular Ca2+ levels
- ChEMBL_858721 (CHEMBL2167032) Inhibition of IKK2 in human A549 cells assessed as inhibition of TNFalpha-induced NFKB activation
- ChEMBL_2194552 (CHEMBL5106912) Activation of human ACKR3 overexpressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment incubated for 90 mins by luminescence based assay
- ChEBML_1769547 Inhibition of Mycobacterium tuberculosis LAT using L-lysine and alpha-ketoglutaric acid as substrate by spectrophotometric analysis
- ChEMBL_2099865 (CHEMBL4808261) Activation of mouse STING expressed in RAW-Lucia ISG cells incubated for 24 hrs by quanti-blue SEAP reporter gene assay
- ChEMBL_2322396 Activation of STING signalling pathway in human PBMC cells assessed as increase in CXCL10 level incubated for 4 hrs by ELISA method
- ChEMBL_2434889 Agonist activity at SOS1 in human HeLa cells assessed as activation of p-ERK1/2 incubated for 30 mins by immunoblot analysis
- ChEMBL_654562 (CHEMBL1243606) Activity at human TRPM8 expressed in HEK293 cells assessed as compound concentration causing leftward shift of voltage for half maximal activation
- ChEMBL_163473 (CHEMBL772308) Transcriptional activation for RAR alpha receptor
- ChEMBL_163477 (CHEMBL772312) Transcriptional activation for RAR beta receptor
- ChEMBL_163481 (CHEMBL772394) Transcriptional activation for RAR gamma receptor
- ChEMBL_164856 (CHEMBL769014) Transcriptional activation for RXR alpha receptor
- ChEMBL_2437756 Inhibition of human ROMK expressed in T-REX-CHO cells incubated for 30 mins by thallium flux assay
- ChEMBL_209245 (CHEMBL814872) Evaluated for the activation of human thrombin receptor measured by platelet aggregation
- ChEMBL_2277154 Activation of recombinant rat Neurolysin using QFS as substrate incubated for 10 mins
- ChEMBL_76081 (CHEMBL879774) Binding affinity of compound towards H+/K+ ATPase for activation was determined
- ChEMBL_2017415 (CHEMBL4670993) Inhibition of hPD-1/hPD-L1 immune checkpoint using PD-L1 expressing human aAPCs and PD-1 expressing human Jurkat cells assessed as activation of effector Jurkat T cells incubated for 6 hrs by luciferase reporter gene based immune checkpoint blockade cell-based assay
- ChEMBL_100276 (CHEMBL712018) Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells
- ChEMBL_153615 (CHEMBL759727) Transcriptional activation of reporter assay by PPAR gamma receptor in CV-1 cells
- ChEMBL_1722144 (CHEMBL4137144) Activation of RasGRP3 in human Ramos cells after 30 mins by immunoblot method
- ChEMBL_196757 (CHEMBL800546) Transcriptional activation of CV-1 cells expressing murine Retinoid X receptor RXR alpha
- ChEMBL_197057 (CHEMBL804833) Transcriptional activation of CV-1 cells expressing murine Retinoid X receptor RXR beta
- ChEMBL_197217 (CHEMBL798965) Transcriptional activation of CV-1 cells expressing murine Retinoid X receptor RXR gamma
- ChEMBL_2268115 Activation of human SIRT6 in human HepG2 cells assessed as decrease in H3K9 acetylation
- ChEMBL_2268116 Activation of human SIRT6 in human HepG2 cells assessed as decrease in H3K56 acetylation
- ChEMBL_529095 (CHEMBL971112) Activation of PPARgamma transfected in human MCF7 cells by luciferase reporter gene assay
- ChEMBL_579352 (CHEMBL1063193) Inhibition of human ERG activation expressed in CHO cells by rubidium efflux assay
- ChEMBL_67185 (CHEMBL677953) Agonist effect on transcriptional activation of T47D cells expressing human estrogen receptor beta
- ChEMBL_736252 (CHEMBL1693396) Activation of KCNQ1 expressed in HEK293 cells by atomic absorption Rb'+ efflux assay
- ChEMBL_2046249 (CHEMBL4700948) Activation of human NPFF2R overexpressing CHO cells assessed as inhibition of forskolin-stimulated cAMP degradation incubated for 30 mins in presence of IBMX by fluorescence based assay
- ChEMBL_942049 (CHEMBL2340279) Inhibition of recombinant full length PDK1 (unknown origin) expressed in insect cells assessed as inhibition of Akt activation measured for 30 mins in presence of [gamma32P-ATP]
- ChEMBL_884121 (CHEMBL2216051) Displacement of Smac-1F from human His-tagged XIAP linker BIR2-BIR3 linker (124 to 356 residues) after 3 hrs by fluorescent polarization assay
- ChEMBL_2251903 (CHEMBL5166113) Inhibition of full-length ERK5 in HEK293 cells assessed as paradoxical activation of ERK5 transcriptional activity incubated for 20 hrs by dual luciferase reporter assay
- ChEMBL_2360293 Activation of Nrf2 in human U2OS cells co-expressing Keap1 assessed as induction of Nrf2 nuclear translocation incubated for 6 hrs by PathHunter chemiluminescence based analysis
- ChEMBL_858381 (CHEMBL2168596) Activation of glucokinase in rat INS-1 cells assessed as stimulation of glucose-induced insulin secretion
- ChEMBL_2110661 (CHEMBL4819511) Activation of human TRPML1deltaNC-YFP expressed in HEK293 cells incubated for 10 mins by Fluo-4 dye calcium imaging based FLIPR analysis
- ChEMBL_2110662 (CHEMBL4819512) Activation of human TRPML2-YFP expressed in HEK293 cells incubated for 10 mins by Fluo-4 dye calcium imaging based FLIPR analysis
- ChEMBL_2110663 (CHEMBL4819513) Activation of human TRPML3-YFP expressed in HEK293 cells incubated for 10 mins by Fluo-4 dye calcium imaging based FLIPR analysis
- ChEMBL_2322395 Activation of STING signalling pathway in human PBMC cells assessed as increase in IFN-beta level incubated for 4 hrs by ELISA method
- ChEMBL_2322397 Activation of STING signalling pathway in human PBMC cells assessed as increase in IL-6 level incubated for 4 hrs by ELISA method
- ChEMBL_651442 (CHEMBL1227415) Inhibition of LFA1-mediated Staphylococcal enterotoxin B-stimulated human T cell activation in presence of 10% fetal bovine serum
- ChEMBL_2549797 Inhibition of SOS1 in human HeLa cells assessed as reduction in RAS activation pretreated for 30 mins followed by EGF stimulation for 3 mins by G-LISA analysis
- ChEMBL_746783 (CHEMBL1776952) Competitive inhibition of human XIAP linker BIR2-BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
- ChEMBL_1866547 (CHEMBL4367522) Activation of BTN3A1 in human PBMC-derived Vgamma9/Vdelta2 T cells assessed as induction of IL2-stimulated cell proliferation by measuring increase in CD3+ cells preincubated for 3 days followed by 11 days incubation post compound washout and subsequent IL2 stimulation for every 3 days measured after 14 days by flow cytometry
- ChEBML_1703623 Activation of PXR (unknown origin)
- ChEMBL_1277658 (CHEMBL3096900) Activation of human CaSR
- ChEMBL_1296096 (CHEMBL3131525) Activation of human glucokinase
- ChEMBL_1520094 (CHEMBL3625558) Activation of human PXR
- ChEMBL_154559 (CHEMBL757894) Activation of PDE4D3 (phosphodiesterase).
- ChEMBL_1591271 (CHEMBL3829804) Activation of human PXR
- ChEMBL_1650126 (CHEMBL3999260) Activation of human PXR
- ChEMBL_1765642 (CHEMBL4200889) Activation of human FXR
- ChEMBL_1829999 (CHEMBL4329873) Activation of human PXR
- ChEMBL_1869833 (CHEMBL4370899) Activation of human ERG
- ChEMBL_1871102 (CHEMBL4372269) Activation of human PXR
- ChEMBL_1904787 (CHEMBL4407145) Activation of human PXR
- ChEMBL_1990611 (CHEMBL4624346) Activation of human glucokinase
- ChEMBL_208243 (CHEMBL877957) Activation of tissue plasminogen
- ChEMBL_2109463 (CHEMBL4818138) Activation of human NAMPT
- ChEMBL_2238426 (CHEMBL5152322) Activation of human P2Y12R
- ChEMBL_2266238 Activation of PXR (unknown origin)
- ChEMBL_2274192 Activation of TLR7 (unknown origin)
- ChEMBL_2274193 Activation of TLR8 (unknown origin)
- ChEMBL_2286631 Activation of PXR (unknown origin)
- ChEMBL_2347837 Activation of CFTR (unknown origin)
- ChEMBL_2364930 Activation of CLpP (unknown origin)
- ChEMBL_2364934 Activation of HDAC1 (unknown origin)
- ChEMBL_2364935 Activation of PDE4D5 (unknown origin)
- ChEMBL_2364946 Activation of NAMPT (unknown origin)
- ChEMBL_2434898 Activation of ULK1 (unknown origin)
- ChEMBL_2434901 Activation of AMPK (unknown origin)
- ChEMBL_2437791 Activation of PXR (unknown origin)
- ChEMBL_2450751 Activation of PXR (unknown origin)
- ChEMBL_2450877 Activation of PKM2 (unknown origin)
- ChEMBL_2455197 Activation of PXR (unknown origin)
- ChEMBL_2483570 Activation of ABCA1 (unknown origin)
- ChEMBL_2483572 Activation of SREBP1c (unknown origin)
- ChEMBL_2498719 Activation of FoxO1(unknown origin)
- ChEMBL_2499851 Activation of SIRT1 (unknown origin)
- ChEMBL_2573187 Activation of PXR (unknown origin)
- ChEMBL_2573188 Activation of AhR (unknown origin)
- ChEMBL_631012 (CHEMBL1110983) Activation of human PXR
- ChEMBL_633016 (CHEMBL1118241) Activation of TRPV1 channel
- ChEMBL_633017 (CHEMBL1118242) Activation of TRPA1 channel
- ChEMBL_633025 (CHEMBL1118250) Activation of TRPM8 channel
- ChEMBL_643487 (CHEMBL1212351) Activation of human CD69
- ChEMBL_718492 (CHEMBL1680287) Activation of human PXR
- ChEMBL_850468 (CHEMBL2150655) Activation of KCNQ2/Q3
- ChEMBL_872345 (CHEMBL2187816) Activation of human PXR
- ChEMBL_885336 (CHEMBL2215199) Activation of human glucokinase
- ChEMBL_1816464 (CHEMBL4316038) Activation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay
- ChEMBL_207282 (CHEMBL811365) Inhibition of acetylation of histone-4 in human T-24 cancer cells
- ChEMBL_1279808 (CHEMBL3095509) Activation of glucokinase in rat INS-1 cells assessed as glucose-stimulated insulin secretion
- ChEMBL_1584412 (CHEMBL3819955) Activation of bovine TREK1 expressed in AZT cells assessed as reduction in channel currents
- ChEMBL_1843854 (CHEMBL4344281) Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells
- ChEMBL_1870563 (CHEMBL4371730) Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells
- ChEMBL_1870564 (CHEMBL4371731) Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells
- ChEMBL_1870565 (CHEMBL4371732) Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells
- ChEMBL_2212565 (CHEMBL5125514) Inhibition of Med25 transcriptional activation in human MCF-7 cells by fluorescence polarization assay
- ChEMBL_2283116 Activation of caspase 3/7 in human 22Rv1 cells by Caspase-Glo reagent based analysis
- ChEMBL_2299035 Activation of Nrf2 in human IMR-32-ARE-Luc cells by Bright-Glo luciferase assay
- ChEMBL_475987 (CHEMBL931441) Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay
- ChEMBL_527926 (CHEMBL975114) Inhibition of hypoxia-induced HIF1 activation in human T47D cells by reporter gene assay
- ChEMBL_527928 (CHEMBL975116) Inhibition of hypoxia-induced HIF1 activation in human PC3 cells by reporter gene assay
