CAP (E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnon-6-enamide Capsaicin (6E)-N-[(4-hydroxy-3-methoxyphenyl)methyl]-8-methylnon-6-enamide BDBM20461 CHEMBL294199 Zostrix
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- Borthwick, AD; Exall, AM; Haley, TM; Jackson, DL; Mason, AM; Weingarten, GG Pyrrolidine-5,5-trans-lactams as novel mechanism-based inhibitors of human cytomegalovirus protease. Part 3: potency and plasma stability. Bioorg Med Chem Lett 12: 1719-22 (2002)
- Bist, G; Luong, NT; Mahabubur Rahman, KM; Ruszaj, DM; Li, C; Hanigan, MH; You, Y SAR of L-ABBA analogs for GGT1 inhibitory activity and L-ABBA's effect on plasma cysteine and GSH species. Bioorg Med Chem Lett 92: (2023)
- Miranda, LP; Winters, KA; Gegg, CV; Patel, A; Aral, J; Long, J; Zhang, J; Diamond, S; Guido, M; Stanislaus, S; Ma, M; Li, H; Rose, MJ; Poppe, L; Véniant, MM Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity. J Med Chem 51: 2758-65 (2008)
- Nisato, D; Wagnon, J; Callet, G; Mettefeu, D; Assens, JL; Plouzane, C; Tonnerre, B; Pliska, V; Fauchère, JL Renin inhibitors. Free-Wilson and correlation analysis of the inhibitory potency of a series of pepstatin analogues on plasma renin. J Med Chem 30: 2287-91 (1988)
- Kotian, PL; Wu, M; Vadlakonda, S; Chintareddy, V; Lu, P; Juarez, L; Kellogg-Yelder, D; Chen, X; Muppa, S; Chambers-Wilson, R; Davis Parker, C; Williams, J; Polach, KJ; Zhang, W; Raman, K; Babu, YS Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE). J Med Chem 64: 12453-12468 (2021)
- Schäfer, H; Schwarzhoff, R; Creutzfeldt, W; Schmidt, WE Characterization of a guanosine-nucleotide-binding-protein-coupled receptor for pituitary adenylate-cyclase-activating polypeptide on plasma membranes from rat brain. Eur J Biochem 202: 951-8 (1991)
- Garcia-Barrantes, PM; Cho, HP; Blobaum, AL; Niswender, CM; Conn, PJ; Lindsley, CW Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs. Bioorg Med Chem Lett 26: 1869-72 (2016)
- Fischer, C; Lamer, T; Wang, W; McKinnie, SMK; Iturrioz, X; Llorens-Cortes, C; Oudit, GY; Vederas, JC Plasma kallikrein cleaves and inactivates apelin-17: Palmitoyl- and PEG-extended apelin-17 analogs as metabolically stable blood pressure-lowering agents. Eur J Med Chem 166: 119-124 (2019)
- Xu, P; Xu, M; Jiang, L; Yang, Q; Luo, Z; Dauter, Z; Huang, M; Andreasen, PA Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor. J Med Chem 58: 8868-76 (2015)
- Colombo, D; Tringali, C; Franchini, L; Cirillo, F; Venerando, B Glycoglycerolipid analogues inhibit PKC translocation to the plasma membrane and downstream signaling pathways in PMA-treated fibroblasts and human glioblastoma cells, U87MG. Eur J Med Chem 46: 1827-34 (2011)
- McKinnie, SMK; Wang, W; Fischer, C; McDonald, T; Kalin, KR; Iturrioz, X; Llorens-Cortes, C; Oudit, GY; Vederas, JC Synthetic Modification within the"RPRL" Region of Apelin Peptides: Impact on Cardiovascular Activity and Stability to Neprilysin and Plasma Degradation. J Med Chem 60: 6408-6427 (2017)
- Vacondio, F; Silva, C; Lodola, A; Carmi, C; Rivara, S; Duranti, A; Tontini, A; Sanchini, S; Clapper, JR; Piomelli, D; Tarzia, G; Mor, M Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability. Eur J Med Chem 46: 4466-73 (2011)
- Obeng, S; Kamble, SH; Reeves, ME; Restrepo, LF; Patel, A; Behnke, M; Chear, NJ; Ramanathan, S; Sharma, A; León, F; Hiranita, T; Avery, BA; McMahon, LR; McCurdy, CR Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. J Med Chem 63: 433-439 (2020)
- Wong, AK; Finch, AM; Pierens, GK; Craik, DJ; Taylor, SM; Fairlie, DP Small molecular probes for G-protein-coupled C5a receptors: conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a. J Med Chem 41: 3417-25 (1998)
- Kobayashi, T; Sasaki, S; Tomita, N; Fukui, S; Nakayama, M; Kiba, A; Kusaka, M; Matsumoto, S; Yamaguchi, M; Itoh, F; Baba, A 2-acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats. Bioorg Med Chem 18: 5157-71 (2010)
- Davie, RL; Edwards, HJ; Evans, DM; Hodgson, ST; Stocks, MJ; Smith, AJ; Rushbrooke, LJ; Pethen, SJ; Roe, MB; Clark, DE; McEwan, PA; Hampton, SL Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema. J Med Chem 65: 13629-13644 (2022)
- Borthwick, AD; Davies, DE; Ertl, PF; Exall, AM; Haley, TM; Hart, GJ; Jackson, DL; Parry, NR; Patikis, A; Trivedi, N; Weingarten, GG; Woolven, JM Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability. J Med Chem 46: 4428-49 (2003)
- Di Maro, S; Trotta, AM; Brancaccio, D; Di Leva, FS; La Pietra, V; Ieranò, C; Napolitano, M; Portella, L; D'Alterio, C; Siciliano, RA; Sementa, D; Tomassi, S; Carotenuto, A; Novellino, E; Scala, S; Marinelli, L Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists. J Med Chem 59: 8369-80 (2016)
- Shi, Y; Li, J; Kennedy, LJ; Tao, S; Hernández, AS; Lai, Z; Chen, S; Wong, H; Zhu, J; Trehan, A; Lim, NK; Zhang, H; Chen, BC; Locke, KT; O'Malley, KM; Zhang, L; Srivastava, RA; Miao, B; Meyers, DS; Monshizadegan, H; Search, D; Grimm, D; Zhang, R; Harrity, T; Kunselman, LK; Cap, M; Muckelbauer, J; Chang, C; Krystek, SR; Li, YX; Hosagrahara, V; Zhang, L; Kadiyala, P; Xu, C; Blanar, MA; Zahler, R; Mukherjee, R; Cheng, PT; Tino, JA ACS Med Chem Lett 7: 590-4 (2016)
- ChEMBL_823236 (CHEMBL2040654) Inhibition of cap 1 ALMV primed Influenza transcriptase
- ChEMBL_823246 (CHEMBL2040664) Inhibition of cap 1 ALMV primed Influenza transcriptase
- ChEMBL_823247 (CHEMBL2040665) Inhibition of cap 1 ALMV primed Influenza transcriptase
- ChEBML_195967 Plasma renin inhibitory activity was evaluated in lyophilized human plasma with 0.1%EDTA
- ChEMBL_157581 (CHEMBL763331) Inhibitory concentration against cap-dependent endonuclease activity of influenza virus RNP
- ChEBML_154901 Inhibition of human plasma renin
- ChEBML_1769525 Inhibition of human plasma kallikrein
- ChEBML_192887 Inhibition of monkey plasma renin
- ChEBML_195744 Inhibition of human plasma renin
- ChEBML_195753 Inhibition of human plasma renin
- ChEBML_195771 Inhibition of Human plasma renin
- ChEBML_195778 Inhibition of human plasma renin.
- ChEBML_195957 Inhibition of human plasma renin
- ChEBML_196306 Inhibition against rat plasma renin.
- ChEBML_196421 Selectivity against rat plasma renin
- ChEBML_196430 Selectivity against sheep plasma renin
- ChEMBL_2297247 Inhibition of human plasma renin
- ChEMBL_2344480 Inhibition of human plasma BChE
- ChEMBL_760109 (CHEMBL1810432) Inhibition of plasma kallikrein
- ChEMBL_776037 (CHEMBL1912507) Inhibition of plasma kallikrein
- ChEMBL_792623 (CHEMBL1930264) Inhibition of plasma kallikrein
- ChEMBL_809738 (CHEMBL2016157) Inhibition of plasma kallikrein
- ChEMBL_1995301 (CHEMBL4629196) Inhibition of human plasma renin assessed as reduction in endogenous angiotensin 1 production in plasma
- ChEMBL_220754 (CHEMBL841914) Inhibitory concentration against cap-dependent endonuclease activity of influenza B/Lee/40 RNP
- ChEMBL_1286473 (CHEMBL3112345) Competitive antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx preincubated for 3 mins followed by CAP challenge by Schlid plot analysis
- ChEBML_192728 Inhibitory activity against monkey plasma renin.
- ChEBML_195941 Inhibitory activity against human plasma renin
- ChEBML_195944 Inhibitory activity against human plasma renin.
- ChEBML_208491 Inhibition of thrombin in human plasma
- ChEMBL_1449330 (CHEMBL3372058) Inhibition of human plasma kallikrein
- ChEMBL_1461144 (CHEMBL3395469) Inhibition of human plasma kallikrein
- ChEMBL_1548351 (CHEMBL3756135) Inhibition of human plasma kallikrein
- ChEMBL_154908 (CHEMBL873412) Binding affinity against plasma thrombin
- ChEMBL_157260 (CHEMBL765460) Inhibitory activity against plasma kallikrein
- ChEMBL_157262 (CHEMBL765462) Binding affinity against plasma kallikrein.
- ChEMBL_1623083 (CHEMBL3865435) Inhibition of human plasma kallikrein
- ChEMBL_1663614 (CHEMBL4013295) Inhibition of human plasma kallikrein
- ChEMBL_1671401 (CHEMBL4021430) Inhibition of human plasma DPP4
- ChEMBL_1671404 (CHEMBL4021433) Inhibition of human plasma ACE
- ChEMBL_192887 (CHEMBL795926) Inhibition of monkey plasma renin
- ChEMBL_192897 (CHEMBL795936) Selectivity against dog plasma renin
- ChEMBL_195744 (CHEMBL801596) Inhibition of human plasma renin
- ChEMBL_195931 (CHEMBL803287) Inhibition against human plasma renin
- ChEMBL_196092 (CHEMBL872310) Inhibition of human plasma renin
- ChEMBL_196305 (CHEMBL805020) Inhibition against rat plasma renin
- ChEMBL_196430 (CHEMBL800433) Selectivity against sheep plasma renin
- ChEMBL_1990501 (CHEMBL4624236) Inhibition of human plasma myeloperoxidase
- ChEMBL_2228804 (CHEMBL5142317) Inhibition of human plasma renin
- ChEMBL_2273937 Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_2317653 Inhibition of ATX in mouse plasma
- ChEMBL_2344359 Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_326966 (CHEMBL853302) Binding affinity to plasma kallikrein
- ChEMBL_344178 (CHEMBL868878) Binding affinity to plasma kallikrein
- ChEMBL_447834 (CHEMBL898084) Inhibition of human plasma kallikrein
- ChEMBL_448742 (CHEMBL897890) Inhibition of human plasma kallikrein
- ChEMBL_461711 (CHEMBL928842) Inhibition of human plasma kallikrein
- ChEMBL_488663 (CHEMBL988353) Inhibition of human plasma DPP4
- ChEMBL_499548 (CHEMBL1010596) Inhibition of human plasma DPP4
- ChEMBL_499549 (CHEMBL1010597) Inhibition of rat plasma DPP4
- ChEMBL_585345 (CHEMBL1054384) Inhibition of human plasma renin
- ChEMBL_673945 (CHEMBL1275122) Inhibition of renin in plasma
- ChEMBL_673989 (CHEMBL1275166) Inhibition of renin in plasma
- ChEMBL_685576 (CHEMBL1285354) Inhibition of renin in plasma
- ChEMBL_688015 (CHEMBL1291739) Inhibition of human plasma DPP4
- ChEMBL_700284 (CHEMBL1647502) Inhibition of human plasma renin
- ChEMBL_751130 (CHEMBL1787067) Inhibition of human plasma AChE
- ChEMBL_751132 (CHEMBL1787069) Inhibition of human plasma BChE
- ChEMBL_939881 (CHEMBL2327103) Inhibition of human plasma renin
- ChEMBL_531161 (CHEMBL974047) Inhibitory concentration against cap-dependent endonuclease activity of influenza A/PR/8/34 RNP
- ChEMBL_64976 (CHEMBL675561) Inhibitory concentration against cap-dependent endonuclease activity of influenza A/PR/8/34 RNP
- ChEBML_155073 Inhibitory activity against plasmin in human plasma
- ChEBML_155251 Inhibitory activity against plasmin in human plasma
- ChEBML_195751 In vitro inhibition against human plasma renin.
- ChEBML_195939 In vitro inhibition of human plasma renin.
- ChEBML_196302 In vitro inhibition of rat plasma renin
- ChEBML_212862 Inhibitory activity against trypsin in human plasma
- ChEBML_49473 Binding affinity against serine protease plasma chymotrypsin
- ChEBML_92382 Binding affinity against serine protease plasma kallikrein
- ChEMBL_1335112 (CHEMBL3239619) Inhibition of DPP4 in mouse plasma
- ChEMBL_1463562 (CHEMBL3398780) Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_1499036 (CHEMBL3584633) Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_154899 (CHEMBL873641) Inhibition of man plasma renin activity
- ChEMBL_154902 (CHEMBL764679) Inhibition of monkey plasma renin activity
- ChEMBL_154905 (CHEMBL764681) Inhibition of rat plasma renin activity
- ChEMBL_157428 (CHEMBL768882) Inhibition of dog plasma renin activity
- ChEMBL_1671399 (CHEMBL4021428) Inhibition of Wistar rat plasma DPP4
- ChEMBL_1671402 (CHEMBL4021431) Inhibition of Wistar rat plasma ACE
- ChEMBL_1671576 (CHEMBL4021605) Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_1712839 (CHEMBL4122888) Inhibition of renin in rat plasma
- ChEMBL_1712840 (CHEMBL4122889) Inhibition of renin in monkey plasma
- ChEMBL_1881389 (CHEMBL4382888) Binding affinity to human plasma kallikrein
- ChEMBL_192728 (CHEMBL801755) Inhibitory activity against monkey plasma renin.
