AR-A014418 BDBM50229962 CHEMBL259850 N-(4-METHOXYBENZYL)-N'-(5-NITRO-1,3-THIAZOL-2-YL)UREA 1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea
BDBM50601415 AR-12286 FREE BASE Ar-12286 VEROSUDIL
BDBM204984 US9249085, I(ar)
US10106501, Example AR BDBM293085
US20230357139, Compound AR BDBM634026
AR-11324 FREE BASE BDBM50546247 AR-13324 US11485707, Example Reference compound 1 Netarsudil
BDBM50318549 Ac-AR-NH2 CHEMBL1085605
BDBM660464 US20240092799, Compound XXIX-AR
BDBM680882 US20240197735, Example AR-30
CHEMBL1668333 (+)-(S)-ar-turmerone BDBM50335905
Trapidil AR-12008 Trapymin BDBM50240032
US12325697, Compound AR-1 BDBM747466
US20240197735, Example AR-31 BDBM680885
US9890185, Example 15(ar) BDBM381054
BDBM50515430 NETARSUDIL US11608319, Compound AR-13324
CHEMBL1668334 BDBM50335906 (+)-(S)-dihydro-ar-turmerone
CHEMBL3236471 US20240174621, Example AR-25 BDBM50496943
US11608319, Compound AR-13503 BDBM50546246 CHEMBL4753043
Ac-AR-(N-Me)A-NH2 CHEMBL1084620 BDBM50318538
BDBM50397205 AR-C126532XX AZD6140 AZD-6140 TICAGRELOR BRILINTA
CHEMBL369928 AR-C67085 Adenosine triphosphate derivative BDBM50118223 CHEMBL336292
US20240174621, Example AR-30 BDBM677078 WO2012118492, Example 30
US20240174621, Example AR-31 BDBM677079 WO2012118492, Example 31
AR42 (S)-HDAC 42 Ar-42 (S)-HDAC-42 BDBM50475225
Azilsartan medoxomilo TAK-491 Azilsartan medoxomil AR-14 BDBM50646531 Edarbi TAK 491
Wammp-5 BDBM23499 7-methoxycoumarin-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH
CHEMBL1088887 BDBM50315286 aR-6-(10-iodoethyl)-1,2,3,9,10,11-hexamethoxy-6-methyl-5H-dibenzo[a,c]cycloheptene
BDBM50315284 aR-6,7-Dihydro-6-(10-hydroxyethyl)-6-methyl-5H-dibenzo[a,c]cycloheptene-1,2,3,9,10,11-hexaol CHEMBL1089510
Iclaprim BDBM18070 AR-100 5-[(2-cyclopropyl-7,8-dimethoxy-2H-chromen-5-yl)methyl]pyrimidine-2,4-diamine
aR-6,7-dihydro-6-(10-hydroxyethyl)-3,9-dimethoxy-6-methyl-5Hdibenzo[a,c]cycloheptene-1,2,10,11-tetraol CHEMBL1089840 BDBM50315285
(2S)-3-(4-bromophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide Nonsteroidal AR Ligand, S-10 BDBM18669
BDBM18664 Nonsteroidal AR Ligand, R-5 (2R)-3-(4-fluorophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
BDBM18666 Nonsteroidal AR Ligand, S-7 (2S)-3-(4-acetylphenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Nonsteroidal AR Ligand, S-11 BDBM18670 (2S)-2-hydroxy-3-(4-iodophenoxy)-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Nonsteroidal AR Ligand, S-12 (2S)-2-hydroxy-2-methyl-3-(4-methylphenoxy)-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide BDBM18671
Nonsteroidal AR Ligand, S-13 (2S)-2-hydroxy-3-(4-methoxyphenoxy)-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide BDBM18672