- ChEMBL_596923 (CHEMBL1048864) Activation of human TAAR1 expressed in CHOK1 cells coexpressing Galpha16 assessed as calcium accumulation
- ChEMBL_736251 (CHEMBL1693395) Activation of KCNQ2/Q3 expressed in CHO cells by atomic absorption Rb'+ efflux assay
- ChEMBL_2549796 Inhibition of SOS1 in human Calu-1 cells assessed as reduction in RAS activation pretreated for 30 mins followed by EGF stimulation for 3 mins by G-LISA analysis
- ChEMBL_1776595 (CHEMBL4233587) Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay
- ChEMBL_1989794 (CHEMBL4623529) Activation of human TRPV1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
- ChEMBL_2046262 (CHEMBL4700961) Activation of human GPR10 overexpressed in CHO-K1 cells assessed as increase in beta arrestin recruitment incubated for 90 mins by PathHunter assay
- ChEMBL_2251327 (CHEMBL5165537) Inhibition of LPA-mediated ATX activation in human BJeH cells assessed as AKT phosphorylation level incubated for 30 mins by Western blot analysis
- ChEMBL_2251328 (CHEMBL5165538) Inhibition of LPA-mediated ATX activation in human BJeH cells assessed as ERK phosphorylation level incubated for 30 mins by Western blot analysis
- ChEMBL_304461 (CHEMBL832509) Effective concentration for activation of human Opioid receptor kappa 1 expressed in chinese hamster ovary cells to enhance [35S]GTP-gamma-S, binding
- ChEMBL_763210 (CHEMBL1820121) Inhibition of EGFR-induced AP1 activation in human HeLa cells preincubated for 1 hr prior to EGF stimulation by luciferase reporter gene assay
- ChEMBL_763211 (CHEMBL1820122) Inhibition of EGFR-induced HIF1alpha activation in human HeLa cells preincubated for 1 hr prior to EGF stimulation by luciferase reporter gene assay
- ChEMBL_807740 (CHEMBL1959868) Inhibition of rat nNOS expressed in HEK293T cells preincubated for 30 mins prior A23187-induced activation measured after 6 hrs by Griess assay
- ChEMBL_1772654 (CHEMBL4229646) Inhibition of activation of recombinant human pro-heparanase expressed in CHO cells by dimethylmethylene blue based assay
- ChEMBL_2475647 Inhibition of NLRP3 in human THP-1 cells assessed as inhibition of LPS/nigericin-induced caspase-1 activation
- ChEMBL_792741 (CHEMBL1930656) Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of cAMP after 15 mins
- ChEMBL_963160 (CHEMBL2390802) Activation of PKM2 in human Huh7 cells assessed as production of pyruvate and ATP by fluorescence assay
- ChEMBL_967438 (CHEMBL2401228) Activation of AMPK in rat L6 cells assessed as increase of [3H]dGlc uptake after 5 hrs
- ChEMBL_2432608 Inhibition of NLRP3 inflammasome activation in mouse J774.A1 cells preincubated with LPS for 4.5 hrs followed by compound addition for 30 mins and further stimulated with ATP for 30 mins by ELISA
- ChEMBL_2112056 (CHEMBL4820906) Antagonist activity at human TLR2 expressed in HEK-Blue cells assessed as inhibition of Pam3CSK4-induced TLR2/TLR1 activation by measuring decrease in NFkappaB activation pretreated for 2 hrs followed by incubation with agonist for 18 hrs by SEAP assay
- ChEMBL_2112057 (CHEMBL4820907) Antagonist activity at human TLR2 expressed in HEK-Blue cells assessed as inhibition of Pam2CSK4-induced TLR2/TLR6 activation by measuring decrease in NFkappaB activation pretreated for 2 hrs followed by incubation with agonist for 18 hrs by SEAP assay
- ChEMBL_1655191 (CHEMBL4004557) Inhibition of PKCtheta in human Jurkat T cells assessed as reduction in anti-CD3/CD28 antibody-induced T-cell activation by measuring decrease in IL-2 secretion after 5 hrs by luciferase reporter gene assay
- ChEMBL_1728177 (CHEMBL4143455) Inhibition of IDO1 in IFNgamma and LPS-stimulated human dendritic cells co-cultured with human T cells assessed as inhibition of T-cell proliferation in presence of soluble anti-CD3 antibody and human recombinant IL-2 incubated for 2 days
- ChEMBL_1891571 (CHEMBL4393398) Activation of human ERbeta assessed as induction of transcriptional activation by luciferase reporter gene assay
- ChEMBL_1728174 (CHEMBL4143452) Inhibition of human IDO1 expressed in T-REx-293 cells
- ChEMBL_1728182 (CHEMBL4143460) Inhibition of human TDO expressed in T-REx-293 cells
- ChEMBL_2285215 Inhibition of IL6-stimulated STAT3 signalling in human CD4+ T cells
- ChEMBL_1824391 (CHEMBL4324155) Inhibition of NLRP3 inflammasome activation in LPS-primed human THP1 cells assessed as reduction in IL-1beta level preincubated for 10 mins followed by addition of nigericin
- ChEMBL_1838263 (CHEMBL4338396) Activation of recombinant human wild-type STING expressed in 293T cells incubated for 7 hrs in absence of digitonin A by bright Glo-luciferase reporter gene assay
- ChEMBL_2240101 (CHEMBL5153997) Activation of AhR in human HepG2 cells assessed as induction of XRE-dependent reporter activity incubated for 4 hrs by Renilla/Firefly based dual-luciferase reporter assay
- ChEMBL_2240102 (CHEMBL5153998) Activation of AhR in mouse NIH3T3 cells assessed as induction of XRE-dependent reporter activity incubated for 4 hrs by Renilla/Firefly based dual-luciferase reporter assay
- ChEMBL_2240103 (CHEMBL5153999) Activation of AhR in human HaCaT cells assessed as induction of XRE-dependent reporter activity incubated for 4 hrs by Renilla/Firefly based dual-luciferase reporter assay
- ChEMBL_2240104 (CHEMBL5154000) Activation of AhR in mouse Hepa1c1c7 cells assessed as induction of XRE-dependent reporter activity incubated for 4 hrs by Renilla/Firefly based dual-luciferase reporter assay
- ChEMBL_2251902 (CHEMBL5166112) Inhibition of ERK5 (1 to 492 residues) in HEK293 cells assessed as paradoxical activation of ERK5 transcriptional activity incubated for 20 hrs by dual luciferase reporter assay
- ChEMBL_2077389 (CHEMBL4733180) Activation of wild-type human STING expressed in HEK293T cells assessed as IRF3 reporter activation measured after 20 hrs by luciferase reporter gene assay
- ChEMBL_2364943 Activation of 6XHis-FP-rhodamine-tagged full-length human LYPLAL1 expressed in Escherichia coli BL21(DE3) cells preincubated for 60 mins followed by FP-rhodamine probe addition for 30 mins
- ChEMBL_2364944 Activation of 6XHis-FP-rhodamine-tagged full-length mouse LYPLAL1 expressed in Escherichia coli BL21(DE3) cells preincubated for 60 mins followed by FP-rhodamine probe addition for 30 mins
- ChEMBL_2112058 (CHEMBL4820908) Inhibition of TNFalpha (unknown origin) in HEK-Blue-hTLR2 cells assessed as inhibition of TNFalpha-induced NFkappaB activation pretreated for 2 hrs followed by incubation with TNFalpha for 18 hrs by SEAP assay
- ChEMBL_2372381 Inhibition of NLRP3 inflammasome activation in LPS-treated mouse BMDM cells assessed as inhibition of ATP-stimulated IL-1beta release incubated for 30 mins followed by ATP stimulation for 1 hr by ELISA method
- ChEMBL_1477114 (CHEMBL3428281) Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins
- ChEMBL_1364503 (CHEMBL3295051) Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay
- ChEMBL_1516465 (CHEMBL3619606) Agonist activity at human FFA1 expressed in CHO cells assessed as induction of receptor activation by measuring Ca2+influx incubated for by FLIPR method
- ChEMBL_1839943 (CHEMBL4340158) Activation of Nrf2 in human HaCaT-ARE-Luc cells expressing Nqo1 ARE-Luc reporter plasmid incubated for 6 hrs by luciferase reporter gene assay
- ChEMBL_1846389 (CHEMBL4346930) Agonist activity at human TLR2 expressed in HEK-Blue cells assessed as activation of SEAP incubated for 24 hrs by quanti-blue SEAP assay
- ChEMBL_1907170 (CHEMBL4409528) Inhibition of Bcl-xl in human U266B1 cells assessed as caspase 3/7 activation for 6 hrs by Caspase 3/7-Glo luminescence assay
- ChEMBL_1989793 (CHEMBL4623528) Activation of rat recombinant TRPA1 expressed in HEK293 cells assessed as calcium influx preincubated for 5 mins by Fluo-4AM dye based fluorescence assay
- ChEMBL_2033481 (CHEMBL4687639) Activation of recombinant human GPR55 expressed in HEK293 cells assessed as increase in [35S]-GTPgammaS stimulation incubated for 60 min by scintillation counting method
- ChEMBL_2186594 (CHEMBL5098676) Activation of caspase 3/7 in human MV4-11 cells incubated for 6 hrs by Caspase-Glo 3/7 reagent based microplate reader analysis
- ChEMBL_2214684 (CHEMBL5127816) Activation of Androgen receptor-mediated transcription (unknown origin) in African green monkey CV-1 cells incubated for 40 hrs by Luciferase reporter gene assay
- ChEMBL_2228073 (CHEMBL5141586) Activation of PKG1alpha in human HEK293 cells stably expressing VASP assessed as VSAP phosphorylation at Ser 239 incubated for 45 mins by HTRF assay
- ChEMBL_2267955 Antagonist activity at human TLR9 expressed in HEK-Blue hTLR9 cells assessed as activation of NFkappaB incubated for 16 hrs by luciferase reporter gene assay
- ChEMBL_2315525 Agonist activity at TGR5 receptor in human NCI-H716 cells assessed as activation of intracellular cAMP production incubated for 1 hr by HTR-FRET assay
- ChEMBL_2330357 Activation of TGR5 (unknown origin) transfected in human NCI-H716 cells assessed as increase in cAMP production incubated for 24 hrs by HTR-FRET assay
- ChEMBL_763212 (CHEMBL1820123) Inhibition of EGFR-induced Beta-casein activation in human HeLa cells preincubated for 1 hr prior to EGF stimulation by luciferase reporter gene assay
- ChEMBL_2046248 (CHEMBL4700947) Activation of human NPFF2R overexpressing CHO cells assessed as inhibition of forskolin-stimulated cAMP degradation incubated for 30 mins in presence of IBMX and 10% FBS by fluorescence based assay
- ChEMBL_2289550 Activation of human AhR expressed in Saccharomyces cerevisiae YCM3 coexpressing ARNT incubated for 18 hrs
- ChEMBL_2344869 Activation of his6-tagged SIRT6 (unknown origin) using H3K9Ac peptide substrate incubated for 30 mins
- ChEBML_164143 Compound was tested for activation of RNase L by measuring concentration required for 50% inhibition of protein synthesis in mouse L cell extracts
- ChEMBL_1458002 (CHEMBL3367176) Inhibition of AP-1-mediated transcriptional activation in HEK293 cells by luciferase reporter gene assay
- ChEMBL_1832319 (CHEMBL4332327) Activation of firefly luciferase activity expressed in HEK293T cells after 6 hrs by luminescence assay
- ChEMBL_1843598 (CHEMBL4344025) Activation of HIF1 in human T47D cells after 30 mins by luciferase reporter gene assay
- ChEMBL_1970361 (CHEMBL4603179) Allosteric activation of AMPK alpha2/beta1/gamma1 in human HepG2 cells by scintillation proximity assay