- ChEMBL_192910 (CHEMBL795271) Selectivity against guinea pig plasma renin
- ChEMBL_195756 (CHEMBL803423) Inhibitory activity against human plasma renin
- ChEMBL_195941 (CHEMBL801667) Inhibitory activity against human plasma renin
- ChEMBL_195954 (CHEMBL806849) Inhibitory activity against human plasma renin
- ChEMBL_195966 (CHEMBL873004) Inhibitory activity against human plasma renin
- ChEMBL_196281 (CHEMBL806635) Inhibitory concentration against renin monkey plasma
- ChEMBL_196282 (CHEMBL806636) Selectivity against rhesus monkey plasma renin
- ChEMBL_2019095 (CHEMBL4672673) Inhibition of thrombin in human plasma
- ChEMBL_2019115 (CHEMBL4672693) Inhibition of thrombin in rat plasma
- ChEMBL_2019116 (CHEMBL4672694) Inhibition of thrombin in rabbit plasma
- ChEMBL_212855 (CHEMBL817807) Inhibition of trypsin in human plasma
- ChEMBL_2158171 (CHEMBL5042921) Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_2162859 (CHEMBL5047720) Inhibition of mouse plasma vanin-1
- ChEMBL_2214170 (CHEMBL5127302) Inhibition of thrombin in human plasma
- ChEMBL_2239501 (CHEMBL5153397) Inhibition of plasma kallikrein (unknown origin)
- ChEMBL_2274760 Inhibition of human plasma coagulation factor XIIIa
- ChEMBL_305654 (CHEMBL829512) Inhibitory concentration against human plasma Butyrylcholinesterase
- ChEMBL_41593 (CHEMBL884137) Inhibitory activity against Butyrylcholinesterase in plasma
- ChEMBL_424298 (CHEMBL910078) Inhibition of MMP13 in rat plasma
- ChEMBL_448898 (CHEMBL898044) Inhibition of human plasma BuChE activity
- ChEMBL_452078 (CHEMBL901239) Inhibition of human plasma carboxypeptidase N
- ChEMBL_454785 (CHEMBL886813) Inhibition of CETP in human plasma
- ChEMBL_501358 (CHEMBL1010541) Inhibition of human plasma derived CETP
- ChEMBL_541719 (CHEMBL1022257) Inhibition of DPP4 in rat plasma
- ChEMBL_685578 (CHEMBL1285356) Inhibition of renin in human plasma
- ChEMBL_685579 (CHEMBL1285357) Inhibition of renin in monkey plasma
- ChEMBL_728473 (CHEMBL1685350) Inhibition of DPP4 in rat plasma
- ChEMBL_92235 (CHEMBL703580) Binding affinity against human plasma kallikrein.
- ChEMBL_92237 (CHEMBL703582) Inhibitory activity against plasma kallikrein (PK.)
- ChEMBL_939877 (CHEMBL2329602) Inhibition of plasma renin (unknown origin)
- ChEBML_105348 In vitro renin inhibitory effect was evaluated for plasma renin activity (PRA) of marmoset plasma renin, Expressed as IC50
- ChEBML_196304 In vitro renin inhibitory effect was evaluated for plasma renin activity (PRA) of rat plasma renin, Expressed as IC50
- ChEMBL_192724 (CHEMBL801751) In vitro renin inhibitory effect was evaluated for plasma renin activity (PRA) of monkey plasma, Expressed as IC50
- ChEMBL_195929 (CHEMBL803285) In vitro renin inhibitory effect was evaluated for plasma renin activity (PRA) of human plasma, Expressed as IC50
- ChEMBL_105348 (CHEMBL872690) In vitro renin inhibitory effect was evaluated for plasma renin activity (PRA) of marmoset plasma renin, Expressed as IC50
- ChEMBL_192895 (CHEMBL795934) In vitro renin inhibitory effect was evaluated for plasma renin activity (PRA) of dog plasma renin, Expressed as IC50
- ChEBML_157258 Compound was tested for inhibition of plasma kallikrein
- ChEBML_192722 In vitro inhibitory activity against monkey plasma renin
- ChEBML_195777 Inhibition of human plasma renin at pH 6
- ChEBML_195961 Inhibitory concentration of compound against renin human plasma
- ChEBML_195971 Tested for the inhibition of human plasma renin
- ChEBML_196299 Inhibitory activity against rat plasma renin in vitro.
- ChEBML_208509 Inhibitory activity against thrombin(fIIa) in human plasma
- ChEMBL_154894 (CHEMBL764013) Inhibition of hog man plasma renin activity
- ChEMBL_154895 (CHEMBL764014) Compound was tested for human plasma renin.
- ChEMBL_157259 (CHEMBL765459) In vitro activity against human Plasma kallikrein.
- ChEMBL_157425 (CHEMBL768880) Inhibition of Cynomolgus monkey plasma renin activity
- ChEMBL_1671400 (CHEMBL4021429) Inhibition of ob/ob mouse plasma DPP4
- ChEMBL_1671403 (CHEMBL4021432) Inhibition of ob/ob mouse plasma ACE
- ChEMBL_1759600 (CHEMBL4194608) Modulation of glucocorticoid receptor in rat plasma
- ChEMBL_192721 (CHEMBL801749) In vitro inhibition of marmoset plasma renin
- ChEMBL_192893 (CHEMBL795932) In vitro inhibition of dog plasma renin
- ChEMBL_195751 (CHEMBL801602) In vitro inhibition against human plasma renin.
- ChEMBL_195774 (CHEMBL801065) In vitro inhibition of Human plasma renin
- ChEMBL_195939 (CHEMBL801665) In vitro inhibition of human plasma renin.
- ChEMBL_195969 (CHEMBL807518) Tested for inhibition of human plasma renin
- ChEMBL_196093 (CHEMBL883523) Inhibition of human plasma renin (pH 7.4)
- ChEMBL_196288 (CHEMBL806642) In vitro inhibition of porcine plasma renin
- ChEMBL_222778 (CHEMBL847107) Inhibitory effect on plasmin in bovine plasma
- ChEMBL_2236013 (CHEMBL5149785) Inhibition of renin activity in human plasma
- ChEMBL_302401 (CHEMBL829646) Binding affinity against thrombin in human plasma
- ChEMBL_304655 (CHEMBL827857) Inhibitory concentration against human plasma mu-calpain
- ChEMBL_357341 (CHEMBL862642) Inhibition of DPP4 in Beagle dog plasma
- ChEMBL_357342 (CHEMBL862643) Inhibition of DPP4 in cynomolgus monkey plasma
- ChEMBL_477678 (CHEMBL924744) Inhibition of CETP in human whole plasma
- ChEMBL_510029 (CHEMBL995172) Inhibition of factor 10a in human plasma
- ChEMBL_664345 (CHEMBL1259494) Inhibition of human recombinant renin in plasma
- ChEMBL_827989 (CHEMBL2051644) Inhibition of renin in cynomolgus monkey plasma
- ChEMBL_92238 (CHEMBL703583) Inhibitory activity against serine protease plasma kallikrein
- ChEMBL_603748 (CHEMBL1039373) Inhibition of human recombinant renin assessed as decrease in plasma renin activity by competitive radioimmunoassay in presence of human plasma
- ChEMBL_2292786 Antagonist activity at cold activated human TRPM8 expressed in HEK293 cells
- ChEBML_101010 Inhibition of lipoprotein associated phospholipase A2 in human plasma
- ChEBML_192725 Inhibitory activity against human plasma renin at pH 7.4
- ChEBML_192896 Inhibitory concentration was measured against plasma renin from dog
- ChEBML_196301 Concentration required for 50% inhibition of rat plasma renin
- ChEBML_196420 Inhibitory concentration was measured against plasma renin from rat
- ChEBML_207986 In vitro inhibitory activity against thrombin in human plasma
- ChEBML_48633 Inhibitory activity against coagulation factor X in human plasma
- ChEBML_48813 Inhibitory activity against Coagulation factor X in human plasma
- ChEBML_92394 Inhibitory activity of compound against human plasma Kallikrein (PK)
- ChEMBL_154892 (CHEMBL763034) In vitro inhibitory activity against hog plasma renin
- ChEMBL_154893 (CHEMBL764012) In vitro inhibitory activity against hog plasma renin
- ChEMBL_154896 (CHEMBL764015) In vitro inhibitory activity against human plasma renin
- ChEMBL_154897 (CHEMBL764016) In vitro inhibitory activity against man plasma renin
- ChEMBL_154904 (CHEMBL878421) In vitro inhibitory activity against rat plasma renin
- ChEMBL_157424 (CHEMBL873635) In vitro inhibitory activity against monkey plasma renin
- ChEMBL_157426 (CHEMBL768881) Inhibitory potency on plasma renin obtained from cats
- ChEMBL_157427 (CHEMBL878083) In vitro inhibitory activity against dog plasma renin
- ChEMBL_1617512 (CHEMBL3859581) Inhibition of renin in human plasma by radioimmunoassay
- ChEMBL_1617920 (CHEMBL3859989) Inhibition of renin in human plasma by radioimmunoassay
- ChEMBL_1712831 (CHEMBL4122880) Inhibition of renin in human plasma by radioimmunoassay
- ChEMBL_1842312 (CHEMBL4342739) Inhibition of human plasma butyrylcholinesterase by Ellman's method
- ChEMBL_195746 (CHEMBL801598) Inhibition of human plasma renin at pH 7.4
- ChEMBL_195791 (CHEMBL801712) Inhibition of human plasma renin at pH 65.0
- ChEMBL_195971 (CHEMBL807520) Tested for the inhibition of human plasma renin
- ChEMBL_195976 (CHEMBL807682) In vitro inhibition of renin in human plasma
- ChEMBL_214382 (CHEMBL821113) Binding affinity against plasma membrane from rat liver
- ChEMBL_222763 (CHEMBL847095) In vitro inhibitory activity against monkey plasma renin
- ChEMBL_222764 (CHEMBL847096) In vitro inhibitory activity against dog plasma renin
- ChEMBL_222765 (CHEMBL847097) In vitro inhibitory activity against hog plasma renin
- ChEMBL_222768 (CHEMBL847099) In vitro inhibitory activity against rat plasma renin
- ChEMBL_2273958 Inhibition of human plasma kallikrein incubated for 1 hrs
- ChEMBL_357340 (CHEMBL862641) Inhibition of DPP4 in Sprague-Dawley rat plasma
- ChEMBL_41408 (CHEMBL653528) In vitro inhibition of Butyrylcholinesterase from human plasma.
- ChEMBL_534768 (CHEMBL986292) Inhibition of human plasma BuchE by Ellman's method
- ChEMBL_592837 (CHEMBL1045780) Inhibition of human plasma BChE by Ellman's method
- ChEMBL_616823 (CHEMBL1100207) Inhibition of rat plasma BChE by Ellman's method
- ChEMBL_813173 (CHEMBL2020839) Inhibition of plasma kallikrein by dixon plot method
- ChEMBL_959186 (CHEMBL2383469) Inhibition of PSA (unknown origin) in female plasma
- ChEMBL_978947 (CHEMBL2424138) Inhibition of human plasma renin by competitive radioimmunoassay
- ChEBML_1690006 Inhibition of ATX in rat plasma assessed as reduction in plasma lysophosphatidic acid 18:2 levels after 2 hrs by LC-MS/MS method
- ChEMBL_2304657 Inhibition of human TRPM8 expressed in HEK293 cells assessed as reduction in cold stimulated Ca2+ efflux preincubated for 5 mins followed by cold stimulation and measured for 3 mins
- ChEBML_151701 Inhibition of PAF receptor binding to rabbit platelet plasma membranes
- ChEBML_154906 Inhibitory potency on plasma renin obtained from Sprague-Dawley rats
- ChEBML_195781 In vitro inhibitory activity against renin from lyophilized human plasma
- ChEBML_200170 Inhibitory activity against bovine plasma semicarbazide-sensitive amine oxidase (SSAO)
- ChEBML_210584 Inhibition of plasma fibrin clot formation by thrombin in vitro.
- ChEBML_218 Inhibitory activity against 12-lipoxygenase in rat platelet rich plasma
- ChEBML_41575 In vitro inhibitory concentration against Butyrylcholinesterase obtained from rat plasma
- ChEMBL_101007 (CHEMBL707409) Inhibitory activity against Lp-PLA2 in whole human plasma
- ChEMBL_154898 (CHEMBL764017) In vitro inhibitory activity against man (human) plasma renin
- ChEMBL_154900 (CHEMBL764678) Inhibitory potency on plasma renin obtained from hypertensive humans
- ChEMBL_157256 (CHEMBL765456) Binding affinity was evaluated on serine protease plasma kallikrein.
- ChEMBL_157429 (CHEMBL768883) Inhibitory potency on plasma renin obtained from mongrel dogs
- ChEMBL_1855604 (CHEMBL4356333) Inhibition of human plasma kallikrein by Michaelis-menten analysis
- ChEMBL_1855616 (CHEMBL4356345) Inhibition of human plasma kallikrein using S2302 as substrate
- ChEMBL_192725 (CHEMBL801752) Inhibitory activity against human plasma renin at pH 7.4
- ChEMBL_192891 (CHEMBL795930) Concentration required for 50% inhibition of dog plasma renin
- ChEMBL_192896 (CHEMBL795935) Inhibitory concentration was measured against plasma renin from dog
- ChEMBL_195754 (CHEMBL801605) Compound was tested for inhibition of human plasma renin.
- ChEMBL_195765 (CHEMBL878549) Concentration required for 50% inhibition of human plasma renin
- ChEMBL_195766 (CHEMBL803431) Concentration required for 50% inhibition of human plasma renin
- ChEMBL_195930 (CHEMBL803286) Inhibition activity against human plasma renin at pH=7.4.
- ChEMBL_195942 (CHEMBL801668) Inhibitory activity against human plasma renin at pH 7.4
- ChEMBL_195943 (CHEMBL801669) Inhibitory activity against human plasma renin at pH 7.4
- ChEMBL_195959 (CHEMBL879242) Inhibitory concentration against human plasma renin at pH 7.4
- ChEMBL_195965 (CHEMBL806859) Inhibitory concentration was measured against plasma renin from human
- ChEMBL_196429 (CHEMBL799833) Concentration required for 50% inhibition of sheep plasma renin
- ChEMBL_219305 (CHEMBL881722) Inhibition of human platelet aggregation in platelet rich plasma
- ChEMBL_219989 (CHEMBL841611) inhibition of platelet aggregation in human platelet rich plasma
- ChEMBL_220118 (CHEMBL840546) Inhibition of platelet aggregation in human platelet rich plasma
- ChEMBL_222766 (CHEMBL872821) In vitro inhibitory activity against man (human) plasma renin
- ChEMBL_222767 (CHEMBL847098) Inhibitory concentration against human plasma renin at pH 6.
- ChEMBL_31096 (CHEMBL640452) Tested for inhibition against human plasma adenosine deaminase (ADA2)
- ChEMBL_432850 (CHEMBL915599) Inhibition of DPP4 in human plasma by fluorescence assay
- ChEMBL_432851 (CHEMBL915600) Inhibition of DPP4 in rat plasma by fluorescence assay
- ChEMBL_454658 (CHEMBL886678) Inhibition of DPP4 in human plasma by fluorescence assay
- ChEMBL_454659 (CHEMBL886679) Inhibition of DPP4 in rat plasma by fluorescence assay
- ChEMBL_46124 (CHEMBL876969) Inhibition canine platelet aggregation in platelet rich plasma (PRP)
- ChEMBL_468822 (CHEMBL932062) Inhibition of DPP4 in human plasma by fluorescence assay
- ChEMBL_468823 (CHEMBL932063) Inhibition of DPP4 in rat plasma by fluorescence assay
- ChEMBL_534536 (CHEMBL985439) Inhibition of DPP4 in human plasma by fluorescence assay
- ChEMBL_625597 (CHEMBL1110678) Inhibition of human recombinant renin in human citreated-plasma
- ChEMBL_741040 (CHEMBL1764268) Inhibition of human recombinant renin in human citreated-plasma
- ChEMBL_838055 (CHEMBL2075429) TP_TRANSPORTER: binding in plasma membranes from CEM/VLB1.0 cells
- ChEMBL_92239 (CHEMBL703584) Inhibitory activity against human serine protease (plasma Kallikrein) (89000*)
- ChEMBL_92395 (CHEMBL699545) Tested in vitro for inhibition of human plasma Kallikriene
- ChEMBL_92396 (CHEMBL699546) Tested in vitro for inhibition of human plasma Kallikriene
- ChEBML_154903 Inhibitory potency on plasma renin obtained from New Zealand white rabbits
- ChEBML_158684 Inhibition of ADP-induced platelet aggregation in canine platelet-rich plasma
- ChEBML_158685 Inhibition of ADP-induced platelet aggregation in canine platelet-rich plasma
- ChEBML_192729 The compound was evaluated for inhibitory activity against monkey plasma renin.