Nonsteroidal AR Ligand, S-8 BDBM18667 (2S)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-3-(4-propanoylphenoxy)propanamide
Nonsteroidal AR Ligand, S-9 BDBM18668 (2S)-3-(4-chlorophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
(4'R,4'aR)-2'-amino-4'-(2,6-difluorophenyl)spiro[1,3-dioxolane-2,6'-4,4a,5,7-tetrahydronaphthalene]-1',3',3'-tricarbonitrile cid_661039 MLS000078475 (4'R,4'aR)-2'-azanyl-4'-[2,6-bis(fluoranyl)phenyl]spiro[1,3-dioxolane-2,6'-4,4a,5,7-tetrahydronaphthalene]-1',3',3'-tricarbonitrile BDBM70321 SMR000036559
(2R)-3-[(4-acetamidophenyl)sulfanyl]-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide Nonsteroidal AR Ligand, R-2 BDBM18661
BDBM18676 (2S)-3-[(4-fluorophenyl)amino]-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide Nonsteroidal AR Ligand, S-17
BDBM18677 (2S)-3-[(4-acetamidophenyl)amino]-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide Nonsteroidal AR Ligand, S-18
N-[(2S,11bR)-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-yl]-N-methylbutane-1-sulfonamide hydrochloride WY26703 BDBM81816 AR-1K2981 CAS_82059-49-2 AC1L33GU
US11673886, Example 83 BDBM510904 US11078197, Example 83 5-{[(aR)-6-(3- cyanobenzamido) spiro[3.3]heptan-2- yl]oxy}thieno[3,2- b]pyridine-6- carboxamide
BDBM18665 Nonsteroidal AR Ligand, S-6 BMC185567 S-4 CHEMBL125236 (2S)-3-(4-acetamidophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Nonsteroidal AR Ligand, S-14 tert-butyl N-{4-[(2S)-2-hydroxy-2-methyl-2-{[4-nitro-3-(trifluoromethyl)phenyl]carbamoyl}ethoxy]phenyl}carbamate BDBM18673
Nonsteroidal AR Ligand, S-15 (2S)-2-hydroxy-3-[4-(1H-indol-5-yl)phenoxy]-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide BDBM18674
Nonsteroidal AR Ligand, S-5 BMC185567 S-1 (2S)-3-(4-fluorophenoxy)-2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide CHEMBL124718 BDBM18663
5-chloro-3-({4-[(2,4-diaminopyrimidin-5-yl)methyl]-6,7-dimethoxy-1-benzofuran-2-yl}methyl)-N,N-dimethyl-1H-indole-2-carboxamide AR-709 BDBM18071
BDBM18675 BMC146525 arylisothiocyanato derivative, S-23 (2S)-2-hydroxy-3-(4-isothiocyanatophenoxy)-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide Nonsteroidal AR Ligand, S-16
BDBM510916 US11078197, Example 95 2,3-dimethyl-5- {[(aR)-6-(3- cyanobenzamido) spiro[3.3]heptan-2- yl]oxy}thieno[3,2- b]pyridine-6- carboxamide US11673886, Example 95
US11078197, Example 98 US11673886, Example 98 3-methyl-5-{[(aR)-6-(3- cyanobenzamido) spiro[3.3]heptan-2- yl]oxy}thieno[3,2- b]pyridine-6- carboxamide BDBM510919
methyl 2-((3aS, aR)-6-(2-(2H-1,2,3-triazol-2- yl)benzoyl)octahydro-1H-pyrrolo[2,3- c]pyridin-1-yl)thiazole-4-carboxylate US9938276, B17 BDBM387122
BDBM351977 4-(5-fluoro-2-methoxyphenyl)-2-((3 aR,6aS)-2-(methylsulfonyl)-1,2,3,3a,4,6a-hexahydrocyclopenta[c]pyrrol-5-yl)-1H-pyrrolo[2,3-b]pyridine US9796708, Example 264