- ChEMBL_2254308 (CHEMBL5168518) Activation of rat GLP-1R expressed in CHO cells assessed as increase in cAMP accumulation
- ChEMBL_2254310 (CHEMBL5168520) Activation of mouse GLP-1R expressed in CHO cells assessed as increase in cAMP accumulation
- ChEMBL_2262085 (CHEMBL5217096) Activation of wild-type human Slack expressed in HEK293 cells measured by thallium flux assay
- ChEMBL_2265233 Inhibition of MCL-1 in human MOLP8 cells assessed as increase in caspase 3/7 activation
- ChEMBL_304179 (CHEMBL829175) Caspase activation activity of compound in cell line H-1299 nonsmall-cell lung cancer cells
- ChEMBL_527927 (CHEMBL975115) Inhibition of 1,10 phenanthroline-induced HIF1 activation in human T47D cells by reporter gene assay
- ChEMBL_550371 (CHEMBL999925) Inhibition of hypoxia-induced HIF1 activation in human HeLa cells by luciferase reporter gene assay
- ChEMBL_633015 (CHEMBL1118240) Activation of TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels
- ChEMBL_647717 (CHEMBL1220314) Inhibition of calcineurin-mediated NFAT activation in human Jurkat cells by luciferase reporter gene assay
- ChEMBL_649482 (CHEMBL1219180) Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay
- ChEMBL_659819 (CHEMBL1246709) Activation of human GLP1 receptor expressed in HEK293 cells assessed as increase in cAMP accumulation
- ChEMBL_723352 (CHEMBL1673549) Activation of M1-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
- ChEMBL_723353 (CHEMBL1673550) Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
- ChEMBL_723354 (CHEMBL1673551) Activation of M5-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal
- ChEMBL_807162 (CHEMBL1959826) Activation of PPAR in human HepG2 cells after 24 hrs by luciferase reporter gene assay
- ChEMBL_826311 (CHEMBL2049322) Activation of PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assay
- ChEMBL_961297 (CHEMBL2390473) Activation of human AMPK alpha2 (1 to 398) expressed in African green monkey COS7 cells
- ChEMBL_961308 (CHEMBL2390484) Activation of human AMPK alpha1 (1 to 394) expressed in African green monkey COS7 cells
- ChEMBL_1567255 (CHEMBL3788712) Activation of GPR109A in human A431 cells assessed as suppression of forskolin-induced cAMP production after 30 mins
- ChEMBL_2316633 Activation of SK3 (unknown origin) expressed in HEK293 cells coexpressing CaM/GFP in presence of Ca2+ by electrophysiological method
- ChEMBL_40438 (CHEMBL652377) Inhibition of increase in [Ca2+] efflux from NG108-15 cells caused by activation of rat Bradykinin receptor B2
- ChEMBL_519379 (CHEMBL948800) Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
- ChEMBL_2018186 (CHEMBL4671764) Inhibition of NLRP3 inflammasome activation in human THP1 cells assessed as inhibition of IL-1beta release in presence of MSU
- ChEMBL_2018187 (CHEMBL4671765) Inhibition of NLRP3 inflammasome activation in human THP1 cells assessed as inhibition of IL-1beta release in presence of nigericin
- ChEMBL_1279400 (CHEMBL3096556) Activation of PXR (unknown origin)
- ChEMBL_1433197 (CHEMBL3387597) Activation of PXR (unknown origin)
- ChEMBL_1438948 (CHEMBL3382459) Activation of PXR (unknown origin)
- ChEMBL_1453119 (CHEMBL3364417) Activation of PXR (unknown origin)
- ChEMBL_1506257 (CHEMBL3599141) Activation of PXR (unknown origin)
- ChEMBL_1512252 (CHEMBL3611648) Activation of PXR (unknown origin)
- ChEMBL_1518830 (CHEMBL3625504) Activation of PXR (unknown origin)
- ChEMBL_1519130 (CHEMBL3624323) Activation of PXR (unknown origin)
- ChEMBL_1544071 (CHEMBL3750579) Activation of PXR (unknown origin)
- ChEMBL_1554419 (CHEMBL3767407) Activation of PXR (unknown origin)
- ChEMBL_1554647 (CHEMBL3768743) Activation of human PX receptor
- ChEMBL_1648680 (CHEMBL3997736) Activation of PXR (unknown origin)
- ChEMBL_1666547 (CHEMBL4016343) Activation of PXR (unknown origin)
- ChEMBL_1667925 (CHEMBL4017813) Activation of PXR (unknown origin)
- ChEMBL_1770487 (CHEMBL4222599) Activation of PXR (unknown origin)
- ChEMBL_1829816 (CHEMBL4329690) Activation of PXR (unknown origin)
- ChEMBL_1838929 (CHEMBL4339062) Activation of PXR (unknown origin)
- ChEMBL_1843860 (CHEMBL4344287) Activation of mouse liver PPARalpha
- ChEMBL_1908504 (CHEMBL4410862) Activation of PXR (unknown origin)
- ChEMBL_1980961 (CHEMBL4614223) Activation of glucokinase (unknown origin)
- ChEMBL_1988876 (CHEMBL4622423) Activation of PXR (unknown origin)
- ChEMBL_1992345 (CHEMBL4626080) Activation of SIRT6 (unknown origin)
- ChEMBL_2018359 (CHEMBL4671937) Activation of BAX (unknown origin)
- ChEMBL_2060644 (CHEMBL4715645) Activation of PXR (unknown origin)
- ChEMBL_2071806 (CHEMBL4727340) Activation of PXR (unknown origin)
- ChEMBL_2074100 (CHEMBL4729634) Activation of rat liver phosphofructokinase
- ChEMBL_2145763 (CHEMBL5030043) Activation of CYP3A4 (unknown origin)
- ChEMBL_2149721 (CHEMBL5034183) Activation of PXR (unknown origin)
- ChEMBL_2185244 (CHEMBL5097326) Activation of ERK5 (unknown origin)
- ChEMBL_2224224 (CHEMBL5137737) Activation of PKM2 (unknown origin)
- ChEMBL_2484956 Activation of GLP-1R (unknown origin)
- ChEMBL_2491281 Activation of human 5-HT2A receptor
- ChEMBL_633010 (CHEMBL1118235) Activation of mouse TRPA1 channel
- ChEMBL_633011 (CHEMBL1118236) Activation of human TRPA1 channel
- ChEMBL_633012 (CHEMBL1118237) Activation of rat TRPV1 channel
- ChEMBL_643486 (CHEMBL1212350) Activation of rat NKR-P1A
- ChEMBL_951811 (CHEMBL2353001) Activation of glucokinase (unknown origin)
- ChEMBL_964291 (CHEMBL2395405) Activation of AHR (unknown origin)
- ChEMBL_1444344 (CHEMBL3371775) Activation of of wild type B-raf in human SK-MEL-2 cells assessed as increase in ERK1/2 phosphorylation incubated for 90 mins by Western blotting method
- ChEMBL_1824402 (CHEMBL4324166) Inhibition of NLRP3 inflammasome activation in LPS-primed mouse NG5 cells assessed as reduction in IL-1beta level incubated for 15followed by addition of ATP by ELISA method
- ChEMBL_2046246 (CHEMBL4700945) Activation of human GPR10 overexpressed in CHO-K1 cells assessed as increase in beta arrestin recruitment incubated for 90 mins in presence of 10% FBS by PathHunter assay
- ChEMBL_2365558 Activation of SERCA2a in human HEK293T cells endoplasmic reticulum assessed as increase in calcium release measured for 10 mins in presence of ATP by NADH fluorescence-coupled ATPase assay
- ChEMBL_946792 (CHEMBL2344596) Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
- ChEMBL_946793 (CHEMBL2344597) Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA
- ChEMBL_305250 (CHEMBL833507) Inhibitory concentration for human complement component C3 activation
- ChEMBL_1632359 (CHEMBL3875065) Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgD-mediated B-cell activation by measuring decrease in CD19+ cells expressing CD69 preincubated for 30 mins followed by IgD activation for 2 hrs by lysis reagent-based FACS analysis
- ChEMBL_71255 (CHEMBL685249) Transcriptional activation in CV-1 cells expressing glucocorticoid receptor
- ChEMBL_2226047 (CHEMBL5139560) Inhibition of hERG transfected in T-REX-CHO cells incubated for 30 mins by BTC-AM dye based fluorescence assay
- ChEMBL_2262823 (CHEMBL5217834) Inhibition of NLRC4 inflammasome activation in LPS/flagellin-treated human THP-1 cells preincubated with LPS for 3 hrs followed by compound addition for 30 mins and further stimulated with flagellin for 90 min
- ChEMBL_2064382 (CHEMBL4719635) Activation of STING in human THP-1-Dual cells assessed as induction of type I IFNs by measuring stimulation of IRF pathway incubated for 48 hrs by luciferase reporter gene assay
- ChEMBL_2127477 (CHEMBL4836822) Inhibition of PD-1/PD-L1 interaction in human Jurkat cells cocultured with CHO cells expressing PD-Ll/TCRAct assessed as activation of effector Jurkat cells incubated for 6 hrs by luciferase reporter gene based immune checkpoint blockade cell-based assay
- ChEMBL_1778842 (CHEMBL4235834) Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA
- ChEMBL_1778843 (CHEMBL4235835) Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA
- ChEMBL_2099864 (CHEMBL4808260) Activation of human STING (139 to 379 residues) expressed in THP1-Blue ISG cells incubated for 24 hrs by quanti-blue SEAP reporter gene assay
- ChEMBL_2283976 Agonist activity at human TLR7 expressed in HEK293 cells assessed as activation of NFkappaB incubated for 18 to 24 hrs by SEAP reporter gene based assay
- ChEMBL_2283977 Agonist activity at human TLR8 expressed in HEK293 cells assessed as activation of NFkappaB incubated for 18 to 24 hrs by SEAP reporter gene based assay
- ChEMBL_2322376 Activation of STING signalling pathway in human wild type THP-1 cells assessed as increase in IFN-beta secretion incubated for 4 hrs by ELISA method
- ChEMBL_965794 (CHEMBL2393733) Inhibition of JNK-mediated c-Jun activation in TNFalpha-induced human SW1353 cells preincubated for 30 mins prior to TNFalpha treatment measured after 20 mins
- ChEMBL_2434376 Inhibition of MCT4 in human EVSA-T cells by lactate transport assay
- ChEMBL_305223 (CHEMBL831643) Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cells
- ChEMBL_463328 (CHEMBL947134) Inhibition of human recombinant CDK9/cyclin T expressed in insect cells
- ChEMBL_603504 (CHEMBL1068423) Inhibition of human T-type calcium channel alpha1G in HEK293 cells
- ChEMBL_164143 (CHEMBL771467) Compound was tested for activation of RNase L by measuring concentration required for 50% inhibition of protein synthesis in mouse L cell extracts
- ChEMBL_2025927 (CHEMBL4679740) Binding affinity to BTN3A1 in human PBMC-derived Vgamma9/Vdelta2 T cells assessed as induction of Vgamma9Vdelta2 T cells proliferation incubated for 3 days by gamma delta TCR/PE-CD3+ antibody staining based FACS analysis
- ChEMBL_1676531 (CHEMBL4026674) Activation of human PXR transfected in human hepatoma cells assessed as induction of CYP3A4 by luciferase reporter gene assay
- ChEMBL_613519 (CHEMBL1073630) Activation of human P2Y1 receptor expressed in human 1321N1 cells assessed as induction of calcium flux by FLIPR assay
- ChEMBL_2341298 Inhibition of interaction of PD-1 (unknown origin) expressed in Jurkat T cells carrying luciferase reporter under the control of NFAT promoter/PD-L1 (unknown origin) expressed in CHO cells co-expressing TCR ligand and T-cell surrogate pretreated with CHO cells for 0.5 hrs followed by Jurkat T cell addition and measured after 5 hrs by luminescence based analysis
- ChEMBL_162332 (CHEMBL768341) Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor.