- ChEBML_195741 Compound was evaluated for inhibition of plasma renin activity in human
- ChEBML_195742 Compound was evaluated for the ability to inhibit human plasma renin.
- ChEBML_195759 Compound was tested for its inhibitory activity against human plasma renin
- ChEBML_195793 In vitro potency against plasma renin at a pH of 7.4
- ChEBML_196297 Compound was evaluated for inhibition of plasma renin activity in rat
- ChEBML_213158 Inhibitory activity against urokinase-type plasminogen activator (microPa) in human plasma
- ChEMBL_1339182 (CHEMBL3243345) Inhibition of TAF1a in human plasma assessed as clot lysis
- ChEMBL_1514807 (CHEMBL3615225) Inhibition of bovine plasma thrombin using S-2238 as substrate
- ChEMBL_1520713 (CHEMBL3625632) Antagonist activity against integrin alpha2bbeta3 in human platelet rich plasma
- ChEMBL_154129 (CHEMBL759800) Inhibition of human platelet aggregation in platelet rich plasma (PRP)
- ChEMBL_157423 (CHEMBL768879) In vitro inhibitory activity against monkey (Callithrix jacchus) plasma renin
- ChEMBL_158828 (CHEMBL884929) Inhibition of canine platelet-rich plasma agregation induced by ADP
- ChEMBL_162738 (CHEMBL765217) The compound was tested for inhibition of rabbit plasma renin.
- ChEMBL_1750381 (CHEMBL4185141) Binding affinity to HIV1 integrase by surface plasma resonance method
- ChEMBL_192718 (CHEMBL801746) Compound was tested for the inhibition of monkey plasma renin
- ChEMBL_192720 (CHEMBL801748) Concentration required for 50% inhibition of rhesus monkey plasma renin
- ChEMBL_192727 (CHEMBL801754) Inhibitory activity against renin in monkey plasma at pH 7.7
- ChEMBL_195920 (CHEMBL803389) In vitro inhibition of human plasma renin at PH 7.4
- ChEMBL_195925 (CHEMBL803394) In vitro potency against human plasma renin at pH 7.4
- ChEMBL_195952 (CHEMBL806847) Inhibitory activity against purified human plasma renin at pH 6.0
- ChEMBL_195956 (CHEMBL806851) Inhibitory activity against human plasma renin; G means not measured
- ChEMBL_210584 (CHEMBL817394) Inhibition of plasma fibrin clot formation by thrombin in vitro.
- ChEMBL_214691 (CHEMBL817654) Binding affinity against plasma membrane from bovine kidney inner medulla
- ChEMBL_2200354 (CHEMBL5112870) Reversible inhibition of human plasma kallikrein assessed as inhibition constant
- ChEMBL_220105 (CHEMBL842870) Inhibition of platelet aggregation in human platelet rich plasma (hPRP)
- ChEMBL_220106 (CHEMBL842871) Inhibition of platelet aggregation in human platelet rich plasma (hPRP)
- ChEMBL_2208446 (CHEMBL5121395) Antagonist activity at P2Y12 receptor in human platelet rich plasma
- ChEMBL_220906 (CHEMBL824660) Inhibition of platelet aggregation in human platelet rich plasma (hPRP)
- ChEMBL_2274768 Inhibition of human plasma coagulation factor XIIIa by fluorescence spectrophotometeric assay
- ChEMBL_2277984 Inhibition of human plasma kallikrein using Z-FR-MCA as substrate
- ChEMBL_2349849 Binding affinity to human galectin 3 by surface plasma resonance analysis
- ChEMBL_2434663 Inhibition of ENPP1 in mouse plasma using [32P]cGAMP as substrate
- ChEMBL_41590 (CHEMBL654884) Ability to inhibit butyrylcholinesterase (BChE), freshly prepared from human plasma
- ChEMBL_49160 (CHEMBL663260) Inhibitory effect on Coagulation factor Xa (FXa) from bovine plasma
- ChEMBL_608130 (CHEMBL1074819) Inhibition of human VLA4 in presence of 90% human plasma
- ChEMBL_613957 (CHEMBL1068997) Inhibition of human plasma BuChE by modified Ellman's spectrophotometric method
- ChEMBL_86494 (CHEMBL696355) Inhibition of platelet aggregation in human platelet rich plasma (PRP)
- ChEBML_155510 Inhibition of ADP induced platelet aggregation in human platelet-rich plasma (PRP)
- ChEBML_155511 Inhibition of ADP induced platelet aggregation in human platelet-rich plasma (PRP).
- ChEBML_155984 Inhibition of ADP-induced platelet aggregation in rabbit platelet rich plasma (PRP)
- ChEBML_1644400 Inhibition of human plasma kallikrein using fluorogenic substrate Z-Phe-Arg-AMC
- ChEBML_195760 Compound was tested for the inhibition of human plasma renin(Hu Renin)
- ChEBML_195776 In vitro inhibition against human plasma renin at pH 7.2 was determined
- ChEBML_196103 The compound was tested in vitro for inhibition of human plasma renin.
- ChEBML_196424 Tested in vitro for inhibitory activity against plasma renin in rat models
- ChEBML_41578 Inhibitory concentration was determined in in vitro for Butyrylcholinesterase in rat plasma
- ChEMBL_1540277 (CHEMBL3739108) Binding affinity to human plasma kallikrein by surface plasmon resonance assay
- ChEMBL_154903 (CHEMBL764680) Inhibitory potency on plasma renin obtained from New Zealand white rabbits
- ChEMBL_155488 (CHEMBL768063) Inhibition of platelet aggregation in citreated human platelet rich plasma (PRP)
- ChEMBL_1649342 (CHEMBL3998476) Binding affinity to PHGDH (unknown origin) by surface plasma resonance method
- ChEMBL_1652024 (CHEMBL4001279) Binding affinity to recombinant human pirin by surface plasma resonance method
- ChEMBL_1711158 (CHEMBL4121207) Binding affinity to PHGDH (unknown origin) by surface plasma resonance method
- ChEMBL_1732209 (CHEMBL4147745) Binding affinity to MCL1 (unknown origin) by surface plasma resonance method
- ChEMBL_1772718 (CHEMBL4229710) Binding affinity to C3 derived from human plasma by ITC analysis
- ChEMBL_1772719 (CHEMBL4229711) Binding affinity to C3b derived from human plasma by SPR analysis
- ChEMBL_1826010 (CHEMBL4325774) Inhibition of endothelial lipase in hepatic lipase knock-out mouse plasma
- ChEMBL_192715 (CHEMBL801743) Compound was evaluated for inhibition of plasma renin activity in monkey
- ChEMBL_192723 (CHEMBL801750) In vitro inhibitory concentration against monkey plasma renin at pH 7.4
- ChEMBL_192888 (CHEMBL795927) Compound was evaluated for inhibition of plasma renin activity in dog
- ChEMBL_192889 (CHEMBL795928) Compound was tested for its inhibitory activity against dog plasma renin
- ChEMBL_192894 (CHEMBL795933) In vitro inhibitory concentration against dog plasma renin at pH 7.4
- ChEMBL_192909 (CHEMBL795270) Compound was tested for the inhibition of guinea pig plasma renin
- ChEMBL_195741 (CHEMBL872996) Compound was evaluated for inhibition of plasma renin activity in human
- ChEMBL_195758 (CHEMBL803425) Compound was tested for its inhibitory activity against human plasma renin
- ChEMBL_195790 (CHEMBL801711) In vitro inhibitory concentration against human plasma renin at pH 7.4
- ChEMBL_195792 (CHEMBL802392) In vitro potency against plasma renin at a pH of 6.0
- ChEMBL_195793 (CHEMBL802393) In vitro potency against plasma renin at a pH of 7.4
- ChEMBL_196298 (CHEMBL806651) Compound was tested for its inhibitory activity against Rat plasma renin
- ChEMBL_196303 (CHEMBL805018) In vitro inhibitory concentration against rat plasma renin at pH 7.4
- ChEMBL_196705 (CHEMBL801532) The compound was tested for inhibition of rhesus monkey plasma renin.
- ChEMBL_2108852 (CHEMBL4817527) Inhibition of ASM (unknown origin)-mediated KRAS mislocalization from plasma membrane
- ChEMBL_219302 (CHEMBL822661) Inhibition of ADP-induced platelet aggregation in human platelet rich plasma
- ChEMBL_219304 (CHEMBL822663) Inhibition of ADP-induced human platelet aggregation in platelet rich plasma
- ChEMBL_220145 (CHEMBL841428) inhibition of ADP-induced platelet aggregation in human platelet rich plasma
- ChEMBL_221702 (CHEMBL823402) Inhibition of PAF-induced platelet aggregation in rabbit platelet rich plasma
- ChEMBL_2236016 (CHEMBL5149788) Inhibition of renin activity in human plasma by competitive radio immunoassay
- ChEMBL_31099 (CHEMBL640455) Tested for binding constant against adenosine deaminase (ADA2) in human plasma
- ChEMBL_312774 (CHEMBL833423) In vitro inhibition of human platelet aggregation in platelet rich plasma
- ChEMBL_36893 (CHEMBL648683) In vitro inhibition of Angiotensin I converting enzyme in Hog plasma
- ChEMBL_41718 (CHEMBL659264) In vitro inhibitory concentration against butyrylcholinesterase (BuChE) obtained from rat plasma
- ChEMBL_511098 (CHEMBL1000390) Inhibition of human plasma BChE after 20 mins by Ellman's method
- ChEMBL_534774 (CHEMBL986298) Inhibition of human plasma BuchE after 60 mins by carbamylation assay
- ChEMBL_542644 (CHEMBL1015033) Inhibition of human plasma-derived CETP activity by scintillation proximity assay
- ChEMBL_616423 (CHEMBL1100709) Inhibition of human plasma BChE after 5 mins by Ellman's method
- ChEMBL_651750 (CHEMBL1228440) Inhibition of human recombinant renin in presence of plasma by immunoassay
- ChEMBL_727164 (CHEMBL1687189) Inhibition of PrCP in mouse plasma assessed as angiotensin 3 cleavage
- ChEMBL_89731 (CHEMBL696585) Inhibition of ADP-induced platelet aggregation in human platelet-rich plasma
- ChEMBL_2375961 Binding affinity to recombinant Influenza A virus polymerase PB2 cap-binding domain (318 to 413 residues) assessed as dissociation constant by ITC method
- ChEBML_195745 Compound was evaluated for the inhibition of human plasma renin at pH 7.4
- ChEMBL_1471171 (CHEMBL3421302) Inhibition of F10a in human plasma assessed as doubling of prothombin time
- ChEMBL_1471173 (CHEMBL3421304) Inhibition of F10a in rabbit plasma assessed as doubling of prothombin time
- ChEMBL_155489 (CHEMBL768064) Inhibition of platelet aggregation in heparin treated human platelet rich plasma (PRP)
- ChEMBL_156370 (CHEMBL761699) Inhibition of the Phospholipase A2 (Lp-PLA2) enzyme in whole human plasma
- ChEMBL_158730 (CHEMBL768738) IC50 against Prostaglandin G/H synthase 1 from human platelet rich plasma
- ChEMBL_158733 (CHEMBL768740) IC50 against Prostaglandin G/H synthase 1 from human platelet rich plasma
- ChEMBL_1923128 (CHEMBL4426084) Inhibition of human plasma kallikrein using S2302 as substrate by spectrophotometric method
- ChEMBL_192898 (CHEMBL795111) Tested in vitro for its ability to inhibit the dog plasma renin
- ChEMBL_192899 (CHEMBL795112) Tested in vitro for its ability to inhibit the dog plasma renin
- ChEMBL_192905 (CHEMBL795266) Tested in vitro for its ability to inhibit the dog plasma renin
- ChEMBL_192906 (CHEMBL795267) Tested in vitro for its ability to inhibit the ferret plasma renin
- ChEMBL_192907 (CHEMBL795268) Tested in vitro for its ability to inhibit the ferret plasma renin
- ChEMBL_192908 (CHEMBL795269) Tested in vitro for its ability to inhibit the ferret plasma renin
- ChEMBL_195760 (CHEMBL803427) Compound was tested for the inhibition of human plasma renin(Hu Renin)
- ChEMBL_195776 (CHEMBL801699) In vitro inhibition against human plasma renin at pH 7.2 was determined
- ChEMBL_195918 (CHEMBL803387) In vitro potency against human plasma renin at a pH of 7.4
- ChEMBL_195973 (CHEMBL879243) Tested in vitro for its ability to inhibit the human plasma renin
- ChEMBL_196422 (CHEMBL872990) Tested in vitro for its ability to inhibit the rat plasma renin
- ChEMBL_196423 (CHEMBL799827) Tested in vitro for its ability to inhibit the rat plasma renin
- ChEMBL_2273959 Inhibition of human plasma kallikrein using H-DPro-Phe-Arg-AFC as substrate
- ChEMBL_306658 (CHEMBL831431) Inhibition of alpha IIb beta3 integrin receptor in human platelet rich plasma
- ChEMBL_53338 (CHEMBL876697) Inhibitory activity against Dipeptidyl peptidase IV (DPP IV) obtained from human plasma
- ChEMBL_53339 (CHEMBL664924) Inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) obtained from human plasma
- ChEMBL_53355 (CHEMBL664525) Inhibitory activity against Dipeptidyl peptidase IV (DPP IV) obtained from rat plasma
- ChEMBL_53356 (CHEMBL664526) Inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) obtained from rat plasma
- ChEMBL_600082 (CHEMBL1041055) Inhibition of plasma kallikrein after 10 to 15 mins by fluorescence assay
- ChEMBL_617885 (CHEMBL1101550) Binding affinity to recombinant Shh N-terminal peptide by surface plasma resonance
- ChEMBL_642169 (CHEMBL1176720) Inhibition of human plasma BChE pretreated for 30 mins by Ellman technique
- ChEMBL_643921 (CHEMBL1211820) Antagonist activity at FITC-tagged alpha3beta3 integrin in human platelet rich plasma
- ChEMBL_853460 (CHEMBL2155357) Inhibition of human plasma renin activity after 60 mins by competitive RIA
- ChEMBL_962065 (CHEMBL2388033) Inhibition of renin in cynomolgus monkey plasma after 1 hr by RIA
- ChEMBL_980914 (CHEMBL2421449) Inhibition of human plasma BuChE using butyrylthiocholine as substrate by Ellman's method
- ChEMBL_633033 (CHEMBL1118501) Antagonist activity at human TRPA1 channel assessed as inhibition of noxious cold-induced receptor activation
- ChEMBL_1286464 (CHEMBL3112196) Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay
- ChEMBL_2300431 Binding affinity to full length Influenza A virus PB2 cap-binding domain assessed as dissociation constant incubated for 60 mins by fluorescence polarization assay
- ChEMBL_826737 (CHEMBL2051184) Inhibition of eIF4E in rabbit reticulocyte cell lysate assessed as inhibition of cap-dependent translation after 90 mins by luciferase reporter gene assay
- ChEMBL_992394 (CHEMBL2445614) Binding affinity to human Arno Sec7 domain immobilized on CAP sensor chip after 15 mins by 1H 1D-NMR-700 MHz spectra analysis
- ChEBML_155612 Plasminogen Activator Inhibitor-1 (PAI-1) activity was determined using plasma clot lysis assay
- ChEBML_192730 The compound was tested in vitro for inhibitory activity against Renin in monkey plasma
- ChEBML_193376 The compound was tested for inhibition of rat plasma renin at pH of 6.0.