- ChEMBL_162334 (CHEMBL768343) Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor.
- ChEMBL_162336 (CHEMBL768345) Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor.
- ChEMBL_162338 (CHEMBL768347) Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor.
- ChEMBL_162340 (CHEMBL768349) Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor.
- ChEMBL_162342 (CHEMBL884078) Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor.
- ChEMBL_162344 (CHEMBL768352) Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor.
- ChEMBL_162346 (CHEMBL768354) Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor.
- ChEMBL_162348 (CHEMBL768356) Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor.
- ChEMBL_162350 (CHEMBL768358) Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor.
- ChEMBL_162352 (CHEMBL768360) Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor.
- ChEMBL_162354 (CHEMBL768362) Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor.
- ChEMBL_162356 (CHEMBL768364) Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor.
- ChEMBL_2330378 Activation of VP16-fused VDR-LBD (unknown origin) incubated for 18 hrs in presence of substrate by luciferase assay
- ChEMBL_1766508 (CHEMBL4201755) Activation of SOS1 in human HeLa cells expressing wild type KRAS assessed as induction of ERK1/2 T202/Y204 phosphorylation incubated for 30 mins by In-cell Western assay
- ChEMBL_1907171 (CHEMBL4409529) Inhibition of Bcl-xl in human U266B1 cells assessed as caspase 3/7 activation in presence of 10 % serum for 6 hrs by Caspase 3/7-Glo luminescence assay
- ChEMBL_946791 (CHEMBL2344595) Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
- ChEMBL_2316553 Inhibition of human HPK1 in human Jurkat T cells assessed as inhibition of SLP76 phosphorylation
- ChEMBL_2034322 (CHEMBL4688480) Activation of human PXR ligand binding domain incubated for 1 hr by TR-FRET assay
- ChEMBL_38798 (CHEMBL652339) Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
- ChEMBL_304233 (CHEMBL829772) Caspase-3 activation activity tested in DLD1 colon cells done for 24 or 48 hr at 37 degree C
- ChEMBL_304238 (CHEMBL841794) Caspase-3 activation activity tested in P338 cancer cells done for 24 or 48 hr at 37 degree C
- ChEMBL_304239 (CHEMBL877120) Caspase-3 activation activity tested in T47D breast cells done for 24 or 48 hr at 37 degree C
- ChEMBL_304244 (CHEMBL841799) Caspase-3 activation activity tested in LnCap cancer cells done for 24 or 48 hr at 37 degree C
- ChEBML_1717829 Antagonist activity at human CXCR4 expressed in COS7 cells assessed as inhibition of CXCL12-induced receptor activation
- ChEMBL_1455680 (CHEMBL3366025) Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
- ChEMBL_1455687 (CHEMBL3366032) Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
- ChEMBL_1457997 (CHEMBL3367171) Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
- ChEMBL_1498280 (CHEMBL3583801) Inhibition of IL6-induced STAT3 activation in human Hep3B cells after 12 hrs by luciferase assay
- ChEMBL_153383 (CHEMBL763569) Transcriptional activation of reporter assay by human Peroxisome proliferator activated receptor alpha in CV-1 cells
- ChEMBL_153485 (CHEMBL761650) In vitro transcriptional activation of peroxisome proliferator activated alpha-receptor (PPAR) expressed in CV-1 cells
- ChEMBL_153857 (CHEMBL761882) Transcriptional activation of reporter assay by human Peroxisome proliferator activated receptor delta in CV-1 cells
- ChEMBL_154537 (CHEMBL760257) In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
- ChEMBL_223075 (CHEMBL842924) Functional activation of human sympathetic ganglionic type nAChRs in IMR-32 cells containing alpha-3 subtype
- ChEMBL_2274188 Agonist activity in TLR8 (unknown origin) expressed in HEK293 cells assessed as induction of NF-kappa activation
- ChEMBL_434568 (CHEMBL914215) Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as activation of K+ currents
- ChEMBL_469602 (CHEMBL933161) Inhibition of hypoxia-induced HIF1 transcriptional activation in human U251-HRE cells by luciferase reporter assay
- ChEMBL_478428 (CHEMBL932617) Inhibition of hypoxia-induced HIF1 activation in human T47D cells by cell based reporter gene assay
- ChEMBL_508157 (CHEMBL1008215) Inhibition of neutrophil elastase activation in beta-estradiol differentiated mouse EcoM-G cells after 24 hrs
- ChEMBL_508158 (CHEMBL1008216) Inhibition of cathepsin G activation in beta-estradiol differentiated mouse EcoM-G cells after 24 hrs
- ChEMBL_508159 (CHEMBL1008217) Inhibition of proteinase-3 activation in beta-estradiol differentiated mouse EcoM-G cells after 24 hrs
- ChEMBL_652924 (CHEMBL1226127) Activation of Shh in mouse Shh Light2 cells after 30 hrs by luciferase reporter gene assay
- ChEMBL_776383 (CHEMBL1914234) Activation of human PXR in DPX2 cells after 24 hrs by microplate reader relative to control
- ChEMBL_1771782 (CHEMBL4223894) Activation of MAGL in mouse B16-F10 cells using 7-HRA as substrate preincubated for 60 mins followed by substrate addition measured every 2.5 mins for 2 hrs by fluorescence assay
- ChEMBL_2348879 Inhibition of NLRP3 inflammasome activation in mouse J774.A1 cells assessed as reduction in LPS-stimulated IL-1beta level pretreated for 1 hr followed by nigericin treatment for 1 hr by ELISA
- ChEMBL_2064380 (CHEMBL4719633) Activation of STING in mouse RAW-Lucia ISG cells assessed as induction of type I IFNs stimulation by measuring induction of IRF pathway incubated for 48 hrs by luciferase reporter gene assay
- ChEMBL_2064384 (CHEMBL4719637) Activation of STING in human THP-1-Dual cells assessed as induction of type I IFNs by measuring stimulation of NF-kappaB pathway incubated for 48 hrs by luciferase reporter gene assay
- ChEMBL_1666747 (CHEMBL4016543) Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgD-mediated B-cell activation by measuring decrease in CD19+ cells expressing CD69 preincubated for 1 hr followed by IgD activation measured after overnight incubation
- ChEMBL_2263475 Activation of PKM2 (unknown origin) in presence of sorafenib
- ChEMBL_326996 (CHEMBL863528) Inhibition of low pH activation of human TRPV1
- ChEMBL_326997 (CHEMBL863529) Inhibition of low pH activation of rat TRPV1
- ChEMBL_460879 (CHEMBL944818) Blockade of pH 5.5-induced activation of TRPV1
- ChEBML_1623557 Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days by Hoechst 33258 staining based assay
- ChEMBL_2019764 (CHEMBL4673577) Activation of human IR-B expressed in mouse NIH3T3 cells assessed as increase in Akt phosphorylation at Ser473 residue incubated for 30 mins by HTRF method
- ChEMBL_2171635 (CHEMBL5056769) Activation of human GCCR expressed in human HEK293 cells assessed as luminescence signal incubated for 16 hrs at 37C measured by CRE-driven luciferase reporter assay
- ChEMBL_2185620 (CHEMBL5097702) Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta level incubated for 1 hr followed by stimulation for 30 mins in presence of ATP by ELISA method
- ChEBML_32961 Effective concentration for retinoic acid receptor RAR alpha transcriptional activation
- ChEMBL_304261 (CHEMBL829031) Effective concentration for glucokinase activation with 5 mM glucose
- ChEMBL_304263 (CHEMBL829033) Effective concentration for glucokinase activation with 15 mM glucose
- ChEBML_196596 Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
- ChEMBL_195481 (CHEMBL798903) Transcriptional activation in CV-1 cells expressing RAR-beta receptor
- ChEMBL_195993 (CHEMBL800482) Transcriptional activation in CV-1 cells expressing RAR-gamma receptor
- ChEMBL_196479 (CHEMBL798293) Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
- ChEMBL_197392 (CHEMBL799711) Transcriptional activation in CV-1 cells expressing RAR-alpha receptor
- ChEMBL_44331 (CHEMBL654087) Transcriptional activation in CV-1 cells expressing human glucocorticoid receptor
- ChEMBL_1686332 (CHEMBL4036811) Activation of KCNQ2/3 (unknown origin)
- ChEMBL_1992346 (CHEMBL4626081) Allosteric activation of SIRT6 (unknown origin)
- ChEMBL_2074099 (CHEMBL4729633) Activation of mouse liver Glycogen phosphorylase
- ChEMBL_2236399 (CHEMBL5150295) Inhibition of mTOR (unknown origin) activation
- ChEMBL_2268098 Activation of SIRT6 (unknown origin) deacetylase activity
- ChEMBL_2316441 Activation of PPP5C (unknown origin) TPR domain
- ChEMBL_2344873 Activation of SIRT6 (unknown origin) deacetylase activity
- ChEMBL_2443866 Activation of CFTR F508del mutant (unknown origin)
- ChEMBL_304162 (CHEMBL830000) Activation of human farnesoid X receptor
- ChEMBL_887616 (CHEMBL2217225) Allosteric activation of human FSH receptor
- ChEMBL_972866 (CHEMBL2411643) Activation of GIRK1/2 (unknown origin)
- ChEMBL_972874 (CHEMBL2411651) Activation of GIRK1/4 (unknown origin)
- ChEMBL_1766509 (CHEMBL4201756) Activation of SOS1 in human NCI-H727 cells expressing KRAS G12V mutant assessed as induction of ERK1/2 T202/Y204 phosphorylation incubated for 30 mins by In-cell Western assay
- ChEMBL_1815979 (CHEMBL4315553) Activation of NRF2 in human U2OS cells co-expressing Keap1 (unknown origin) assessed as induction of NRF2 translocation to nucleus incubated for 6 hrs by beta-galactosidase based chemiluminescent assay
- ChEMBL_1824399 (CHEMBL4324163) Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774A.1 cells assessed as reduction in IL-1beta level incubated for 30 mins in presence of ATP by ELISA method
- ChEMBL_2152290 (CHEMBL5036837) Activation of wild-type human STING expressed in digitonin treated HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation by luciferase reporter gene assay
- ChEMBL_1699599 (CHEMBL4050581) Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay
- ChEMBL_1699601 (CHEMBL4050583) Antagonist activity at recombinant rat TRPV4 expressed in CHOK1 cells assessed as inhibition of 4alphaPDD-induced activation pretreated for 5 mins followed by 4alphaPDD stimulation measured for 5 mins by FLIPR assay
- ChEMBL_1457593 (CHEMBL3368443) Inhibition of PKCzeta in human U937 cells assessed as inhibition of TNFalpha-induced NF-kappaB activation by reporter gene assay
- ChEMBL_1473380 (CHEMBL3419340) Activation of tumorigenic wild type B-Raf in human IPC-298 cells with Ras mutation assessed as phosphorylation of ERK
- ChEMBL_209246 (CHEMBL814873) Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
- ChEMBL_2109871 (CHEMBL4818546) Activation of PXR (unknown origin) expressed in human DPX2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as induction of CYP3A4 transcriptional activity incubated for overnight by luminescence based analysis
- ChEBML_214951 In vitro inhibition of human T-cells voltage-gated potassium channel subunit Kv1.3
- ChEMBL_2132533 (CHEMBL4842048) Displacement of [125I]MIP-1beta from CCR5 in human peripheral T cells
- ChEMBL_460402 (CHEMBL927454) Displacement of [3H]nisoxetine from human NET t expressed in HEK293 cells
- ChEMBL_469648 (CHEMBL934326) Inhibition of human T-cell receptor zeta chain phosphorylation in Jurkat cells
- ChEMBL_495622 (CHEMBL1000314) Inhibition of recombinant perforin-mediated lysis of human Jurkat T cells by 51Cr release assay
- ChEMBL_304237 (CHEMBL841793) Caspase-3 activation activity tested in HT-29 cancer cells done for 24 or 48 hr at 37 degree C
- ChEMBL_304257 (CHEMBL829728) Caspase-3 activation activity tested in H1299 lung cancer cells done for 24 or 48 hr at 37 degree C
- ChEMBL_1849395 (CHEMBL4349936) Inverse agonist activity at RORgammat in mouse splenocytes derived naive T cells assessed as suppression of T cell differentiation to Th17 cells by measuring IL-17 secretion in presence of anti-CD4/anti-IFNgamma/TGFbeta/IL-6 for 6 days by ELISA
- ChEMBL_1453812 (CHEMBL3365189) Activation of AhR in human HepG2 cells assessed as fluorescence after 24 hrs incubation by EROD assay
- ChEMBL_1462967 (CHEMBL3398677) Activation of human PPARgamma ligand binding domain expressed in COS7 cells by dual luciferase reporter gene assay
- ChEMBL_1699612 (CHEMBL4050594) Antagonist activity at recombinant human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced activation
- ChEMBL_1722140 (CHEMBL4137140) Activation of GFP-tagged RasGRP1 (unknown origin) expressed in HEK293 cells after 30 mins by immunoblot method
- ChEMBL_1722141 (CHEMBL4137141) Activation of GFP-tagged RasGRP3 (unknown origin) expressed in HEK293 cells after 30 mins by immunoblot method
- ChEMBL_1921814 (CHEMBL4424659) Activation of human GIRK1/2 expressed in HEK293 cells co-expressing rat mGlu8 by thallium flux assay
- ChEMBL_1921816 (CHEMBL4424661) Activation of human GIRK1/4 expressed in HEK293 cells co-expressing rat mGlu8 by thallium flux assay
- ChEMBL_2272341 Activation of caspase 3 in human MDA-MB-231 cells measured after 48 hrs by Plate reader method
- ChEMBL_2293974 Antagonist activity at NOD2 in human HEK-Blue hNOD2 cells assessed as inhibition of MDP-induced NOD2 activation
- ChEMBL_2364945 Activation of N-terminal His-tagged human NAMPT-mediated NMN production expressed in Escherichia coli BL21(DE3) cells
- ChEMBL_2381124 Activation of Nrf2 in human PathHunter U2OS Keap1-Nrf2 cells assessed as Nrf2 nuclear translocation by chemiluminescent assay
- ChEMBL_2468461 Inhibition of NLRP3 inflammasome activation in mouse BMDM cells assessed as reduction in IL-1beta release by ELISA
- ChEMBL_313095 (CHEMBL836811) Inhibition of 10e-9 M E2 stimulated transcriptional activation in ER+MCF-7/2a breast cancer cells
- ChEMBL_313096 (CHEMBL836812) Inhibition of 10e-9 M E2 stimulated transcriptional activation in ER+MCF-7/2a breast cancer cells
- ChEMBL_402359 (CHEMBL867424) Activity at ERalpha L384M/M421G/G521R mutant in HeLa cells assessed as activation of SEAP reporter gene
- ChEMBL_478429 (CHEMBL932618) Inhibition of 1,10-phenanthroline-induced HIF1 activation in human T47D cells by cell based reporter gene assay
- ChEMBL_501553 (CHEMBL986820) Activation of mouse wild type TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium concentration
- ChEMBL_537144 (CHEMBL989804) Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
- ChEMBL_573857 (CHEMBL1056199) Inhibition of hypoxia-induced HIF1 activation in human Hep3B cells by pGL3-HRE-luciferase reporter gene assay
- ChEMBL_619005 (CHEMBL1101830) Inhibition of hypoxia-induced HIF1 activation in human T47D cells by pTK-HRE3-luciferase reporter gene assay
- ChEMBL_647729 (CHEMBL1220326) Inhibition of calcineurin-mediated streptavidin-coupled NFAT activation in human Jurkat cells by luciferase reporter gene assay
- ChEMBL_698465 (CHEMBL1647397) Inhibition of hypoxia-induced HIF1 activation in human T47D cells by HRE3-TK-luciferase reporter gene assay
- ChEMBL_698468 (CHEMBL1647400) Inhibition of hypoxia-induced HIF1 activation in human PC3 cells by HRE3-TK-luciferase reporter gene assay
- ChEMBL_770820 (CHEMBL1837625) Inhibition of hypoxia-induced HIF1alpha activation in human ME180 cells by HRE3-Bla-luciferase reporter gene assay
- ChEMBL_874808 (CHEMBL2188852) Activation of ERalpha in human MCF7/2a cells by luciferase reporter gene assay relative to untreated control
- ChEMBL_971018 (CHEMBL2404357) Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis
- ChEMBL_144025 (CHEMBL750440) Receptor activation after 10 uM application and 300 uM of ACh for Nicotinic acetylcholine receptor alpha7
- ChEMBL_144026 (CHEMBL750441) Receptor activation after 100 uM application and 300 uM of ACh for Nicotinic acetylcholine receptor alpha7
- ChEMBL_2467261 Activation of N-terminal 6His-tagged mouse NAMPT measured for 20 mins by fluorescence based spectrometer analysis
- ChEMBL_984799 (CHEMBL2432301) Allosteric activation of human glucokinase using glucose as substrate measured every 10 secs for 5 mins
- ChEMBL_2438144 Inhibition of NLRP3 inflammasome activation in LPS primed human differentiated THP-M cells derived PMA induced THP-1 cells assessed as inhibition of IL-1 beta level preincubated with compound for 24 hrs followed by LPS stimulation for 3 hrs and further incubated with ATP for 1 hr by ELISA method
- ChEMBL_945536 (CHEMBL2344013) Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assay
- ChEMBL_952779 (CHEMBL2351028) Inhibition of T-140 binding to CXCR4 (unknown origin) expressed in dog Cf2Th cells incubated for 30 mins prior to T-140 addition measured after 30 mins by fluorescence assay
- ChEMBL_2372376 Inhibition of NLRP3 inflammasome activation in LPS-treated human THP-1 cells assessed as inhibition of ATP-stimulated IL-1beta release at 1 uM incubated for 30 mins followed by ATP stimulation for 1 hr by ELISA method
- ChEMBL_2372156 Inhibition of IL-2 in human Jurkat T cells pretreated with compound for 16 hrs followed by anti-CD3 stimulation by ELISA analysis
- ChEMBL_2437757 Inhibition of human ROMK expressed in T-REX-CHO cells incubated for 3 to 8 mins by whole cell manual patch clamp assay
- ChEMBL_2496565 Inhibition of Kv1.3 (unknown origin) expressed in PBMC derived PHA-activated T-lymphocyte cells incubated for 5 days by manual patch clamp method
- ChEMBL_2363305 Inhibition of NLRP3 inflammasome activation in LPS-activated human PBMC cells assessed as inhibition of ATP/nigericin induced IL-1beta secretion preincubated with LPS for 3 hrs followed by compound addition for 30 mins and further stimulated with ATP for 1 hr by ELISA
- ChEMBL_2466742 Inhibition of NLRP3 inflammasome activation in LPS-activated mouse BMDM cells assessed as inhibition of nigericin induced IL-1beta secretion preincubated with LPS for 3 hrs followed by compound addition for 40 mins and further stimulated with nigericin for 40 mins by ELISA method
- ChEMBL_2466743 Inhibition of NLRP3 inflammasome activation in LPS-activated human PBMC cells assessed as inhibition of nigericin induced IL-1beta secretion preincubated with LPS for 3 hrs followed by compound addition for 40 mins and further stimulated with nigericin for 40 mins by ELISA method
- ChEMBL_1623557 (CHEMBL3865969) Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days by Hoechst 33258 staining based assay
- ChEMBL_1772646 (CHEMBL4229638) Activation of caspase cascade in human T47D cells using N-(Ac-DEVD)-N'-ethoxycarbonyl-R110 fluorogenic substrate incubated for 48 hrs by fluorescent plate reader based assay
- ChEMBL_1985011 (CHEMBL4618417) Inhibition of proMMP2 activation in human WM115 cells assessed as reduction in MMP2 activity at 0.1 nM to 1 uM incubated for 24 hrs by gelatin zymography
- ChEMBL_2160820 (CHEMBL5045570) Activation of STING pathway harboring WT/WT genotype in human PBMC cells assessed as increase in iFIT3 mRNA expression incubated for 6 hrs by RT-PCR analysis
- ChEMBL_2160821 (CHEMBL5045571) Activation of STING pathway harboring WT/HAQ genotype in human PBMC cells assessed as increase in iFIT3 mRNA expression incubated for 6 hrs by RT-PCR analysis
- ChEMBL_2160823 (CHEMBL5045573) Activation of STING pathway harboring WT/R232H genotype in human PBMC cells assessed as increase in iFIT3 mRNA expression incubated for 6 hrs by RT-PCR analysis
- ChEMBL_2160824 (CHEMBL5045574) Activation of STING pathway harboring WT/WT genotype in human PBMC cells assessed as increase in MX1 mRNA expression incubated for 6 hrs by RT-PCR analysis
- ChEMBL_2160825 (CHEMBL5045575) Activation of STING pathway harboring WT/HAQ genotype in human PBMC cells assessed as increase in MX1 mRNA expression incubated for 6 hrs by RT-PCR analysis
- ChEMBL_2160826 (CHEMBL5045576) Activation of STING pathway harboring WT/R232H genotype in human PBMC cells assessed as increase in MX1 mRNA expression incubated for 6 hrs by RT-PCR analysis
- ChEMBL_2307578 Activation of human wild-type CFTR stably expressed in rat FRT cells assessed as increase in apical membrane chloride current incubated for 20 mins by patch-clamp assay
- ChEMBL_2365557 Activation of SERCA2a in mouse HL-1 cells assessed as increase in caffeine-induced calcium release incubated for 2 hrs by FLIPR Calcium 6 dye based caffeine assay
- ChEMBL_328063 (CHEMBL863929) Inhibitory activity against dengue 2 NS3 protease fused via a linker to region of NS2B
- ChEMBL_154378 (CHEMBL758987) Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells
- ChEMBL_1699600 (CHEMBL4050582) Antagonist activity at recombinant human TRPV4 expressed in CHOK1 cells assessed as inhibition of hypotonicity-induced activation pretreated for 5 mins followed by hypotonic solution addition measured for 5 mins by FLIPR assay
- ChEMBL_2250050 (CHEMBL5164260) Inhibition of NLRP3 inflammasome activation in LPS-primed mouse BMDM cells assessed as reduction in ATP induced IL-1beta release pretreated for 15 mins followed by ATP stimulation for 30 mins by ELISA
- ChEMBL_460878 (CHEMBL944817) Blockade of N-arachidonoyl-dopamine-induced activation of TRPV1
- ChEMBL_162333 (CHEMBL768342) Compound was measured for the antagonism of the activation of phospholipase C in mutant(F226A) human P2Y1 receptor in presence of MRS2179.