- ChEBML_193377 The compound was tested for inhibition of rat plasma renin at pH of 7.4.
- ChEBML_195763 Concentration required to inhibit human plasma renin by 50% using radio-immunoassay was determined
- ChEBML_196300 Concentration required to inhibit rat plasma renin by 50% using radio-immunoassay was determined
- ChEBML_212941 Inhibition of Thromboxane B2 formation in collagen-stimulated human platelets in platelet rich plasma.
- ChEMBL_1451472 (CHEMBL3364651) Inhibition of CETP-mediated [3H]-CE from HDL to LDL in human plasma
- ChEMBL_1464639 (CHEMBL3406660) Inhibition of human recombinant renin in presence of plasma by TR-FRET assay
- ChEMBL_1504788 (CHEMBL3595073) Inhibition of human plasma kallikrein using S2302 as substrate measured for 30 mins
- ChEMBL_158731 (CHEMBL878778) IC50 value against Prostaglandin G/H synthase 1 of human platelet rich plasma
- ChEMBL_1619504 (CHEMBL3861673) Inhibition of activated human plasma TAFI incubated for 15 mins by chromogenic assay
- ChEMBL_1622607 (CHEMBL3864959) Inhibition of 15-LOX-mediated lipid oxidation in 10% C57BL/6J mouse plasma
- ChEMBL_1722778 (CHEMBL4137778) Inhibition of human plasma BuChE using acetylthiocholine iodide as substrate by Ellman's method
- ChEMBL_2018330 (CHEMBL4671908) Inhibition of TAFIalpha in human plasma incubated for 15 mins by chromogenic assay
- ChEMBL_2153967 (CHEMBL5038514) Inhibition of human plasma kallikrein using fluorogenic substrate measured by microplate reader analysis
- ChEMBL_218203 (CHEMBL824552) Inhibition of platelet aggregation in human platelet-rich plasma by alphaIIb-beta3 integrin
- ChEMBL_219303 (CHEMBL822662) Inhibition of 2.5 uM ADP induced human platelet aggregation in platelet rich plasma
- ChEMBL_219306 (CHEMBL822664) Inhibition of glycoprotein IIb/III and platelet aggregation in human platelet rich plasma
- ChEMBL_2261353 (CHEMBL5216364) Inhibition of human plasma BChE using S-butyrylthiocholine as substrate by enzymatic assay
- ChEMBL_2261356 (CHEMBL5216367) Inhibition of human plasma BChE using S-butyrylthiocholine as substrate by Ellman's method
- ChEMBL_312865 (CHEMBL874943) In vitro inhibition of Collagen-induced platelet aggregation in canine platelet rich plasma
- ChEMBL_476655 (CHEMBL927168) Inhibition of factor 5a-mediated prothrombin activation in human plasma by prothrombinase assay
- ChEMBL_533530 (CHEMBL990507) Binding affinity to complement component C3 in human plasma by isothermal titration calorimetry
- ChEMBL_534343 (CHEMBL978815) Displacement of [125I]beta-CIT from human SERT in human platelet plasma membrane
- ChEMBL_628977 (CHEMBL1120827) Binding affinity to human Bcl-XL by surface plasma resonance based biosensor system
- ChEMBL_70921 (CHEMBL683739) In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
- ChEMBL_73011 (CHEMBL681690) In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
- ChEMBL_790793 (CHEMBL1926246) Inhibition of human plasma kallikrein using chromogenic substrate S2302 by dixon plot analysis
- ChEMBL_816393 (CHEMBL2024791) Inhibition of human Erg by patch clamp assay in absence of plasma protein
- ChEMBL_853461 (CHEMBL2155358) Inhibition of cynomolgus monkey plasma renin activity after 60 mins by competitive RIA
- ChEMBL_861913 (CHEMBL2173641) Inhibition of human plasma F10a assessed as spectrozyme TH hydrolysis after 10 mins
- ChEMBL_885260 (CHEMBL2214233) Inhibition of renin in cynomolgus monkey plasma after 60 mins by competitive radioimmunoassay
- ChEMBL_89284 (CHEMBL879040) Inhibition of 17.5 uM ADP-induced platelet aggregation of human platelet-rich plasma
- ChEMBL_89594 (CHEMBL696531) Inhibition of 20 uM ADP-induced platelet aggregation in human platelet-rich plasma
- ChEMBL_89710 (CHEMBL696413) Inhibition ADP-induced (fibrinogen-mediated) platelet aggregation in human platelet-rich plasma (PRP)
- ChEMBL_584058 (CHEMBL1056681) Inhibition of PGHS-1 in human platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation in human platelet rich plasma treated 5 min before arachidonic acid challenge by turbidimetry
- ChEBML_215813 Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line
- ChEMBL_653215 (CHEMBL1226418) Inhibition of eIF4A-mediated cap-dependent protein synthesis in FF-HCV-Ren mRNA transfected Swiss mouse Krebs2 cell extract by [35S]methionine metabolic labeling study
- ChEBML_192731 The concentration producing 50% inhibition of renin activity in monkey plasma was determined by radioimmunoassay.
- ChEBML_195978 The compound was evaluated in vitro for inhibition of human plasma renin at pH 7.4.
- ChEMBL_1289411 (CHEMBL3116907) Inhibition of CETP in human whole plasma using [3H]-CE/HDL after 10 mins
- ChEMBL_1363408 (CHEMBL3295543) Binding affinity to human plasma full length Glu-plasminogen by surface plasmon resonance analysis
- ChEMBL_1364435 (CHEMBL3294776) Inhibition of bovine plasma factor 10a using CH3OCO-D-CHA-Gly-Arg-pNA.AcoH substrate
- ChEMBL_1443466 (CHEMBL3377180) Inhibition of human plasma kallikrein using H-D-Pro-Phe-Arg-pNA as substrate
- ChEMBL_1465616 (CHEMBL3404918) Inhibition of recombinant human renin by fluorescence based FRET assay in presence of plasma
- ChEMBL_1471172 (CHEMBL3421303) Inhibition of F10a in human plasma assessed as doubling of activated partial thromboplastin time
- ChEMBL_1471174 (CHEMBL3421305) Inhibition of F10a in rabbit plasma assessed as doubling of activated partial thromboplastin time
- ChEMBL_155494 (CHEMBL768069) In vitro inhibition of ADP-induced platelet aggregation in human platelet rich plasma (hPRP)
- ChEMBL_155612 (CHEMBL766347) Plasminogen Activator Inhibitor-1 (PAI-1) activity was determined using plasma clot lysis assay
- ChEMBL_1772820 (CHEMBL4229812) Competitive inhibition of human plasma kallikrein using S2302 as substrate by UV-visible spectrophotometer
- ChEMBL_1902632 (CHEMBL4404854) Inhibition of ATX in mouse plasma after 2 hrs by LC-MS/MS analysis
- ChEMBL_1921542 (CHEMBL4424387) Inhibition of human plasma kallikrein preincubated for 15 mins followed by chromogenic substrate addition
- ChEMBL_1921543 (CHEMBL4424388) Inhibition of mouse plasma kallikrein preincubated for 15 mins followed by chromogenic substrate addition
- ChEMBL_192719 (CHEMBL801747) Concentration required to inhibit monkey plasma renin by 50% using radio-immunoassay was determined
- ChEMBL_192730 (CHEMBL801757) The compound was tested in vitro for inhibitory activity against Renin in monkey plasma
- ChEMBL_192890 (CHEMBL795929) Concentration required to inhibit dog plasma renin by 50% using radio-immunoassay was determined
- ChEMBL_193377 (CHEMBL798070) The compound was tested for inhibition of rat plasma renin at pH of 7.4.
- ChEMBL_195747 (CHEMBL801599) Compound was evaluated for the inhibitory concentration against human plasma renin at pH 7.4
- ChEMBL_2118640 (CHEMBL4827706) Inhibition of LPA in human plasma after 18 hrs by LC-MS/MS analysis
- ChEMBL_2118641 (CHEMBL4827707) Inhibition of LPA in rat plasma after 18 hrs by LC-MS/MS analysis
- ChEMBL_214381 (CHEMBL881107) Binding affinity against plasma membrane from rat liver using [3H]-AVP as a radioligand
- ChEMBL_2273963 Inhibition of human plasma kallikrein usingPro-Phe-Arg-AMC as substrate incubated for 5 mins
- ChEMBL_2329786 Inhibition of thrombin in human plasma measured after 10 mins by chromogenic substrate hydrolysis assay
- ChEMBL_2356230 Inhibition of plasma Kallikrein (unknown origin) in buffer measured after 40 mins by fluorescence assay
- ChEMBL_53211 (CHEMBL664032) In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from human plasma
- ChEMBL_532110 (CHEMBL969429) Inhibition of rat plasma butyrylcholine esterase in presence of butyrylcholine substrate by chemiluminescent assay
- ChEMBL_53337 (CHEMBL664923) In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from human plasma.
- ChEMBL_53353 (CHEMBL664523) In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from rat plasma
- ChEMBL_53354 (CHEMBL664524) In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from rat plasma.
- ChEMBL_583577 (CHEMBL1059092) Inhibition of NHE1 in Sprague-Dawley rat platelet-rich plasma by optical swelling assay
- ChEMBL_595728 (CHEMBL1045251) Inhibition of human somatic ACE in presence of 1:50 diluted SHR rat plasma
- ChEMBL_595729 (CHEMBL1045252) Inhibition of human somatic ACE in presence of 1:100 diluted SHR rat plasma
- ChEMBL_611222 (CHEMBL1068251) Inhibition of cholesteryl ester transfer protein in human plasma by [3H]CE HDL assay
- ChEMBL_799451 (CHEMBL1942259) Inhibition of PrCP-mediated conversion of Ang3 to Ang(2-7) in mouse plasma
- ChEMBL_823303 (CHEMBL2046142) Inhibition of NPM-ALK autophosphorylation in human KARPAS299 cells in presence of mouse plasma
- ChEMBL_834153 (CHEMBL2072893) Inhibition of BuChE activity in rat plasma using butyrylcholine as substrate by Ellman's method
- ChEMBL_1687677 (CHEMBL4038156) Inhibition of plasma kallikrein in human plasma using HMWK as substrate assessed as suppression of kaolin-activated protein induced bradykinin release preincubated for 15 mins followed by substrate addition measured after 15 min by ELISA
- ChEMBL_215813 (CHEMBL820102) Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line
- Biological Assay Example 4 Inhibition assay using 11β-HSD1 in the presence of 50% human plasma.
- ChEBML_1681594 Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method
- ChEBML_1686641 Inhibition of human plasma thrombin using chromogenix AB as substrate after 30 secs by UV-spectrophotometry
- ChEBML_1686642 Inhibition of bovine plasma thrombin using chromogenix AB as substrate after 30 secs by UV-spectrophotometry
- ChEBML_214690 Binding affinity against plasma membrane from bovine kidney inner medulla using [3H]AVP as a radioligand
- ChEMBL_1363407 (CHEMBL3295542) Binding affinity to human plasma N-terminal truncated Lys-plasminogen by surface plasmon resonance analysis
- ChEMBL_1433267 (CHEMBL3388805) Inhibition of human recombinant CETP in presence of 88% human plasma by fluorescence transfer assay
- ChEMBL_157265 (CHEMBL765465) In vitro inhibition of bound [125I]L-T3 rat plasma membrane 3,5,3'' L-triiodothyronine receptor
- ChEMBL_1788970 (CHEMBL4260704) Reversible inhibition of human plasma BChE using acetylthiocholine iodide as substrate by Ellman spectrophotometric method
- ChEMBL_1871020 (CHEMBL4372187) Inhibition of plasma KLK (unknown origin) using Ac-NLTR-pNA as substrate after 30 mins
- ChEMBL_1878298 (CHEMBL4379692) Inhibition of BuChE in human plasma using butyrylthiocholine iodide substrate by Ellman's protocol based assay
- ChEMBL_1891830 (CHEMBL4393751) Inhibition of HIV1 reverse transcriptase derived from HIV patient plasma by LC/MS/MS analysis
- ChEMBL_195927 (CHEMBL803396) In vitro renin inhibition was measured at pH 7.4 by using human plasma renin assay
- ChEMBL_1984898 (CHEMBL4618304) Inhibition of human plasma kallikrein using H-(D)-Pro-Phe-Arg-pNA substrate by spectrophotometry
- ChEMBL_220109 (CHEMBL881458) In vitro inhibition of ADP (2 uM) induced platelet aggregation of human platelet rich plasma
- ChEMBL_221751 (CHEMBL821959) In vitro inhibition of ADP (5 uM) induced platelet aggregation of mouse platelet rich plasma
- ChEMBL_2355339 Displacement of [3H]CP55490 from CB1 receptor in mouse brain plasma membrane by radioligand displacement analysis
- ChEMBL_2364169 Inhibition of human plasma kallikrein using Acetyl-K- P-R-AFC substrate by fluorescence based assay
- ChEMBL_2438093 Modulation of human gamma-secretase assessed as reduction in amyloidbeta42 level in plasma by ELISA analysis
- ChEMBL_45639 (CHEMBL655449) In vitro inhibition of purified Carboxypeptidase B (CPB) by clot lysis assay in human plasma
- ChEMBL_45790 (CHEMBL660086) In vitro inhibition of purified Carboxypeptidase M (CPM) by clot lysis assay in human plasma
- ChEMBL_498038 (CHEMBL1000241) Displacement of [3H]PDBu form human PKCalpha in presence of plasma membrane lipid mimetic mixture
- ChEMBL_498039 (CHEMBL1000242) Displacement of [3H]PDBu form human PKCbeta in presence of plasma membrane lipid mimetic mixture
- ChEMBL_498040 (CHEMBL1000243) Displacement of [3H]PDBu form human PKCgamma in presence of plasma membrane lipid mimetic mixture
- ChEMBL_498041 (CHEMBL995912) Displacement of [3H]PDBu form human PKCdelta in presence of plasma membrane lipid mimetic mixture
- ChEMBL_498042 (CHEMBL995913) Displacement of [3H]PDBu form human PKCepsilon in presence of plasma membrane lipid mimetic mixture
- ChEMBL_600878 (CHEMBL1042836) Displacement of [125I]IP10 from CXCR3 receptor expressed in PBMC in presence of human plasma
- ChEMBL_611613 (CHEMBL1068950) Inhibition of human plasma BuChE preincubated for 30 mins before substrate addition by Ellman's assay
- ChEMBL_814571 (CHEMBL2021090) Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis
- ChEMBL_849433 (CHEMBL2149434) Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis
- ChEMBL_946315 (CHEMBL2345930) Inhibition of BuChE in human plasma using butyrylthiocholine iodide as substrate by Ellman's colorimetric method
- ChEMBL_2444755 Binding affinity to N-terminal His-tagged TOSV cap-ENDO expressed in Escherichia coli BL21 Gold (DE3) assessed as dissociation constant in presence of MnCl2 by ITC analysis
- Shift AlphaScreen Assay The AlphaScreen Assay is modified to include the testing of inhibitors against ADAMTS-5 in the presence of 50% Lewis rat plasma in order to determine the effects of plasma protein binding on inhibitor potency. The ratio between the IC50 of the inhibitor against ADAMTS-5 in 50% Lewis rat plasma versus the IC50 of the inhibitor in buffer is calculated and is described as the plasma shift of the inhibitor. The assay is completed in the same manner using 10 nM ADAMTS-5 instead of 2.1 nM. A similar assay is used with dog ADAMTS-4 in the presence of 25% dog plasma.