- ChEMBL_162337 (CHEMBL768346) Compound was measured for the antagonism of the activation of phospholipase C in mutant(H277A) human P2Y1 receptor in presence of MRS2179
- ChEMBL_162339 (CHEMBL768348) Compound was measured for the antagonism of the activation of phospholipase C in mutant(K280A) human P2Y1 receptor in presence of MRS2179
- ChEMBL_162341 (CHEMBL768350) Compound was measured for the antagonism of the activation of phospholipase C in mutant(Q307A) human P2Y1 receptor in presence of MRS2179
- ChEMBL_162343 (CHEMBL768351) Compound was measured for the antagonism of the activation of phospholipase C in mutant(R310K) human P2Y1 receptor in presence of MRS2179
- ChEMBL_162345 (CHEMBL768353) Compound was measured for the antagonism of the activation of phospholipase C in mutant(S314T) human P2Y1 receptor in presence of MRS2179
- ChEMBL_162347 (CHEMBL768355) Compound was measured for the antagonism of the activation of phospholipase C in mutant(S317A) human P2Y1 receptor in presence of MRS2179
- ChEMBL_1334656 (CHEMBL3239856) Activation of human VR1 expressed in HEK293 cells assessed as stimulation of Ca2+ influx by Fluo-3 staining-based fluorescence assay
- ChEMBL_1619068 (CHEMBL3861237) Activation of human TRESK channel expressed in HEK293 cells assessed as induction of channel current by whole cell patch clamp assay
- ChEMBL_631037 (CHEMBL1113762) Inhibition of hypoxia-induced HIF1 activation in human T47D cells in presence of 1% O2 by HRE3-TK-luc reporter assay
- ChEMBL_792737 (CHEMBL1930652) Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting
- ChEMBL_792738 (CHEMBL1930653) Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by competitive binding assay
- ChEMBL_2578562 Inhibition of Itk in human Jurkat T cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA analysis
- ChEMBL_835400 (CHEMBL2072106) Inhibition of alpha4beta7 assessed as inhibition of Mn(2+)-activated adhesion of mouse TK-1 T cells to mouse MAdCAM-1 incubated for 1 hr by cell adhesion assay
- ChEMBL_1719030 (CHEMBL4134030) Activation of BTN3A1 in human PBMC-derived Vgamma9Vdelta2 T cells assessed as induction of interleukin 2 stimulated cell proliferation by measuring increase in CD3 positive cells incubated for 3 days followed by 11 days incubation post compound wash out with subsequent stimulation with IL-2 every 3 days measured after 14 days by flow cytometry
- ChEBML_195463 Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor alpha
- ChEBML_195653 Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR beta
- ChEBML_195832 Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta
- ChEBML_196497 Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
- ChEBML_196651 Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
- ChEBML_197086 Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta
- ChEBML_197247 Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma
- ChEMBL_153614 (CHEMBL759726) Transcriptional activation in COS cells expressing PPAR gamma and RXR alpha
- ChEMBL_196594 (CHEMBL800472) Transcriptional activation in CV-1 cells expressing Retinoid X receptor alpha
- ChEMBL_196596 (CHEMBL800474) Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
- ChEMBL_196892 (CHEMBL807544) In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
- ChEMBL_196895 (CHEMBL806514) In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
- ChEMBL_43804 (CHEMBL656374) Transcriptional activation in COS cells expressing PPAR gamma and RXR alpha
- ChEMBL_32961 (CHEMBL644525) Effective concentration for retinoic acid receptor RAR alpha transcriptional activation
- ChEMBL_39042 (CHEMBL652856) Effective concentration for retinoic acid receptor RAR beta transcriptional activation
- ChEMBL_70525 (CHEMBL681082) Effective concentration for retinoic acid receptor RAR gamma transcriptional activation
- ChEMBL_2461134 Agonist activity at human PPARgamma transfected in african green monkey COS7 cells assessed transcriptional activation incubated for 24 hrs by luciferase assay
- ChEMBL_304247 (CHEMBL829718) Caspase-3 activation activity tested in ZR-75-1 cancer cells done for 24 or 48 hr at 37 degree C
- ChEMBL_1616866 (CHEMBL3858935) Inhibition of LCK in human peripheral T cells assessed as suppression of TCR-dependant cell proliferation
- ChEMBL_629042 (CHEMBL1120946) Inhibition of LFA1-mediated adhesion of human T cells to ICAM1-expressing HUVEC by fluorescence assay
- ChEMBL_312359 (CHEMBL837472) Inhibitory activity against voltage-gated potassium channel subunit Kv1.3 of human T cells
- ChEMBL_331631 (CHEMBL862887) Displacement of [3H]MPEP from cloned human mGluR5 transfected in HEK293-T cells
- ChEMBL_350436 (CHEMBL861673) Inhibition of anti-CD3 antibody-induced IL2 production in human jurkat T cells
- ChEMBL_839632 (CHEMBL2090653) Inhibition of human recombinant CDK9/cyclin T expressed in baculovirus-infected insect cells
- ChEMBL_2207916 (CHEMBL5120624) Inhibition of JAK1/JAK3 in human primary T-cells assessed as reduction of IL-2 stimulated STAT5 phosphorylation preincubated for 1 hr followed by IL-2 stimulation for 15 mins by FACS method
- ChEBML_1690071 Activation of GAL4 fused human LXR alpha expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
- ChEBML_1690072 Activation of GAL4 fused human LXR beta expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
- ChEMBL_103159 (CHEMBL711304) Compound concentration required to induce transcriptional activation in MVLN cells comparable to 50% of 0.1 nM estradiol response
- ChEMBL_103160 (CHEMBL707870) Compound concentration required to induce transcriptional activation in MVLN cells equal to 50% of 0.1 nM estradiol response
- ChEMBL_1463242 (CHEMBL3399384) Activation of human TLR7 expressed in HEK293 cells after 24 hrs by NFkappaB-mediated SEAP reporter gene assay
- ChEMBL_1463243 (CHEMBL3399385) Activation of human TLR8 expressed in HEK293 cells after 24 hrs by NFkappaB-mediated SEAP reporter gene assay
- ChEMBL_1506134 (CHEMBL3596064) Activation of human TRPA1 expressed in TREx-HEK cells by Fluo-4 AM dye-based Ca2+ imaging assay
- ChEMBL_1506136 (CHEMBL3596066) Activation of human TRPV1 expressed in TREx-HEK cells by Fluo-4 AM dye-based Ca2+ imaging assay
- ChEMBL_1522887 (CHEMBL3630760) Antagonist activity at human TRPV1 heterologously expressed in CHO cells assessed as inhibition of low pH-induced activation
- ChEMBL_1584396 (CHEMBL3819817) Activation of TREK1 (unknown origin) expressed in HEK293 cells assessed as increase in current density relative to control
- ChEMBL_1722142 (CHEMBL4137142) Activation of GFP-tagged RasGRP1 (unknown origin) expressed in human LNCAP cells after 30 mins by immunoblot method
- ChEMBL_1722143 (CHEMBL4137143) Activation of GFP-tagged RasGRP3 (unknown origin) expressed in human LNCAP cells after 30 mins by immunoblot method
- ChEMBL_1722154 (CHEMBL4137154) Activation of RasGRP3 in human Ramos cells assessed as ERK1/2 phosphorylation after 30 mins by immunoblot method
- ChEMBL_1883887 (CHEMBL4385386) Activation of human homomeric KCNQ4 expressed in CHOK1 cells at -10 mV by whole cell patch clamp assay
- ChEMBL_2018158 (CHEMBL4671736) Activation of human sGC subunit alpha1/beta1 expressed in CHO cells assessed as cGMP production by CASA assay
- ChEMBL_2249001 (CHEMBL5163211) Positive allosteric modulator activity at human GLP-1R expressed in HEK293 cells assessed as activation of calcium flux
- ChEMBL_452324 (CHEMBL901549) Inhibition of hypoxia-induced HIF1 activation in human T47D cells after 16 hrs by cell based luciferase assay
- ChEMBL_515379 (CHEMBL1025534) Antagonist activity at TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced activation by FLIPR assay
- ChEMBL_515381 (CHEMBL1025536) Antagonist activity at TRPV1 expressed in HEK293 cells assessed as inhibition of PMA-induced activation by FLIPR assay
- ChEMBL_550357 (CHEMBL999911) Inhibition of hypoxia-induced HIF1 activation in human T47D cells after 16 hrs by luciferase reporter gene assay
- ChEMBL_620294 (CHEMBL1105079) Activation of progesterone receptor in human T47D cells after 20 hrs by PRE-tagged luciferase reporter gene assay
- ChEMBL_753564 (CHEMBL1799182) Inhibition of hypoxia-induced HIF1alpha activation in human Hep3B cells after 16 hrs by HRE-luciferase reporter assay
- ChEMBL_834995 (CHEMBL2073448) Transcriptional activation of ERalpha receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay
- ChEMBL_834996 (CHEMBL2073449) Transcriptional activation of ERbeta receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay
- ChEMBL_940885 (CHEMBL2330504) Activation of human RXRalpha activity expressed in COS1 cells after 12 hrs by RXRE-luciferase reporter gene assay
- ChEMBL_984148 (CHEMBL2432076) Antagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activation
- ChEMBL_1721223 (CHEMBL4136223) Inhibition of IL-6-Induced STAT3 activation (unknown origin) expressed in human HepG2 cells expressing pSTAT3-luciferase pre-incubated for 1 hr before IL-6 stimulation for 6 hrs by luciferase reporter gene assay
- ChEMBL_2217915 (CHEMBL5131047) Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse J774A.1 cells assessed as decrease in IL-1beta level pretreated for 0.5 hrs followed by stimulation with nigericin for 1 hr by ELISA
- ChEMBL_1509419 (CHEMBL3603427) Inhibition of TNFR in human THP1-XBlue cells containing NF-kappaB-inducible SEAP reporter gene assessed as inhibition of TNFalpha-induced TNFR activation incubated at 37 degC for 1 hr by spectrophotometry
- ChEMBL_1849764 (CHEMBL4350305) Activation of human AMPK alpha1/beta1/gamma1 expressed in baculovirus/Sf9 cells using SAMS peptide as substrate incubated for 15 mins by in presence of 33P-ATP by liquid scintillation counting method
- ChEMBL_2498443 Displacement of [3H]-Mesulergine from human 5-HT2C expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 1 hr
- ChEBML_139551 Activation of murine PPAR alpha ligand binding domain
- ChEBML_139552 Activation of murine PPAR delta ligand binding domain
- ChEBML_139553 Activation of murine PPAR gamma ligand binding domain
- ChEBML_153232 Maximum transcriptional activation of human PPAR gamma receptor
- ChEBML_153401 Maximum transcriptional activation of human PPAR alpha receptor
- ChEBML_1619071 Activation of human TRESK channel relative to control
- ChEBML_195193 Transcriptional activation of retinoic acid receptor RAR alpha
- ChEBML_195650 Transcriptional activation of retinoic acid receptor RAR beta
- ChEBML_196170 Transcriptional activation of retinoic acid receptor RAR gamma
- ChEMBL_1461012 (CHEMBL3395070) Activation of human recombinant AMPK alpha1 subunit
- ChEMBL_1467479 (CHEMBL3411102) Activation of MOR in guinea pig ileum
- ChEMBL_1467482 (CHEMBL3411105) Activation of DOR in mouse vas deferens
- ChEMBL_1477926 (CHEMBL3429347) Activation of Staphylococcus aureus FtsZ GTPase activity
- ChEMBL_17044 (CHEMBL630618) Activation of cAMP dependent protein kinase (PKA)
- ChEMBL_217013 (CHEMBL821548) Activation of cAMP dependent protein kinase (PKA)
- ChEMBL_220890 (CHEMBL824645) In vitro transcriptional activation of hPPAR delta
- ChEMBL_2297895 Activation of Kir6.2/SUR1 (unknown origin) channel opening
- ChEMBL_2432610 Inhibition of NLRP3 inflammasome activation in mouse BMDMs
- ChEMBL_305437 (CHEMBL830113) Inhibition of Fibroblast activation protein alpha (seprase)
- ChEMBL_476696 (CHEMBL933486) Activation of procaspase 2 after 24 hrs
- ChEMBL_479067 (CHEMBL933818) Activation of SIRT2 by mass spectrometry assay
- ChEMBL_479068 (CHEMBL933819) Activation of SIRT3 by mass spectrometry assay
- ChEMBL_567195 (CHEMBL1029107) Activation of human CYP3A4 using DEF substrate
- Inhibition Assay Inhibition assay of olfactory receptors 17 activation.
- ChEBML_72305 Compound was tested for the inhibition of Escherichia coli glutamyl-t-RNA synthetase
- ChEMBL_2152295 (CHEMBL5036842) Activation of wild-type human STING expressed in HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 30 mins by luciferase reporter gene assay
- ChEMBL_2152297 (CHEMBL5036844) Activation of wild-type human STING expressed in HEK293T cells co-expressing IRF3-activated ISRE assessed as IRF3 reporter activation measured after 7 hrs by luciferase reporter gene assay
- ChEMBL_1778844 (CHEMBL4235836) Inhibition of PDGF-BB-induced PDGFRbeta activation in human SH-SY5Y cells pretreated for 60 mins followed by PDGF-BB addition and measured after 10 mins by ELISA
- ChEMBL_2033602 (CHEMBL4687760) Inhibition of Pam3CSK4-induced TLR1/TLR2 activation in mouse RAW 264.7 cells assessed as reduction in NO production incubated for 24 hrs by 2,3-diaminonaphthalene reagent based assay
- ChEMBL_2115840 (CHEMBL4824781) Activation of GLP1R (unknown origin) CRE-bla expressed in CHO-K1 cells assessed as receptor potency incubated for 1 hrs by time resolved fluorescence resonance energy transfer immunoassay
- ChEMBL_2116578 (CHEMBL4825519) Activation of PPARalpha LBD (unknown origin) co-expressed with Gal4UAS-luciferase reporter in HEK293 cells incubated for 24 hrs by Steady-Glo luciferase reporter gene based luminescence analysis
- ChEMBL_2116579 (CHEMBL4825520) Activation of PPARgamma LBD (unknown origin) co-expressed with Gal4UAS-luciferase reporter in HEK293 cells incubated for 24 hrs by Steady-Glo luciferase reporter gene based luminescence analysis
- ChEMBL_2116580 (CHEMBL4825521) Activation of PPARdelta LBD (unknown origin) co-expressed with Gal4UAS-luciferase reporter in HEK293 cells incubated for 24 hrs by Steady-Glo luciferase reporter gene based luminescence analysis
- ChEMBL_2487605 Inhibition of NLuc-fused DNMT1 expressed hypomorphic in human HCT-116 cells assessed as TSG repoter activation at 3 uM incubated for 72 hrs by Nano-Glo Luciferase assay
- ChEMBL_851752 (CHEMBL2156220) Activation of human HIF1alpha expressed in DFX-induced human U2OS cells incubated for 30 mins prior to DFX-induction measured after overnight incubation by luciferase reporter gene assay
- ChEMBL_27784 (CHEMBL645920) Binding affinity for adenosine A2 receptor using [3H]- NECA antagonism of adenylate cyclase activation in human platelets
- ChEMBL_1972898 (CHEMBL4605716) Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated B cells activation by measuring reduction in CD69 expression
- ChEMBL_1972899 (CHEMBL4605717) Inhibition of SYK (unknown origin) in B cells assessed as reduction in alpha IgM-stimulated B cells activation by measuring reduction in CD86 expression
- ChEMBL_2466688 Inhibition of NLRP3 inflammasome activation in LPS-activated human THP-1 cells assessed as inhibition of nigericin induced IL-1beta secretion preincubated with LPS for 3 hrs followed by compound addition for 40 mins and further stimulated with nigericin for 40 mins by ELISA method
- ChEMBL_2478784 Inhibition of NLRP3 inflammasome activation in PMA-differentiated human THP-1 cells assessed as inhibition of LPS/nigericin induced IL-1beta production preincubated with LPS for 4 hrs followed by compound addition for 30 mins and further incubated with nigericin for 30 mins by ELISA
- ChEMBL_1838909 (CHEMBL4339042) Inhibition of TGFbetaR1 in TGFbeta-stimulated human T cells assessed as reduction in SMAD3 phosphorylation preincubated for 1 hr followed by TGFbeta-stimulation for 90 mins by Alphalisa assay
- ChEBML_209980 Tested for inhibitory activity against thymidylate synthase of L1210 cells
- ChEMBL_65879 (CHEMBL681171) Affinity for estrogen receptor of human MCF-7 cells
- ChEMBL_1287611 (CHEMBL3110493) Activation of mouse wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
- ChEMBL_1287612 (CHEMBL3110494) Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
- ChEMBL_1487565 (CHEMBL3531532) Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
- ChEMBL_2018163 (CHEMBL4671741) Activation of human sGC subunit alpha1/beta1 expressed in CHO cells assessed as cGMP production in presence of ODQ by CASA assay
- ChEMBL_439940 (CHEMBL890257) Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
- ChEMBL_439941 (CHEMBL890258) Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
- ChEMBL_519767 (CHEMBL955373) Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
- ChEMBL_519771 (CHEMBL957801) Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
- ChEMBL_769902 (CHEMBL1831995) Inhibition of PKCzeta in human U937 cells assessed as inhibition of TNF-alpha-induced NF-kB activation by luciferase reporter gene assay
- ChEMBL_792740 (CHEMBL1930655) Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting
- ChEMBL_839692 (CHEMBL2089519) Activation of SHh in mouse Light2 cells assessed as induction of Gli-mediated luciferase activity after 24 hrs by reporter gene assay
- ChEMBL_1503827 (CHEMBL3592811) Activation of PXR (unknown origin) assessed as induction of CYP3A4
- ChEMBL_951257 (CHEMBL2353483) Inhibition of MDM2 (unknown origin) assessed as activation of p53
- ChEMBL_1993914 (CHEMBL4627809) Inverse agonist activity at RORgammat in human CD4-positive T cells assessed as suppression of T cell differentiation to Th17 cells by reduction in measuring IL-17A secretion
- ChEMBL_2035337 (CHEMBL4689495) Inhibition of HPK1 in anti-CD3/anti-CD28-stimulated human T-cells assessed as inhibition of SLP76 phosphorylation preincubated for 1 hr followed by anti-CD3/CD28 stimulation for 30 mins by AlphaLISA assay
- ChEMBL_2217914 (CHEMBL5131046) Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse J774A.1 cells assessed as decrease in LDH release pretreated for 0.5 hrs followed by stimulation with nigericin for 1 hr by LDH release assay
- ChEMBL_2109737 (CHEMBL4818412) Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse BMDM cells assessed as inhibition of LPS and nigericin-induced IL-1beta production pre-treated for 1 hr measured after 1 hr of stimulation by ELISA
- ChEMBL_2155360 (CHEMBL5040020) Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
- ChEMBL_1623558 (CHEMBL3865970) Activation of NQO1 in human A549 cells assessed as decrease in cell survival incubated for 2 hrs measured after 7 days in presence of NQO1 inhibitor dicoumarol by Hoechst 33258 staining based assay
- ChEMBL_2539530 Activation of PKC in human U1 cells infected with latent HIV-1 assessed as reversal of HIV-1 latency by measuring increase in p24 antigen level incubated for 48 hrs by chemiluminescent enzyme immunoassay
- ChEMBL_1435524 (CHEMBL3385344) Inhibition of LPS-induced TLR4 activation (unknown origin) expressed in HEK293 Blue cells compound treated for 30 mins prior LPS treatment measured after 2 to 4 hrs by spectrophotometry
- ChEMBL_1504485 (CHEMBL3590825) Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
- ChEMBL_1504487 (CHEMBL3590827) Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
- ChEMBL_1742295 (CHEMBL4158045) Inhibition of IFNgamma-stimulated STAT3 activation in human AD293 cells incubated with IFNgamma for 16 hrs followed by compound addition measured after 24 hrs by luciferase reporter gene assay
- ChEMBL_1742299 (CHEMBL4158049) Inhibition of IFNgamma-stimulated STAT3 activation in human HeLa cells incubated with IFNgamma for 16 hrs followed by compound addition measured after 24 hrs by luciferase reporter gene assay
- ChEMBL_2034105 (CHEMBL4688263) Inhibition of exogenous human TNFalpha in HEK-Blue-CD40L cells assessed as reduction in TNF-alpha-induced NFkappaB activation incubated for 18 hrs by quanti-blue based SEAP assay
- ChEMBL_2116581 (CHEMBL4825522) Activation of human LXRalpha co-expressed with TK-luciferase reporter in African green monkey CV-1 cells incubated for overnight by Steady-Glo luciferase reporter gene based luminescence analysis
- ChEMBL_2116582 (CHEMBL4825523) Activation of human LXRbeta co-expressed with TK-luciferase reporter in African green monkey CV-1 cells incubated for overnight by Steady-Glo luciferase reporter gene based luminescence analysis
- ChEMBL_2279563 Agonist activity at human PXR in human HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as transcriptional activation incubated for 24 hrs by luminescence based analysis
- ChEMBL_2279659 Agonist activity at human muscarinic M3 receptor expressed in human HEK293T cells assessed as activation of G-protein signaling by measuring inositol accumulation incubated for 90 mins by HTRF assay
- ChEMBL_2325367 Antagonist activity at wild type androgen receptor expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of androgen receptor incubated for 24 hrs by Steady-Glo assay
- ChEMBL_2325369 Antagonist activity at androgen receptor F876L mutant expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of androgen receptor incubated for 24 hrs by Steady-Glo assay
- ChEMBL_2325371 Antagonist activity at androgen receptor W741L mutant expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of androgen receptor incubated for 24 hrs by Steady-Glo assay
- ChEMBL_2325373 Antagonist activity at androgen receptor T877A mutant expressed in HEK293 cells assessed as reduction in DHT-induced transcriptional activation of androgen receptor incubated for 24 hrs by Steady-Glo assay
- ChEMBL_2377983 Agonist activity at TLR7 in human HEK-Blue hTLR7 cells assessed as activation of NF-kappaB incubated for 20 hrs by SEAP reporter gene based quanti-blue reagent spectrophotometric analysis
- ChEMBL_2499846 Activation of N-terminal His-tagged recombinant human SIRT1 (193 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 15 to 45 mins by luminescence based assay
- ChEMBL_2315757 Inhibition of CYP1B1 (unknown origin) expressed in HEK293-T-REx cells co-expressing POR incubated for 1 hr by resorufin dye based plate reader analysis
- ChEMBL_2315758 Inhibition of CYP1A1 (unknown origin) expressed in HEK293-T-REx cells co-expressing POR incubated for 1 hr by resorufin dye based plate reader analysis
- ChEBML_196753 Transcriptional activation in CV-1 cells expressing human Retinoid X receptor RXR-alpha
- ChEBML_197221 Transcriptional activation in CV-1 cells expressing mouse Retinoid X receptor RXR gamma
- ChEBML_67352 Agonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha
- ChEMBL_163471 (CHEMBL772306) Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR alpha
- ChEMBL_163475 (CHEMBL772310) Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR beta
- ChEMBL_163479 (CHEMBL772314) Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR gamma
- ChEMBL_164850 (CHEMBL769008) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