- ChEBML_162869 Inhibition of platelet aggregation using Adenosine diphosphate (ADP) as activating agent in rabbit platelet rich plasma (PRP)
- ChEBML_195788 In vitro inhibitory activity against human plasma renin at pH 5.5 for suppression of angiotensin I formation.
- ChEMBL_1363405 (CHEMBL3295540) Binding affinity to human plasma full length Glu-plasminogen K1 domain by surface plasmon resonance analysis
- ChEMBL_1591231 (CHEMBL3829623) Inhibition of ATX-mediated LPA release in human plasma after 3 hrs by mass spectrometric analysis
- ChEMBL_1681594 (CHEMBL4031871) Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method
- ChEMBL_1714513 (CHEMBL4124562) Inhibition of human plasma activated thrombin-activatable fibrinolysis inhibitor after 10 mins in presence of DTT
- ChEMBL_1714514 (CHEMBL4124563) Inhibition of human plasma activated thrombin-activatable fibrinolysis inhibitor after 10 mins in absence of DTT
- ChEMBL_1855609 (CHEMBL4356338) Inhibition of human plasma kallikrein using S2302 as substrate after 10 mins by UV/Vis photometry
- ChEMBL_195974 (CHEMBL807522) Tested in vitro for its ability to inhibit the human plasma renin at pH of 7.4
- ChEMBL_2086997 (CHEMBL4768260) Inhibition of human plasma BuChE using butyrylthiocholine as substrate measured after 5 mins by Ellman's method
- ChEMBL_213398 (CHEMBL818056) Inhibition of alpha4-beta1 (very late) antigen binding with VCAM-1 immunoglobulin plus 5% human plasma
- ChEMBL_214690 (CHEMBL817653) Binding affinity against plasma membrane from bovine kidney inner medulla using [3H]AVP as a radioligand
- ChEMBL_220548 (CHEMBL822041) In vitro inhibition of ADP (3 uM)induced platelet aggregation of guinea pig platelet rich plasma
- ChEMBL_2266438 Inhibition of human plasma kallikrein using Acetyl-K- P-R-AFC as substrate by fluorescence based analysis
- ChEMBL_2527471 Inhibition of human recombinant IGF-1 receptor in 90% mouse plasma measured by HPLC-MS/MS analysis
- ChEMBL_2527472 Inhibition of human recombinant IGF-1 receptor in 90% human plasma measured by HPLC-MS/MS analysis
- ChEMBL_364766 (CHEMBL854188) Activity at DP receptor assessed as inhibition of PGD2-induced cAMP accumulation in platelet rich plasma
- ChEMBL_364767 (CHEMBL854189) Activity at TP receptor assessed as inhibition of U46619-induced platelet aggregation in platelet rich plasma
- ChEMBL_425880 (CHEMBL907941) Activity at human TP receptor in platelet rich plasma assessed as inhibition U44619-induced platelet aggregation
- ChEMBL_45620 (CHEMBL655431) In vitro inhibition of Carboxypeptidase A (CPA) was determined by clot lysis assay using human plasma
- ChEMBL_615621 (CHEMBL1104195) Inhibition of human plasma CETP assessed as cholesterol ester transfer after 24 hrs by fluorescence assay
- ChEMBL_65135 (CHEMBL677470) Inhibitory concentration compound against EFGR tyrosine kinase obtained from plasma membrane vesicles from cultured A431 cells
- ChEMBL_730212 (CHEMBL1696307) Inhibition of Pdr5p-mediated rhodamine 6G transport in Saccharomyces cerevisiae MKPDR5h plasma membrane by spectrofluorometric assay
- ChEMBL_802883 (CHEMBL1953701) Inhibition of PrCP in mouse plasma assessed as angiotensin 3 cleavage by whole serum shift assay
- ChEMBL_2292797 Agonist activity at human TRMP8 expressed in HEK293 cells measured after 24 hrs of cold activation by patch clamp assay
- ChEMBL_1989849 (CHEMBL4623584) Inhibition of eIF4E in rabbit reticulocyte lysate system assessed as reduction in ARCA mRNA cap-dependent translation measured after 60 mins by luciferase reporter gene based luminescence assay
- ChEMBL_702910 (CHEMBL1655535) Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology
- ChEBML_90019 Ability to inhibit blood platelet aggregation of human platelet-rich plasma induced by TP-receptor agonist U 46619
- ChEMBL_1335496 (CHEMBL3239281) Inhibition of DPP4 purified from human seminal plasma using Gly-Pro-p-nitroanilide as substrate by spectrophotometry
- ChEMBL_1335499 (CHEMBL3239284) Inhibition of DPP2 purified from human seminal plasma using Lys-Ala-p-nitroanilide as substrate by spectrophotometry
- ChEMBL_1363406 (CHEMBL3295541) Binding affinity to human plasma N-terminal truncated Lys-plasminogen K1 domain by surface plasmon resonance analysis
- ChEMBL_1436531 (CHEMBL3382310) Inhibition of DPP4 in human plasma using Gly-Pro-AMC substrate incubated for 20 mins by fluorometry
- ChEMBL_1454019 (CHEMBL3367078) Antagonist activity at P2Y12 receptor in human platelet rich plasma assessed as inhibition of ADP-induced aggregation
- ChEMBL_1463431 (CHEMBL3399768) Inhibition of bovine plasma thrombin using Benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin hydrochloride by spectrophotometry
- ChEMBL_158651 (CHEMBL763437) Inhibition of platelet-derived growth factor receptor beta phosphorylation in MG63 cells in the absence of plasma
- ChEMBL_158732 (CHEMBL768739) IC50 value was determined against Prostaglandin G/H synthase 1 of human platelet rich plasma; Not active
- ChEMBL_1589711 (CHEMBL3829866) Binding affinity to RXRalpha-LBD (unknown origin) measured up to 300 sec by surface plasma resonance method
- ChEMBL_1615951 (CHEMBL3858020) Inhibition of human plasma BuChE using S-butyrylthiocholine iodide as substrate after 30 mins by Ellman's method
- ChEMBL_162869 (CHEMBL767230) Inhibition of platelet aggregation using Adenosine diphosphate (ADP) as activating agent in rabbit platelet rich plasma (PRP)
- ChEMBL_1628764 (CHEMBL3871390) Agonist activity at PGI2 in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation
- ChEMBL_1649602 (CHEMBL3998736) Binding affinity to RXRalpha-LBD (unknown origin) measured up to 120 sec by surface plasma resonance method
- ChEMBL_166182 (CHEMBL879108) Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
- ChEMBL_1888871 (CHEMBL4390548) Inhibition of porcine pancreatic lipase using pNPB as substrate measured after 30 mins using plasma treated sample
- ChEMBL_1908155 (CHEMBL4410513) Inhibition of human plasma kallikrein using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate
- ChEMBL_1923122 (CHEMBL4426078) Inhibition of human plasma kallikrein using Mes-DArg-Pro-Arg-AMC as substrate by Dixon plot analysis
- ChEMBL_2046809 (CHEMBL4701508) Displacement of FITC-diclofenac from human plasma derived TTR measured after overnight incubation by fluorescence polarization assay
- ChEMBL_2125982 (CHEMBL4835327) Inhibition of recombinant human plasma CPN incubated for 25 mins using hippuryl-arginine as substrate by spectrophotometry
- ChEMBL_2201900 (CHEMBL5114608) Reactivation of tabun induced inhibition of BChE in human plasma using ATCh as substrate by Ellman's method
- ChEMBL_2228779 (CHEMBL5142292) Displacement of 125I-labeled angiotensin I from from human plasma renin by gamma counter based competitive radioimmunoassay
- ChEMBL_306667 (CHEMBL832268) In vitro inhibition of Platelet derived growth factor receptor beta autophosphorylation in MG-63 cells without plasma
- ChEMBL_425879 (CHEMBL907940) Activity at human DP receptor in platelet rich plasma assessed as inhibition of PGD2-induced cAMP accumulation
- ChEMBL_501293 (CHEMBL971479) Antagonist activity at TP1 in human platelet-rich plasma assessed as inhibition of U44619-induced platelet aggregation
- ChEMBL_542645 (CHEMBL1015034) Inhibition of CETP-mediated transfer of [3H]cholesteryl ester from HDL in human plasma after 18 hrs
- ChEMBL_542648 (CHEMBL1015037) Inhibition of CETP-mediated transfer of cholesteryl ester to LDL/VLDL in human plasma by Roar assay
- ChEMBL_655590 (CHEMBL1244634) Inhibition of human plasma kallikrein using Z-Phe-Arg-AMC substrate after 30 mins by spectrophotometric assay
- ChEMBL_73016 (CHEMBL681695) Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
- ChEMBL_762816 (CHEMBL1816173) Inhibition of DPP4 in rat plasma incubated for 60 mins using H-lys-Ala-pNA.2HCl substrate
- ChEMBL_89718 (CHEMBL696421) Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma (PRP)
- ChEMBL_89719 (CHEMBL696422) Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma PRP
- ChEMBL_979177 (CHEMBL2421977) Inhibition of cynomolgus monkey plasma renin assessed as angiotensin 1 level after 60 mins by competitive radioimmunoassay
- ChEMBL_1351825 (CHEMBL3271331) Inhibition of human plasma kallikrein using S-2302 as substrate at 25 degC after 20 to 180 mins
- ChEMBL_1351826 (CHEMBL3271332) Inhibition of human plasma kallikrein using S-2302 as substrate at 37 degC after 20 to 180 mins
- ChEMBL_1435760 (CHEMBL3388952) Inhibition of human ADAMTS-5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide substrate by AlphaScreen assay in presence of 50% rat plasma
- ChEMBL_1540253 (CHEMBL3738914) Inhibition of human plasma kallikrein for 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
- ChEMBL_1540254 (CHEMBL3738915) Inhibition of mouse plasma kallikrein for 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
- ChEMBL_158652 (CHEMBL763438) Inhibition of platelet derived growth factor receptor beta phosphorylation in MG63 cells in the presence of human plasma
- ChEMBL_1856733 (CHEMBL4357462) Inhibition of G-alphaq/11 in human platelet rich plasma assessed as inhibition of ADP-mediated platelet aggregation
- ChEMBL_2148790 (CHEMBL5033188) Binding affinity to human plasma TTR tetramer assessed as displacement of diclofenac-coupled FITC by fluorescence polarization assay
- ChEMBL_2172606 (CHEMBL5057740) Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
- ChEMBL_2201899 (CHEMBL5114607) Reactivation of OP compound induced inhibition of BChE in human plasma using ATCh as substrate by Ellman's method
- ChEMBL_2273962 Inhibition of human plasma kallikrein using H-D-Pro-Phe-Arg-p-nitroaniline as substrate assessed as inhibition constant
- ChEMBL_2306843 Inhibition of CD73 in human plasma incubated for 15 mins in presence of 15N5-AMP by LC/MS analysis
- ChEMBL_2306849 Inhibition of CD73 in mouse plasma incubated for 5 mins in presence of 15N5-AMP by LC/MS analysis
- ChEMBL_2496624 Inhibition of beta-FXIIa in human plasma using S-2302 as substrate incubated for 10 mins by chromogenic assay
- ChEMBL_33317 (CHEMBL645613) Inhibition of [3H]p-aminoclonidine (PAC) binding to alpha-2 adrenergic receptor of purified human platelet plasma membranes
- ChEMBL_459075 (CHEMBL925169) Inhibition of human CETP assessed as transfer of [3H]cholesterol esters from HDL to LDL in humna plasma
- ChEMBL_461809 (CHEMBL928938) Displacement of [125I]IP-10 from CXCR3 receptor expressed in human PBMC in EDTA-anti-coagulated human plasma
- ChEMBL_461810 (CHEMBL928939) Antagonist activity at CXCR3 assessed as ITAC-mediated migration of human PBMC in presence of 100% human plasma
- ChEMBL_590737 (CHEMBL1049137) Inhibition of MAO-B from Wistar rat brain by radioenzymatic assay in presence of human platelet rich plasma
- ChEMBL_615619 (CHEMBL1104193) Inhibition of human plasma CETP assessed as [3H]cholesterol ester transfer after 18 hrs by scintillation proximity assay
- ChEMBL_619907 (CHEMBL1110297) Inhibition of human rennin in human plasma assessed as accumulation of angiotensin 1 using human tetradecapeptide by immunoassay
- ChEMBL_759351 (CHEMBL1809814) Inhibition of human plasma thrombin benzoyl-Phe-Val-Arg-7-amino-4-methylcoumarin as substrate by spectrophotometric analysis
- ChEMBL_817423 (CHEMBL2027646) Inhibition of renin in human plasma assessed as formation of angiotensin1 product after 90 mins by competitive radioimmunoassay
- ChEMBL_818747 (CHEMBL2033274) Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry
- ChEMBL_829364 (CHEMBL2060155) Inhibition of BuChE in Wistar rat plasma using acetylthiocholine iodide as substrate after 0.5 hrs by Ellman's method
- ChEMBL_833218 (CHEMBL2067582) Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma
- ChEMBL_850194 (CHEMBL2149800) Inhibition of DPP4 in human plasma using GLY-Pro-MCA as substrate after 60 mins by fluorescence assay
- ChEMBL_850195 (CHEMBL2149801) Inhibition of DPP4 in rat plasma using GLY-Pro-MCA as substrate after 60 mins by fluorescence assay
- ChEMBL_860698 (CHEMBL2168015) Inhibition of CETP-mediated [3H]cholesteryl ester transfer activity in human plasma after 2.5 hrs by scintillation counter
- ChEMBL_90007 (CHEMBL701680) Compound was evaluated for the inhibition of platelet aggregation, assessed turbidimetrically in citreated human platelet rich plasma (PRP)
- Plasma Kallikrein assay Plasma kallikrein determinations were made in 0.1 M sodium phosphate buffer at a pH of 7.5 containing 0.1-0.2 M sodium chloride and 0.5% PEG 8000. Determinations were made using purified human plasma kallikrein (Enzyme Research Laboratories) at a final assay concentration of 200 pM and the synthetic substrate S-2302 (H-(D)-Pro-Phe-Arg-pNA; CHROMOGENIX) at a concentration of 0.00008-0.0004 M.
- ChEBML_158917 Inhibitory activity against human prostaglandin G/H synthase 1 in platelet-rich plasma measured by the presence of thromboxane A2
- ChEBML_1619507 Inhibition of activated human plasma TAFI incubated for 15 mins in presence of 1% human serum albumin by chromogenic assay
- ChEMBL_1295409 (CHEMBL3131046) Inhibition of Streptococcus pyogenes UMAA2616 streptokinase assessed as plasmin activity in human plasma after 24 hrs by colorimetric analysis
- ChEMBL_1431796 (CHEMBL3385092) Inhibition of neutrophil elastase in human plasma using MeOSuc-Ala-Ala-Pro-Val-AMC as substrate by fluorescence assay
- ChEMBL_1454020 (CHEMBL3367079) Antagonist activity at P2Y12 receptor in Sprague-Dawley rat platelet rich plasma assessed as inhibition of ADP-induced aggregation
- ChEMBL_145923 (CHEMBL752591) Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of plasma membrane homogenates of guinea pig brain
- ChEMBL_1517854 (CHEMBL3620650) Inhibition of neutrophil elastase in human plasma using MeOSuc-Ala-Ala-Pro-Val-AMC as substrate by fluorescence assay
- ChEMBL_1619619 (CHEMBL3861788) Inhibition of Lp-PLA2 in whole human plasma pre-incubated for 15 mins before 2-thio-PAF substrate addition
- ChEMBL_1709730 (CHEMBL4119779) Inhibition of human plasma kallikrein using H-Pro-Phe-Arg-AMC as substrate after 1 hr by fluorescence assay
- ChEMBL_1744979 (CHEMBL4179489) Inhibition of renin in human plasma using angiotensinogen as substrate measured for 90 mins by [125I]-angiotensin based radioimmunoassay
- ChEMBL_1798035 (CHEMBL4270152) Inhibition of thrombin in human platelet rich plasma assessed as reduction in thrombin-induced platelet aggregation after 5 mins
- ChEMBL_1798038 (CHEMBL4270155) Inhibition of thrombin in human platelet rich plasma assessed as reduction in ADP-induced platelet aggregation after 5 mins
- ChEMBL_1856732 (CHEMBL4357461) Inhibition of G-alphaq/11 in human platelet rich plasma assessed as inhibition of ADP-mediated calcium ion mobilization
- ChEMBL_1871030 (CHEMBL4372197) Inhibition of plasma KLK (unknown origin) using Ac-NLTR-pNA as substrate after 30 mins relative to untreated control
- ChEMBL_1930530 (CHEMBL4433781) Binding affinity to human recombinant His/GST-tagged PARP1 catalytic domain (655-end residues) by surface plasma resonance method
- ChEMBL_216098 (CHEMBL817687) In vitro inhibition of ADP (10 uM) and epinephrine (10 uM) induced platelet aggregation of dog platelet rich plasma
- ChEMBL_2229343 (CHEMBL5142856) Inhibition of purified human plasma kallikrein using Acetyl-K- P-R-AFC as substrate by fluorescence based spectrofluorimetric analysis
- ChEMBL_2356231 Inhibition of human plasma Kallikrein using H-Pro-Phe-Arg-AMC as substrate measured after 40 mins by fluorescence assay
- ChEMBL_2356235 Inhibition of human plasma Kallikrein using H-Pro-Phe-Arg-AMC as substrate incubated for 30 mins by fluorometric assay
- ChEMBL_2356241 Inhibition of human plasma Kallikrein using H-Pro-Phe-Arg-AMC as substrate measured for 30 mins by fluorometric assay
- ChEMBL_2357492 Inhibition of human seminal plasma DPP4 using Ala-Pro-paranitroanilide as substrate incubated for 15 mins by fluorescence based analysis
- ChEMBL_306777 (CHEMBL831532) In vitro inhibition of Platelet derived growth factor receptor beta autophosphorylation in MG-63 cells with 45% human plasma
- ChEMBL_463733 (CHEMBL932091) Displacement of [125I]IP10 from human recombinant CXCR3 receptor expressed in IL2-activated human PBMC in presence of plasma
- ChEMBL_501174 (CHEMBL975287) Inhibition of human recombinant rennin in human plasma assessed as accumulation of angiotensin 1 using human tetradecapeptide by immunoassay
- ChEMBL_585134 (CHEMBL1060023) Antagonist activity at human P2Y12 receptor assessed as inhibition of ADP-induced platelet-rich plasma aggregation by turbidimetric method
- ChEMBL_619411 (CHEMBL1104169) Displacement of [125I]-1P10 from human CXCR3 expressed in human PBMC after 2 hrs by scintillation counting in plasma
- ChEMBL_852277 (CHEMBL2155543) Inhibition of CETP in human plasma using [3H]cholesterol ester/HDL as substrate after 10 mins by scintillation counting
- ChEMBL_861803 (CHEMBL2173396) Inhibition of SYK in human platelet-rich plasma assessed as reduction in convulxin-induced GPV1/FcRgamma-mediated platelet aggregation
- ChEMBL_89593 (CHEMBL698785) Inhibition of platelet aggregation induced by 20 uM adenosine 5'-diphosphate (ADP) in human platelet rich plasma (h-PRP).
- ChEMBL_958169 (CHEMBL2384261) Inhibition of COX-2 in human whole blood assessed as inhibition of LPS-induced plasma PGE2 level by radioimmunoassay
- ChEBML_90324 Inhibition of platelet aggregation using human platelet rich plasma (hPRP) assay (200microL, 2-3 x 10e 8 platelets/mL, n=1)
- ChEMBL_1289924 (CHEMBL3119935) Inhibition of COX-2 in human whole blood assessed as PGE2 level in plasma after 5 mins by enzyme immunoassay
- ChEMBL_1364477 (CHEMBL3295025) Displacement of [3H]-PGD2 from human CRTH2 expressed in HEK293 cells in presence of 50% human plasma by scintillation counting
- ChEMBL_1520710 (CHEMBL3625629) Antagonist activity against integrin alpha2bbeta3 open form in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation
- ChEMBL_1520712 (CHEMBL3625631) Antagonist activity against integrin alpha2bbeta3 closed form in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation
- ChEMBL_1543046 (CHEMBL3743969) Inhibition of human plasma thrombin using pyroGlu-Pro-Arg-pNA-HCl as substrate measured for 5 mins by spectrophotometric assay
- ChEMBL_1543049 (CHEMBL3743972) Inhibition of human plasma plasmin using pyroGlu-Pro-Arg-pNA-HCl as substrate measured for 5 mins by spectrophotometric assay
- ChEMBL_1591236 (CHEMBL3829628) Inhibition of ATX in human plasma assessed as inhibition of LPA production after 2 hrs by LC-MS/MS analysis
- ChEMBL_1619507 (CHEMBL3861676) Inhibition of activated human plasma TAFI incubated for 15 mins in presence of 1% human serum albumin by chromogenic assay
- ChEMBL_1765368 (CHEMBL4200615) Inhibition of human plasma kallikrein using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay
- ChEMBL_1798037 (CHEMBL4270154) Inhibition of thrombin in human platelet rich plasma assessed as reduction in arachidonic acid-induced platelet aggregation after 5 mins
- ChEMBL_1929987 (CHEMBL4433163) Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA level after 3 hrs by mass spectrometric analysis
- ChEMBL_2056501 (CHEMBL4711502) Inhibition of BChE in human plasma assessed as reduction in butyrylthiocholineiodide hydrolysis preincubated for 3 mins followed by substrate addition
- ChEMBL_2087002 (CHEMBL4768265) Non competitive inhibition of human plasma BuChE using varying levels of butyrylthiocholine iodide as substrate by Lineweaver-Burk plot analysis
- ChEMBL_2223144 (CHEMBL5136478) Inhibition of human plasma kallikrein assessed as substrate hydrolysis using acetyl-K-P-R-AFC as substrate by spectrofluorometric analysis
- ChEMBL_2244092 (CHEMBL5158302) Inhibition of human plasma BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition by Ellman's method
- ChEMBL_2273952 Inhibition of rat recombinant plasma kallikrein using Z-FR-AMC as substrate assessed as inhibition constant by fluorescence plate reader analysis
- ChEMBL_2356184 Inhibition of human plasma trypsin using Boc-Ile-Glu-Gly-Arg-AMC as substrate measured for 30 mins by fluorometric assay
- ChEMBL_2356185 Inhibition of human plasma thrombin using Boc-Asp(OBzl)-Pro-Arg-AMC as substrate measured for 30 mins by fluorometric assay
- ChEMBL_2356240 Inhibition of human plasma FXa using Boc-Ile-Glu-Gly-Arg-AMC as substrate measured for 30 mins by fluorometric assay
- ChEMBL_595730 (CHEMBL1045253) Inhibition of human somatic ACE in presence of 1:100 diluted SHR rat plasma complemented with 5 uM serum albumin
- ChEMBL_749400 (CHEMBL1785190) Inhibition of purified human plasma BuChE preincubated for 30 mins before DTNB substrate addition by spectrophotometric assay based Ellman's method
- ChEMBL_802810 (CHEMBL1953544) Displacement of [3H]PGD2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of 50% plasma
- ChEMBL_90326 (CHEMBL699169) Inhibition of platelet aggregation induced by 20 uM adenosine 5-diphosphate (ADP) in citreated human platelet rich plasma (h-PRP)
- ChEMBL_970209 (CHEMBL2406476) Inhibition of cMET in human MKN45 cells assessed as phosphorylated MET levels after 4 hrs in presence of mouse plasma
- ChEBML_152620 Binding potency towards PGF-2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)
- ChEBML_209935 Inhibition of thromboxane A2 synthetase as reduced ADP-induced aggregation of human platelet rich plasma in the presence of pig aortal microsomes
- ChEMBL_1363410 (CHEMBL3295545) Binding affinity to full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin in presence of tPA
- ChEMBL_1364479 (CHEMBL3295027) Displacement of [3H]-PGD2 from human DP receptor expressed in HEK293 cells in presence of 50% human plasma by scintillation counting
- ChEMBL_1464283 (CHEMBL3404312) Inhibition of BchE in human plasma incubated for 30 mins using butyrylthiocholine substrate at 37 degC by DTNB dye based spectrophotometry
- ChEMBL_1481882 (CHEMBL3540573) Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
- ChEMBL_149045 (CHEMBL762238) Binding affinity against human oxytocin receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_149057 (CHEMBL873306) Binding affinity against human oxytocin receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_1543050 (CHEMBL3743973) Inhibition of human plasma kallikrein using D-Pro-Phe-Arg-pNA-2HCl as substrate measured for 5 mins by spectrophotometric assay
- ChEMBL_1634330 (CHEMBL3877122) Inhibition of human plasma kallikrein using D-Pro-Phe-Arg-pNA as substrate preincubated for 30 mins followed by substrate addition
- ChEMBL_1698580 (CHEMBL4049562) Antagonist activity at integrin alpha2b beta3 receptor in citrated human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation
- ChEMBL_1925849 (CHEMBL4428921) Inhibition of human BSEP in plasma membrane vesicles after 10 mins in presence of [3H]-taurocholate by topcount based transport assay
- ChEMBL_1929828 (CHEMBL4433004) Inhibition of bovine plasma MAO preincubated for 15 mins followed by addition of benzylamine hydrochloride as substrate measured after 30 mins
- ChEMBL_1930218 (CHEMBL4433469) Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate measured after 30 mins by Ellman's method relative to control
- ChEMBL_2134840 (CHEMBL4844450) Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as substrate measured after 5 mins by microplate reader analysis
- ChEMBL_2231079 (CHEMBL5144851) Inhibition of urea-induced Transthyretin denaturation in human plasma preincubated for 1 hr followed by urea addition by Western blot analysis
- ChEMBL_2262414 (CHEMBL5217425) Inhibition of endogenous human plasma kallikrein using Z-Phe-Arg-AMC.HCl as substrate measured after 5 mins by microplate reader analysis
- ChEMBL_2370552 Covalent inhibition of urea-induced Transthyretin denaturation in human plasma preincubated for 1 hr followed by urea addition by Western blot analysis
- ChEMBL_2454279 Inhibition of human plasma BChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method
- ChEMBL_326140 (CHEMBL862695) Inhibition of poly(Glu4-Tyr)peptide phosphorylation by recombinant VEGFR2 at 10 uM ATP and in presence of 5% mouse plasma
- ChEMBL_467044 (CHEMBL929125) Displacement of 5'-phosphorylated, 2',5'-oligoadenylate from human recombinant RNase L assessed as decrease in resonance by surface plasma resonance
- ChEMBL_585275 (CHEMBL1061890) Antagonist activity at human P2Y12 receptor assessed as inhibition of ADP-induced platelet-rich plasma aggregation by chronolog PRP aggregometry assay
- ChEMBL_619413 (CHEMBL1104171) Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma
- ChEMBL_622646 (CHEMBL1104957) Displacement of [3H]PGD2 from human CRTH2 receptor expressed in 293 cells by scintillation counting in presence of 50% human plasma
- ChEMBL_753403 (CHEMBL1799738) Inhibition of renin in human plasma using Q-FRET substrate pretreated for 10 mins before substrate addition measured after 1 hr
- ChEMBL_795751 (CHEMBL1936638) Displacement of [3H]PGD2 from human CRTh2 receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
- ChEMBL_795752 (CHEMBL1936639) Displacement of [3H]PGD2 from human DP receptor expressed in 293 cells by scintillation counting in presence of 50 % human plasma
- ChEMBL_92380 (CHEMBL701593) Concentration required to inhibit enzymatic cleavage of the chromogenic substrate (H-D-Pro-Phe-Arg-pNA) for plasma kallikrein in vitro.
- Fluorescent Assay The assays were performed by mixing either 0.2 μM E. coli OPPS, Y107A/F108A S. cerevisiae GGPPS, or Y96A/F97A human GGPPS with various concentrations of MANT-O-GPP and cold IPP as specified. For MANT-O-GPP Km measurements, 0.5−5 μM MANT-O-GPP was used with 50 μM cold IPP. For IPP Km and kcat determination, 3.5 μMMANT-O-GPP was utilized to saturate the enzyme with cold IPP from 2 to 50 μM. A standard curve was generated to correlate the fluorescence changes upon incubation with 0.2 μM enzyme, 0.5, 1, 2, 3.5, or 5 μM MANT-O-GPP, and 50 μM cold IPP for 30 min until the reaction reached completion.