- ChEMBL_164860 (CHEMBL772119) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta
- ChEMBL_164862 (CHEMBL772121) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
- ChEMBL_195182 (CHEMBL801815) Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR alpha
- ChEMBL_195183 (CHEMBL801816) Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR alpha
- ChEMBL_195197 (CHEMBL798387) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha
- ChEMBL_195302 (CHEMBL884092) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha
- ChEMBL_195305 (CHEMBL799861) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha
- ChEMBL_195309 (CHEMBL799864) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha
- ChEMBL_195638 (CHEMBL795956) Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR beta
- ChEMBL_195639 (CHEMBL795957) Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR beta
- ChEMBL_195652 (CHEMBL796047) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta
- ChEMBL_195653 (CHEMBL796048) Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR beta
- ChEMBL_195655 (CHEMBL796050) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta
- ChEMBL_195795 (CHEMBL802395) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta
- ChEMBL_195799 (CHEMBL802570) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta
- ChEMBL_196161 (CHEMBL804934) Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR gamma
- ChEMBL_196162 (CHEMBL804935) Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR gamma
- ChEMBL_196163 (CHEMBL804936) Transcriptional activation in CV-1 cells expressing retinoic A receptor RAR gamma
- ChEMBL_196173 (CHEMBL804946) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma
- ChEMBL_196174 (CHEMBL804947) Transcriptional activation in CV-1 cells expressing retinoic acid receptor RAR gamma
- ChEMBL_196176 (CHEMBL804949) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma
- ChEMBL_196179 (CHEMBL804952) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma
- ChEMBL_196310 (CHEMBL805025) Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma
- ChEMBL_196492 (CHEMBL798306) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
- ChEMBL_196493 (CHEMBL798307) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
- ChEMBL_196494 (CHEMBL798308) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
- ChEMBL_196497 (CHEMBL798311) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
- ChEMBL_196601 (CHEMBL799679) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
- ChEMBL_196633 (CHEMBL879143) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta
- ChEMBL_196647 (CHEMBL800760) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
- ChEMBL_196650 (CHEMBL800763) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
- ChEMBL_196651 (CHEMBL800764) Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
- ChEMBL_196903 (CHEMBL807187) Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR alpha
- ChEMBL_197074 (CHEMBL806662) Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta
- ChEMBL_197231 (CHEMBL801377) Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma
- ChEMBL_67355 (CHEMBL676810) Agonist effect on transcriptional activation in T47D cells expressing estrogen receptor alpha
- ChEMBL_1476521 (CHEMBL3428072) Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced activation by FLIPR assay
- ChEMBL_1476522 (CHEMBL3428073) Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of pH-induced activation by FLIPR assay
- ChEMBL_1487568 (CHEMBL3531874) Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
- ChEMBL_1520354 (CHEMBL3624092) Agonist activity at human TLR8 transfected in HEK293 cells assessed as activation of NF-kB by reporter gene assay
- ChEMBL_1747068 (CHEMBL4181578) Activation of human PPARdelta LBD expressed in CHO-K1 cells by beta galactosidase enzyme fragment complement based fluorescence assay
- ChEMBL_1747072 (CHEMBL4181582) Activation of human PPARalpha LBD expressed in CHO-K1 cells by beta galactosidase enzyme fragment complement based fluorescence assay
- ChEMBL_1747074 (CHEMBL4181584) Activation of human PPARgamma LBD expressed in CHO-K1 cells by beta galactosidase enzyme fragment complement based fluorescence assay
- ChEMBL_2117575 (CHEMBL4826641) Inhibition of TNFalpha-induced IKKbeta mediated NF-kappaB activation in human Pancreatic cancer cells by luciferase reporter gene assay
- ChEMBL_2292796 Agonist activity at human TRMP8 expressed in HEK293 cells measured after 24 hrs of menthol activation by patch clamp assay
- ChEMBL_2292797 Agonist activity at human TRMP8 expressed in HEK293 cells measured after 24 hrs of cold activation by patch clamp assay
- ChEMBL_461292 (CHEMBL927311) Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
- ChEMBL_501715 (CHEMBL981463) Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
- ChEMBL_501717 (CHEMBL982353) Activation of human dopamine D2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
- ChEMBL_536039 (CHEMBL991609) Activation of human GLP1R expressed in HEK293 cells assessed as effect on cAMP responsive element promoter driven luciferase expression
- ChEMBL_562894 (CHEMBL1018831) Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR
- ChEMBL_610119 (CHEMBL1074484) Activation of ERalpha-mediated ERE activity in human T47D/neo cells after 18 hrs by luciferase reporter gene assay
- ChEMBL_610892 (CHEMBL1065047) Inhibition of hypoxia-induced HIF1alpha activation in human HeLa cells after 12 hrs by HRE-luciferase reporter gene assay
- ChEMBL_67194 (CHEMBL678129) In vitro inhibition of 1 nM 17-beta-estradiol induced transcriptional activation in T47D cells expressing estrogen receptor beta
- ChEMBL_698466 (CHEMBL1647398) Inhibition of 1, 10-phenanthroline-induced HIF1 activation in human T47D cells by HRE3-TK-luciferase reporter gene assay
- ChEMBL_698469 (CHEMBL1647401) Inhibition of 1, 10-phenanthroline-induced HIF1 activation in human PC3 cells by HRE3-TK-luciferase reporter gene assay
- ChEMBL_789883 (CHEMBL1925190) Inhibition of acid-induced matriptase activation in human 184A1N4 cells using mAb M69 by cell-based ELISA like assay
- ChEMBL_792744 (CHEMBL1930659) Activation of human TAAR1 expressed in human HEK293T cells assessed as cAMP accumulation after 10 mins by BRET assay
- ChEMBL_851754 (CHEMBL2156222) Activation of human HIF1alpha expressed in human U2OS cells assessed as increase in VEGF expression by RT-PCR analysis
- ChEMBL_874806 (CHEMBL2188850) Activation of human ERalpha expressed in human U2-OS cells by luciferase reporter gene assay relative to untreated control
- ChEMBL_874815 (CHEMBL2188859) Activation of human ERbeta expressed in human U2-OS cells by luciferase reporter gene assay relative to untreated control
- ChEMBL_980171 (CHEMBL2424209) Activation of GIRK1/4 (unknown origin) transfected in HEK293 cells after 4 mins by thallium flux-based fluorescence assay
- ChEMBL_980173 (CHEMBL2424211) Activation of GIRK1/2 (unknown origin) transfected in HEK293 cells after 4 mins by thallium flux-based fluorescence assay
- ChEMBL_162331 (CHEMBL766586) Compound was measured for the antagonism of the activation of phospholipase C in mutant(F131A) human P2Y1 receptor in presence of MRS2179 (P<0.05)
- ChEMBL_162335 (CHEMBL768344) Compound was measured for the antagonism of the activation of phospholipase C in mutant(H132A) human P2Y1 receptor in presence of MRS2179 (P<0.005)
- ChEMBL_162349 (CHEMBL768357) Compound was measured for the antagonism of the activation of phospholipase C in mutant(T221A) human P2Y1 receptor in presence of MRS2179 (P<0.005)
- ChEMBL_162351 (CHEMBL768359) Compound was measured for the antagonism of the activation of phospholipase C in mutant(T222A) human P2Y1 receptor in presence of MRS2179 (P<0.005)
- ChEMBL_162353 (CHEMBL768361) Compound was measured for the antagonism of the activation of phospholipase C in mutant(WT) human P2Y1 receptor in presence of MRS2179 (P<0.005)
- ChEMBL_162355 (CHEMBL768363) Compound was measured for the antagonism of the activation of phospholipase C in mutant(Y136A) human P2Y1 receptor in presence of MRS2179 (P<0.005)
- ChEBML_195473 Agonist activity for retinoic acid receptor RAR beta in transcriptional activation assay
- ChEBML_195985 Agonist activity for retinoic acid receptor RAR gamma in transcriptional activation assay
- ChEBML_196628 Agonist activity for retinoic acid receptor RXR alpha in transcriptional activation assay
- ChEBML_197054 Agonist activity for retinoic acid receptor RXR beta in transcriptional activation assay
- ChEBML_197215 Agonist activity for retinoic acid receptor RXR gamma in transcriptional activation assay
- ChEBML_197380 Agonist activity for retinoic acid receptor RAR alpha in transcriptional activation assay
- ChEMBL_139142 (CHEMBL743989) Agonist activity for murine PPAR alpha receptor in transcriptional activation assay
- ChEMBL_139147 (CHEMBL747680) Agonist activity for murine PPAR delta receptor in transcriptional activation assay
- ChEMBL_139152 (CHEMBL747685) Agonist activity for murine PPAR gamma receptor in transcriptional activation assay
- ChEMBL_88427 (CHEMBL700787) Agonist activity for Human PPAR alpha receptor in transcriptional activation assay
- ChEMBL_88431 (CHEMBL879147) Agonist activity for Human PPAR delta receptor in transcriptional activation assay
- ChEMBL_88436 (CHEMBL701905) Agonist activity for Human PPAR gamma receptor in transcriptional activation assay
- ChEMBL_90223 (CHEMBL697068) Agonist activity for Human PPAR gamma receptor in transcriptional activation assay
- ChEBML_1582258 Activation of human liver cathepsin L using Z-FR-AMC as substrate measured for 120 mins by fluorescence assay
- ChEMBL_1901853 (CHEMBL4404075) Activation of LasR in Pseudomonas aeruginosa PAO-JP2 harboring plasI-LVAgfp incubated for 6 hrs by fluorescence method
- ChEMBL_2224223 (CHEMBL5137736) Activation of PKM2 (unknown origin) Leu353, Tyr390, Phe26 residues incubated for 30 mins by ATP colorimetric/fluorometric assay
- ChEMBL_2268025 Activation of recombinant human PP5 (16 to 499 residues) Escherichia coli BL21 (DE3) using pNPP incubated for 60 mins
- ChEMBL_2268104 Activation of SIRT6 (unknown origin) deacetylase activity using EALPKK-Myr-AMC substrate incubated for 2 hrs by FDL assay
- ChEMBL_746784 (CHEMBL1776953) Binding affinity to human XIAP linker BIR2-BIR3 domain expressed in Escherichia coli BL21(DE3) cells by fluorescence polarization-based assay
- Activation Assay Activation of p38 kinase assay was measured by fluorescence emission using a Perkin-Elmer LS 50B fluorimeter.
- ChEMBL_1447676 (CHEMBL3375012) Displacement of [3H]GR100679 from NK2 receptor (unknown origin) expressed in CHO/T cells