- ChEBML_1564075 Inhibition of human plasma kallikrein assessed as reduction in release of p-nitroaniline after 10 to 120 mins by Michaelis-Menten equation analysis
- ChEBML_1717668 Inhibition of Wistar rat plasma angiotensin 1-converting enzyme using H-hippuryl-His-Leu-OH as substrate after 20 mins by fluorescence assay
- ChEMBL_1338846 (CHEMBL3242936) Inhibition of human plasma urokinase using Glu-Gly-Arg-pNA (S-2444) peptide as substrate assessed as reduction of enzyme hydrolytic activity
- ChEMBL_1452195 (CHEMBL3365817) Inhibition of human recombinant renin in presence of human plasma using Ac- IHPFHL-VIHNK-(DY-505-X5)-COOH substrate by fluorimetric assay
- ChEMBL_152620 (CHEMBL762787) Binding potency towards PGF-2 alpha receptor (competitive binding) with natural [3H]-PGF 2 alpha in bovine corpora lutea plasma membranes (BCLM)
- ChEMBL_1540270 (CHEMBL3739101) Inhibition of human wild-type plasma kallikrein catalytic domain after 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
- ChEMBL_1540271 (CHEMBL3739102) Inhibition of human plasma kallikrein catalytic domain E217A mutant after 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
- ChEMBL_1540272 (CHEMBL3739103) Inhibition of human plasma kallikrein catalytic domain E217R mutant after 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
- ChEMBL_1540273 (CHEMBL3739104) Inhibition of human plasma kallikrein catalytic domain G99Y mutant after 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
- ChEMBL_1583725 (CHEMBL3815812) Inhibition of CETP in human whole plasma assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to LDL/VLDL
- ChEMBL_1700908 (CHEMBL4051890) Inhibition of ATX in mouse plasma assessed as reduction in LPA 18:2 production after 2 hrs by LC-MS/MS analysis
- ChEMBL_1700909 (CHEMBL4051891) Inhibition of ATX in rat plasma assessed as reduction in LPA 18:2 production after 2 hrs by LC-MS/MS analysis
- ChEMBL_1700910 (CHEMBL4051892) Inhibition of ATX in human plasma assessed as reduction in LPA 18:2 production after 2 hrs by LC-MS/MS analysis
- ChEMBL_1752777 (CHEMBL4187537) Inhibition of Lp-PLA2 in human plasma LDL fractions using 2-thio platelet-activating factor as substrate by TMB dye based spectrophotometry
- ChEMBL_1979949 (CHEMBL4613084) Inhibition of autotaxin in mouse plasma assessed as reduction in LPA (18:2) production incubated for 2 hrs LC-MS-/MS analysis
- ChEMBL_1979950 (CHEMBL4613085) Inhibition of autotaxin in human plasma assessed as reduction in LPA (18:2) production incubated for 2 hrs LC-MS-/MS analysis
- ChEMBL_2019091 (CHEMBL4672669) Inhibition of purified human plasma thrombin using Boc-Asp(OBzl)-Pro-Arg-AMC substrate incubated for 30 mins by fluorescence based assay
- ChEMBL_214414 (CHEMBL820278) Binding affinity against human vasopressin V1a receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_214687 (CHEMBL817650) Binding affinity against human vasopressin V1b receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_214721 (CHEMBL817921) Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_2162818 (CHEMBL5047679) Inhibition of human plasma vanin-1 using pantetheine-7-amino-4-trifluoromethykournarin as substrate preincubated for 30 mins followed by substrate addition
- ChEMBL_2380668 Displacement of 12G5 antibody from CXCR4 in human SUP-T1 cells in presence of human plasma media by flow cytometry based competitive analysis
- ChEMBL_595037 (CHEMBL1042522) Antagonist activity at P2Y12 receptor in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation by light transmission aggregometry
- ChEMBL_600879 (CHEMBL1042837) Antagonistic activity to CXCR3 receptor expressed in PBMC assessed as inhibition of ITAC-mediated cell migration in presence of 100% human plasma
- ChEMBL_805476 (CHEMBL1955369) Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
- ChEMBL_963755 (CHEMBL2395754) Inhibition of monocyte COX2 in human whole blood assessed as inhibition of LPS-induced plasma PGE2 production after 24 hrs by radioimmunoassay
- ChEMBL_970201 (CHEMBL2406468) Inhibition of aurora-B in human HT-29 cells assessed as phosphorylation of histone H3 at Ser10 in presence of mouse plasma
- ChEBML_1681813 Inhibition of human plasma kallikrein using pyro-Glu-Pro-Arg-pNA as substrate at 37 degC after 10 to 120 mins by spectrophotometric method
- ChEMBL_1481883 (CHEMBL3540574) Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
- ChEMBL_1564075 (CHEMBL3783216) Inhibition of human plasma kallikrein assessed as reduction in release of p-nitroaniline after 10 to 120 mins by Michaelis-Menten equation analysis
- ChEMBL_1620071 (CHEMBL3862354) Binding affinity to human plasma wild type TTR assessed as dissociation constants for second binding site of TTR by isothermal titration calorimetric method
- ChEMBL_1620072 (CHEMBL3862355) Binding affinity to human plasma wild type TTR assessed as dissociation constants for first binding site of TTR by isothermal titration calorimetric method
- ChEMBL_1663585 (CHEMBL4013266) Inhibition of human ADAMTS5 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs in the presence of 50% Lewis rat plasma by Alphascreen assay
- ChEMBL_1922602 (CHEMBL4425558) Inhibition of human ADAMTS5 using 43-mer-VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG as substrate in presence of Lewis rat plasma measured after 3 hrs by AlphaScreen assay
- ChEMBL_2306850 Inhibition of CD73 in human plasma derived from HNSCC cancer patient incubated for 15 mins in presence of 15N5-AMP by LC/MS analysis
- ChEMBL_2306851 Inhibition of CD73 in human plasma derived from ovarian cancer patient incubated for 15 mins in presence of 15N5-AMP by LC/MS analysis
- ChEMBL_2306852 Inhibition of CD73 in human plasma derived from TNBC cancer patient incubated for 15 mins in presence of 15N5-AMP by LC/MS analysis
- ChEMBL_2306853 Inhibition of CD73 in human plasma derived from esophageal cancer patient incubated for 15 mins in presence of 15N5-AMP by LC/MS analysis
- ChEMBL_451545 (CHEMBL900721) Antagonist activity at rat P2X7 receptor transfected in HEK cells assessed as inhibition of benzoyl-ATP-induced changes in plasma membrane pore formation
- ChEMBL_675406 (CHEMBL1273486) Inhibition of recombinant 11betaHSD1 expressed in CHO cells assessed as [3H]-cortisone to [3H]-cortisol by microscintillation plate reader in presence of plasma
- ChEMBL_805217 (CHEMBL1955695) Inhibition of PrCP-mediated angiotensin3 cleavage in mouse plasma using Mca-Ala-Lys-Dnp as substrate for 8 mins by LC/MS analysis
- ChEMBL_805478 (CHEMBL1955371) Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
- ChEMBL_809590 (CHEMBL2015716) Displacement of [3H]-PGH2 from human CRTH2 receptor expressed in HEK293 cells by scintillation counting in presence of buffer containing 50% human plasma
- ChEMBL_815271 (CHEMBL2026486) Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production in presence of plasma
- ChEMBL_852806 (CHEMBL2156113) Binding affinity to human Brd2 containing bromodomain BD1 expressed in Escherichia coli assessed as dissociation constant at 25 degC by surface plasma resonance
- ChEMBL_852807 (CHEMBL2156114) Binding affinity to human Brd2 containing bromodomain BD2 expressed in Escherichia coli assessed as dissociation constant at 25 degC by surface plasma resonance
- ChEMBL_948812 (CHEMBL2339774) Inhibition of human recombinant polyhistidine-tagged plasma kallikrein expressed in Escherichia coli XL1 blue using Z-FR-AMC as substrate by fluorimetric analysis
- ChEBML_1644777 Inhibition of human plasma kallikrein using H-(D)-Pro-Phe-Arg-pNA as substrate after 10 to 120 mins at 37 degC by spectrophotometric method
- ChEBML_86450 Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF.
- ChEMBL_1338845 (CHEMBL3242935) Inhibition of human plasma kallikerin using H-D-Phe-Pro-Arg-pNA (S-2302) peptide as substrate assessed as reduction of enzyme hydrolytic activity
- ChEMBL_146879 (CHEMBL750006) Inhibition of [3H]c[D-Pen2,p-Cl-Phe4,D-Pen5]enkephalin binding to delta opioid receptor of guinea pig brain plasma membrane homogenates
- ChEMBL_1475035 (CHEMBL3424606) Inhibition of thrombin-activated F13-A (unknown origin) in plasma assessed as inhibition of fibrin clot formation after 7 mins by biotin incorporation assay
- ChEMBL_1508576 (CHEMBL3602659) Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis
- ChEMBL_1622747 (CHEMBL3865099) Inhibition of ATX in human plasma assessed as decrease in LPA C18:1 levels after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay
- ChEMBL_1865111 (CHEMBL4366086) Inhibition of CETP in human whole plasma assessed as reduction in [3H]-CE/HDL transfer incubated for 2.5 hrs by topcount scintillation counting assay
- ChEMBL_1925805 (CHEMBL4428877) Inhibition of human plasma kallikrein using Ac-RM(O2)YRpNA as substrate incubated for 30 mins measured for 7 mins by morrison plot analysis
- ChEMBL_2122329 (CHEMBL4831476) Inhibition of human plasma kallikrein using H-Pro-Phe-AMC as fluorogenic substrate measured every 2 mins for 12 mins by microplate reader analysis
- ChEMBL_2134238 (CHEMBL4843848) Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
- ChEMBL_2134838 (CHEMBL4844448) Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as substrate measured after 3 mins by microplate reader analysis
- ChEMBL_2262413 (CHEMBL5217424) Inhibition of purified human plasma kallikrein using H-D-Pro-Phe-Arg-pNA.2HCl as substrate measured after 3 mins by microplate reader analysis
- ChEMBL_2306706 Binding affinity to Influenza A virus recombinant 6 his tagged N-terminal domain of PA endonuclease assessed as dissociation constant by surface plasma resonance analysis
- ChEMBL_862370 (CHEMBL2173314) Inhibition of NHE1 in rat platelet rich plasma assessed as reduction of propionate medium induced platelet swelling measured every 6 secs for 5 mins
- ChEMBL_862404 (CHEMBL2173434) Inhibition of NHE1 in human platelet rich plasma assessed as reduction of propionate medium induced platelet swelling measured every 6 secs for 5 mins
- ChEMBL_89709 (CHEMBL696412) Inhibition of the platelet GPIIb-IIIa receptor measured as ability to attenuate ADP-induced (fibrinogen-mediated) platelet aggregation in human platelet-rich plasma (PRP)
- ChEMBL_937466 (CHEMBL2320214) Inhibition of human plasma kallikrein using H-D-Pro-Phe-Arg-pNA as substrate after 5 to 10 mins by micro plate reader analysis
- ChEMBL_943196 (CHEMBL2346227) Inhibition of human plasma Lp-PLA2 using 2- thio-PAF as substrate incubated for 20 mins prior to substrate addition measured after 1 hr
- Inhibition Assay The inhibition of a microsomal preparation of 11β-HSD1 in the presence of 50% human plasma by compounds of the invention was measured.
- Radioligand Assay Membranes were removed from −80° C., thawed and diluted in cold radioligand assay buffer (20 mM HEPES pH 7.4/5 mM MgCl2/1 mM CaCl2/Roche protease inhibitor)
- ChEMBL_1475048 (CHEMBL3424619) Inhibition of F13-A in human plasma assessed as inhibition of fibrin clot formation by biotin incorporation assay in presence of 1 mM reduced GSH
- ChEMBL_1590872 (CHEMBL3830393) Inhibition of human plasma BChE assessed as butyrylthiocholine hydrolysis preincubated for 10 mins followed by addition of substrate measured after 2 mins by spectrophotometric method
- ChEMBL_1629275 (CHEMBL3871901) Inhibition of rabbit thrombin-induced platelet aggregation in rabbit platelet-rich plasma preincubated with rabbit liver microsomes for 4 hrs followed by addition to platelet
- ChEMBL_1644777 (CHEMBL3993706) Inhibition of human plasma kallikrein using H-(D)-Pro-Phe-Arg-pNA as substrate after 10 to 120 mins at 37 degC by spectrophotometric method
- ChEMBL_1666191 (CHEMBL4015987) Inhibition of IRAK4 in human PBMC assessed as reduction in R848-stimulated TNF alpha production by measuring plasma protein binding corrected IC50 after 3 hrs
- ChEMBL_1675787 (CHEMBL4025930) Inhibition of human plasma BuChE using butyrylthiocholine iodine as substrate pretreated for 10 mins followed by substrate addition measured for 5 mins by Ellman's method
- ChEMBL_1698578 (CHEMBL4049560) Antagonist activity at integrin alpha2b beta3 receptor in human platelet-rich plasma assessed as inhibition of ADP-induced platelets aggregation by light transmittance agregometric analysis
- ChEMBL_1842273 (CHEMBL4342700) Inhibition of human plasma butyrylcholinesterase using butyrylthiocholine as substrate preincubated for 30 mins followed by substrate addition and measured after 25 mins by Ellman's method
- ChEMBL_1888475 (CHEMBL4390152) Inhibition of endothelial lipase in hepatic lipase knock-out mouse plasma using D31-POPC-HDL as substrate incubated for 2 hrs by LC/MS analysis
- ChEMBL_1888476 (CHEMBL4390153) Inhibition of hepatic lipase in endothelial lipase knock-out mouse plasma using D31-POPC-HDL as substrate incubated for 2 hrs by LC/MS analysis
- ChEMBL_1904794 (CHEMBL4407152) Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of SFFLRR-induced platelet aggregation preincubated for 5 mins followed by SFFLRR addition
- ChEMBL_1904795 (CHEMBL4407153) Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 5 mins followed by ADP addition
- ChEMBL_1904796 (CHEMBL4407154) Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation preincubated for 5 mins followed by collagen addition
- ChEMBL_1904797 (CHEMBL4407155) Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of U46619-induced platelet aggregation preincubated for 5 mins followed by U46619 addition
- ChEMBL_1985911 (CHEMBL4619317) Inhibition of LysoPLD activity of ATX in human plasma assessed as reduction in choline release using LPC(16:0) as substrate incubated for 15 hrs
- ChEMBL_2134237 (CHEMBL4843847) Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
- ChEMBL_2261358 (CHEMBL5216369) Inhibition of human plasma BChE using butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by Ellman's method
- ChEMBL_48932 (CHEMBL665927) In vitro concentration required to inhibit 50% of cholesteryl ester transfer protein mediated cholesteryl ester transfer from HDL to VLDL and LDL in human plasma
- ChEMBL_764466 (CHEMBL1821018) Inhibition of DPP4 in human plasma assessed as formation of 7-amino-4-methylcoumarin from glycyl-L-proline 4-methylcoumaryl-7-amide by fluorescence assay
- ChEBML_48936 In vitro inhibition of CETP activity was assessed by measuring the rate of [3H]- cholesteryl ester transfer from HDL to apoprotein B-containing lipoproteins in human plasma
- ChEMBL_1347152 (CHEMBL3253051) Competitive inhibition of 2 X 10'-7 M human plasma kallikrein using Z-Lys-nitrophenyl ester as substrate incubated up to 1 hr at pH 6
- ChEMBL_1657928 (CHEMBL4007540) Inhibition of human plasma BuChE using S-butyrylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method
- ChEMBL_1675783 (CHEMBL4025926) Inhibition of human plasma AChE using acetyl-(beta-methyl)thiocholine as substrate pretreated for 30 mins followed by substrate addition after 25 mins by spectrophotometric method
- ChEMBL_1742673 (CHEMBL4158423) Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELISA
- ChEMBL_1772724 (CHEMBL4229716) Inhibition of factor D in human plasma assessed as decrease in alternative pathway-mediated MAC formation preincubated for 30 mins measured after 30 mins by fluorometer.
- ChEMBL_1825987 (CHEMBL4325751) Inhibition of EL in human HT1080 cells using D31-POPC-HDL as substrate incubated for 2 hrs in presence of mouse plasma by LC/MS analysis
- ChEMBL_1842256 (CHEMBL4342683) Inhibition of human plasma butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 15 mins by Ellman's method
- ChEMBL_1849550 (CHEMBL4350091) Inhibition of human plasma BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition and measured at 6 mins by Ellman's method
- ChEMBL_1855602 (CHEMBL4356331) Inhibition of human plasma kallikrein preincubated for 15 mins followed by H-Pro-Phe-Arg-AMC substrate addition and measured after 30 mins by fluorescence method
- ChEMBL_2088471 (CHEMBL4769734) Inhibition of human plasma AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by Ellman's method
- ChEMBL_2121957 (CHEMBL4831104) Inhibition of BuChE in human plasma using BTC as substrate preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method
- ChEMBL_2200293 (CHEMBL5112809) Inhibition of human plasma kallikrein using H-D-Pro-Phe-Arg-AFC as flurogenic substrate preincubated for 5 mins followed by substrate addition by fluorometer analysis
- ChEMBL_2380669 Displacement of 12G5 antibody from CXCR4 in human SUP-T1 cells in presence of human plasma media incubated for 2 hrs by flow cytometry based competitive analysis
- ChEMBL_2380670 Displacement of 12G5 antibody from CXCR4 in human SUP-T1 cells in presence of human plasma media incubated for 8 hrs by flow cytometry based competitive analysis
- ChEMBL_2443691 Inhibition of bovine plasma VAP-1 using 6-(5-Pheny1-2H-tetrazol-2-yl)hexan-1-amine as substrate measured after 30 mins by UV-HPLC analysis
- ChEMBL_788409 (CHEMBL1918137) Antagonist activity at prostanoid DP receptor in human platelet rich plasma assessed as inhibition of PGD2-induced intracellular cAMP production after 10 mins by enzyme immunoassay
- ChEMBL_801831 (CHEMBL1947443) Inhibition of human plasma plasmin using pyroGlu-Pro-Arg-p-NA.HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry
- ChEMBL_801833 (CHEMBL1947445) Inhibition of human plasma thrombin using pyroGlu-Pro-Arg-p-NA.HCl as substrate preincubated for 15 mins prior substrate addition measured for 10 mins by spectrophotometry
- ChEMBL_2336155 Inhibition of N-terminal hexa-histidine tagged recombinant SARS-CoV-2 nsp14 RNA cap N7-methyltransferase activity expressed in Escherichia coli C2566 using GpppAC4 synthetic RNA and [3H]-SAM as substrate incubated for 30 mins by filter binding assay based liquid scintillation counter analysis
- ChEMBL_2444750 Inhibition of N-terminal His-tagged TOSV cap-ENDO expressed in Escherichia coli BL21 Gold (DE3) using 6-FAM/BHQ-1-labeled 12mer poly(A) ssRNA as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by FRET assay
- ChEMBL_2444751 Inhibition of N-terminal His-tagged ANDV cap-ENDO expressed in Escherichia coli BL21 Gold (DE3) using 6-FAM/BHQ-1-labeled 12mer poly(A) ssRNA as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by FRET assay
- ChEMBL_2444752 Inhibition of N-terminal His-tagged LACV cap-ENDO expressed in Escherichia coli BL21 Gold (DE3) using 6-FAM/BHQ-1-labeled 12mer poly(A) ssRNA as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by FRET assay
- ChEBML_1687651 Inhibition of pig plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
- ChEMBL_1275613 (CHEMBL3090744) Inhibition of Influenza A virus Udorn/72 M2 ion channel V27A mutant expressed in Xenopus oocyte plasma membranes after 2 mins by two-electrode voltage clamp assay
- ChEMBL_1275615 (CHEMBL3090746) Inhibition of Influenza A virus Udorn/72 M2 ion channel S31N mutant expressed in Xenopus oocyte plasma membranes after 2 mins by two-electrode voltage clamp assay
- ChEMBL_1364181 (CHEMBL3292896) Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs
- ChEMBL_1612869 (CHEMBL3854669) Inhibition of human plasma kallikrein using H-(D)-Pro-Phe-Arg-pNA as substrate assessed as release of pNA after 10 to 120 mins by spectrophotometric method
- ChEMBL_1622711 (CHEMBL3865063) Inhibition of ATX in human plasma assessed as decrease in hydrolysis of lysophosphatidylcholine by measuring choline release after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay
- ChEMBL_1653961 (CHEMBL4003327) Inhibition of human plasma AChE using acetyl-(beta-methyl)thiocholine as substrate preincubated for 30 mins followed by substrate addition measured after 25 mins by spectrophotometric method
- ChEMBL_1707129 (CHEMBL4058362) Inhibition of ATX in human plasma using LPC as substrate pretreated for 15 mins followed by substrate addition measured after 3 hrs by LC-MS/MS analysis
- ChEMBL_1762373 (CHEMBL4197620) Inhibition of ENPP2 in human plasma using LPC as substrate preincubated for 15 mins followed by substrate addition measured after 3 hrs by LC-MS/MS analysis
- ChEMBL_1885292 (CHEMBL4386874) Inhibition of human plasma BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured at 2 mins interval by Ellman's method
- ChEMBL_1993977 (CHEMBL4627872) Inhibition of human plasma BChE using S-butyrylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition and measured for 5 mins by Ellman's method
- ChEMBL_2032691 (CHEMBL4686849) Positive allosteric modulation of GABAA alpha1beta3gamma2L in HEK cell plasma membrane assessed as increase in [3H]muscimol binding measured after 10 mins by liquid scintillation counting method
- ChEMBL_2032692 (CHEMBL4686850) Positive allosteric modulation of GABAA alpha1beta3 in HEK cell plasma membrane assessed as increase in [3H]muscimol binding measured after 10 mins by liquid scintillation counting method
- ChEMBL_2032695 (CHEMBL4686853) Positive allosteric modulation of GABAA alpha1beta3gamma2L in HEK cell plasma membrane assessed as increase in [3H]flunitrazepam binding measured after 10 mins by liquid scintillation counting method
- ChEMBL_2077650 (CHEMBL4733441) Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
- ChEMBL_2164415 (CHEMBL5049276) Inhibition of plasma kallikrein (unknown origin) assessed as chromogenic substrate hydrolysis using CS-31(02) as substrate incubated for 1 hr by spectrophotometer based microplate reader method
- ChEMBL_800507 (CHEMBL1948627) Inhibition of human plasma lipoprotein-associated phospholipase A2 using 2-thio-PAF as substrate preincubated for 20 mins measured 1 hr post substrate addition by spectrophotometric analysis
- ChEMBL_826811 (CHEMBL2051432) Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
- ChEMBL_941531 (CHEMBL2330522) Inhibition of plasminogen/fibrinogen interaction in pooled citreated human platelet-poor plasma assessed as inhibition of lysis of CaCl2/t-PA-induced clot by microtiter plate analysis
- ChEMBL_1994363 (CHEMBL4628258) Inhibition of NSD2 (unknown origin) preincubated for 15 mins followed by addition of [3H]-SAM as substrate and peptide solution after 240 mins cold SAM was added measured by radioisotope assay
- Determination of the IC50 for Plasma Kallikrein Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori et al., Biochem. Pharmacol., 1992, 43, 1209; Sturzebecher et al., Biol. Chem. Hoppe-Seyler, 1992, 373, 1025). Human plasma kallikrein (Protogen) was incubated at 25° C. with the fluorogenic substrate H-DPro-Phe-Arg-AFC and various concentrations of the test compound. Residual enzyme activity (initial rate of reaction) was determined by measuring the change in optical absorbance at 410 nm and the IC50 value for the test compound was determined.
- Determination of the IC50 for plasma kallikrein Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori et al., Biochem. Pharmacol., 1992, 43, 1209; Sturzebecher et al., Biol. Chem. Hoppe-Seyler, 1992, 373, 1025). Human plasma kallikrein (Protogen) was incubated at 25° C. with the fluorogenic substrate H-DPro-Phe-Arg-AFC and various concentrations of the test compound. Residual enzyme activity (initial rate of reaction) was determined by measuring the change in optical absorbance at 410 nm and the IC50 value for the test compound was determined.
- Plasma kallikrein assay Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori et al., Biochem. Pharmacol., 1992, 43, 1209; St rzebecher et al., Biol. Chem. Hoppe-Seyler, 1992, 373, 1025). Human plasma kallikrein (Protogen) was incubated at 37° C. with the fluorogenic substrate H-DPro-Phe-Arg-AFC and various concentrations of the test compound. Residual enzyme activity (initial rate of reaction) was determined by measuring the change in optical absorbance at 410 nm and the IC50 value for the test compound was determined.
- Plasma kallikrein inhibitory activity Plasma kallikrein inhibitory activity in vitro was determined using standard published methods (see e.g. Johansen et al., Int. J. Tiss. Reac. 1986, 8, 185; Shori et al., Biochem. Pharmacol., 1992, 43, 1209; St rzebecher et al., Biol. Chem. Hoppe-Seyler, 1992, 373, 1025). Human plasma kallikrein (Protogen) was incubated at 37° C. with the fluorogenic substrate H-DPro-Phe-Arg-AFC and various concentrations of the test compound. Residual enzyme activity (initial rate of reaction) was determined by measuring the change in optical absorbance at 410 nm and the IC50 value for the test compound was determined.
- ChEBML_1694650 Inhibition of P2Y12 in human platelet rich plasma assessed as reduction in ADP-induced platelet aggregation pre-incubated before ADP addition and measured after 10 mins by Bruker spectrophotometry
- ChEMBL_1471014 (CHEMBL3420061) Inhibition of wild type Influenza A virus (A/udorn/1972(H3N2)) M2 channel expressed in Xenopus oocyte plasma membranes after 2 mins by two-electrode voltage clamp assay
- ChEMBL_1471017 (CHEMBL3420249) Inhibition of Influenza A virus (A/udorn/1972(H3N2)) M2 V27A mutant channel expressed in Xenopus oocyte plasma membranes after 2 mins by two-electrode voltage clamp assay
- ChEMBL_1686634 (CHEMBL4037113) Inhibition of GP2b/3a in human platelet-rich plasma assessed as reduction in collagen-induced platelet aggregation preincubated for 1 min followed by collagen addition by aggregometric analysis
- ChEMBL_1687646 (CHEMBL4038125) Inhibition of human plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
- ChEMBL_1772700 (CHEMBL4229692) Inhibition of human plasma C1s using Cbz-Gly-Arg-S-Bzl as substrate preincubated with substrate for 15 mins followed by enzyme addition and measured after 5 mins
- ChEMBL_1830149 (CHEMBL4330023) Inhibition of plasma kallikrein (unknown origin) using Ac-NLTR-pNA as substrate preincubated for 30 mins followed by substrate addition and measured for 7 mins by spectrophotometric method
- ChEMBL_1888464 (CHEMBL4390141) Inhibition of mouse endothelial lipase expressed in HEK293F cells using D31-POPC-HDL as substrate incubated for 2 hrs in presence of mouse plasma by LC/MS analysis
- ChEMBL_2117199 (CHEMBL4826265) Binding affinity to plasma kallikrein (unknown origin) assessed as inhibition constant using D-Pro-Phe,Arg,pNa,2HCl as substrate preincubated for 10 mins followed by substrate addition
- ChEMBL_2134889 (CHEMBL4844499) Inhibition of purified human plasma kallikrein assessed as inhibition constant using H-D-Pro-Phe-Arg-pNA.2HCl as substrate measured after 3 mins by microplate reader analysis
- ChEMBL_2200325 (CHEMBL5112841) Inhibition of DXS induced human whole plasma kallikrein using H-D-Pro-Phe-Arg-AFC as substrate preincubated for 5 mins followed by DXS stimulation by fluorometer analysis
- ChEMBL_2264124 In vivo receptor occupancy in Wistar rat assessed as compound required for 50% 5HT4 receptor occupancy in plasma administered orally measured after 1 hr by LC-MS/MS analysis
- ChEMBL_2352415 Inhibition of DPP4 in human plasma using GP-BAN as fluorescent substrate preincubated for 5 mins followed by substrate addition and measured for 20 mins by microplate reader analysis
- ChEMBL_501292 (CHEMBL971478) Antagonist activity at DP1 in human platelet-rich plasma assessed as inhibition of PGD2-induced [125I]cAMP production preincubated 10 mins before PGD2 challenge by scintillation proximity assay
- ChEMBL_943192 (CHEMBL2346223) Inhibition of human plasma Lp-PLA2 using 2- thio-PAF as substrate incubated for 20 mins prior to substrate addition measured after 1 hr in presence of FeCl3
- ChEMBL_943193 (CHEMBL2346224) Inhibition of human plasma Lp-PLA2 using 2- thio-PAF as substrate incubated for 20 mins prior to substrate addition measured after 1 hr in presence of EDTA
- Inhibition Assay Plasma kallikrein determinations were made in 0.1 M sodium phosphate buffer at a pH of 7.5 containing 0.1-0.2 M sodium chloride and 0.5% PEG 8000. Determinations were made using purified human plasma kallikrein (Enzyme Research Laboratories) at a final assay concentration of 200 pM and the synthetic substrate S-2302 (H-(D)-Pro-Phe-Arg-pNA; CHROMOGENIX ) at a concentration of 0.00008-0.0004 M.
- ChEMBL_1565823 (CHEMBL3789430) Inhibition of histidine-tagged recombinant human full length PI3Kdelta expressed in baculovirus preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 20 mins in presence of MgCl2
- ChEMBL_1565824 (CHEMBL3789431) Inhibition of GST-tagged recombinant human full length VPS34 expressed in baculovirus preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 1 hr in presence of MnCl2
- ChEMBL_2293100 Inhibition of P32-[alpha-GTP] cap radiolabelled RNA binding to recombinant eIF4E (unknown origin) assessed as decrease in cross linked RNA-eIF4E complex formation preincubated with UV radiation for 30 mins followed by RNase addition and measured after 30 mins by SDS-PAGE based autoradiographic analysis
- ChEMBL_1565822 (CHEMBL3789429) Inhibition of histidine-tagged recombinant human full length PI3Kgamma expressed in insect cells preincubated for 15 mins followed by addition of cold ATP/gamma32P-ATP measured after 15 mins in presence of MgCl2
- ChEBML_1696835 Inhibition of porcine pancreatic lipase using p-nitrophenyl butyrate as substrate pretreated for 15 mins followed by substrate addition measured after 15 mins in presence of plasma by spectrophotometric method
- ChEMBL_1570587 (CHEMBL3794955) Agonist activity at human IP receptor in platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation preincubated for 1 min followed by addition of ADP by aggregometry
- ChEMBL_1624820 (CHEMBL3867232) Inhibition of NAMPT in human HT1080 cells assessed as decrease in cell viability by measuring plasma protein binding corrected IC50 after 96 hrs by CyQuant-Direct reagent based assay
- ChEMBL_1823689 (CHEMBL4323453) Inhibition of human plasma BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 2.5 mins by DTNB reagent based spectrometric method
- ChEMBL_2053697 (CHEMBL4708698) Inhibition of human butyrylcholinesterase in plasma using butyrylthiocholineiodide as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured at 2 mins interval by Ellman's method
- ChEMBL_2155710 (CHEMBL5040370) Binding affinity to human plasma kallikrein assessed as inhibition constant using H-D-Prolyl-L-phenylalanyl-L-arginine p-Nitroaniline as substrate measured upto 120 mins by spectrophotometric analysis
- ChEMBL_2249166 (CHEMBL5163376) Inhibition of human plasma thrombin using Z-Gly-Pro-Arg-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by based spectrofluorimetric method
- ChEMBL_48935 (CHEMBL661649) In vitro human CETP inhibitory activity was assessed by measuring the rate of [3H]cholesteryl ester ([3H]CE) from HDL donor particles to LDL acceptor particles using human plasma
- ChEMBL_740128 (CHEMBL1763188) Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma
- ChEMBL_1994361 (CHEMBL4628256) Inhibition of SMYD3 (unknown origin) preincubated for 15 mins followed by addition of [3H]-SAM as substrate and peptide solution after 240 mins cold SAM was added measured after 1 hr by radioisotope assay