BDBM571968 2-{[(aR)-6-{2,5- dioxo-4-[2-(2,2,2- trifluoroethoxy)- ethyl]imidazolidin- 1-yl}spiro[3.3]- heptan-2-yl]oxy}- pyridine-3-carbox- amide US11447487, Example 61
US11078197, Example 85 2-{[(aR)-6-(3- cyanobenzamido) spiro[3.3]heptan-2- yl]oxy}-5H,7H,8H- pyrano[4,3- b]pyridine-3- carboxamide BDBM510906 US11673886, Example 85
US11673886, Example 102 BDBM510923 US11078197, Example 102 1-methyl-6-{[(aR)-6-(3- cyanobenzamido) spiro[3.3]heptan-2- yl]oxy}-1H- pyrazolo[3,4- b]pyridine-5- carboxamide
2-cyclopropyl-4- {[(aR)-6-[6-(2,2,2- trifluoroethoxy)pyrazolo [1,5-a]pyridine-3- amido]spiro[3.3] heptan-2-yl]oxy}-1,3- thiazole-5- carboxamide US11078197, Example 62 BDBM510885
2-{[(aR)-6-[3- (cyanomethyl) benzamido] spiro[3.3]heptan- 2-yl]oxy}- 5H,7H,8H- pyrano[4,3- b]pyridine-3- carboxamide US11078197, Example 88 US11673886, Example 88 BDBM510909
BDBM510839 1-phenyl-3-({(aR)- 6-[6-(3,3,3- trifluoropropoxy) pyrazolo[1,5- a]pyridine-3- amido]spiro[3.3] heptan-2-yl}oxy)-1H- pyrazole-4- carboxamide US11078197, Example 16
BDBM510925 1-cyclopropyl-3- {[(aR)-6-(4-benzyl-2,5- dioxoimidazolidin- 1-yl)spiro[3.3]heptan- 2-yl]oxy}-1H- pyrazole-4- carboxamide US11673886, Example 104 US11078197, Example 104
BDBM510932 2-cyclopropyl-4- {[(aR)-6-[4-(2- methylpropyl)-2,5- dioxoimidazolidin-1- yl]spiro[3.3]heptan- 2-yl]oxy}-1,3- thiazole-5- carboxamide, diastereomer 2 US11078197, Example 111
US11078197, Example 108 2-cyclopropyl-4- {[(aR)-6-(4-ethyl-2,5- dioxoimidazolidin- 1-yl)spiro[3.3]heptan- 2-yl]oxy}-1,3- thiazole-5- carboxamide US11673886, Example 108 BDBM510929
US11078197, Example 86 5-{[(aR)-6-(4-benzyl-2,6- dioxopiperazin-1- yl)spiro[3.3]heptan- 2-yl]oxy}thieno[3,2- b]pyridine-6- carboxamide US11673886, Example 86 BDBM510907
- Hicks, JW; Wilson, AA; Rubie, EA; Woodgett, JR; Houle, S; Vasdev, N Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [(11)C-carbonyl] AR-A014418 by [(11)C]CO(2) fixation. Bioorg Med Chem Lett 22: 2099-101 (2012)
- Yang, Y; Lv, G; Xiu, R; Yang, H; Wang, W; Yu, P; Zhang, J; Ye, L; Wang, H; Tian, J Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer. Eur J Med Chem 271:
- Xiang, W; Zhao, L; Han, X; Xu, T; Kregel, S; Wang, M; Miao, B; Qin, C; Wang, M; McEachern, D; Lu, J; Bai, L; Yang, CY; Kirchhoff, PD; Takyi-Williams, J; Wang, L; Wen, B; Sun, D; Ator, M; Mckean, R; Chinnaiyan, AM; Wang, S Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer. J Med Chem 66: 13280-13303 (2023)
- MUKHIJA, S; BANDERA, M; PARISI, S; RIGO, S; LIEB, S; LOCIURO, S; GILLESSEN, D; ISLAM, K AR-709-An Investigational diaminopyrimidine: Inhibition, Binding and Mode of Action. Interscience Conference on Antimicrobial Agents in Chemotherapy 1-1 (2006)
- Ohta, K; Goto, T; Fijii, S; Suzuki, T; Ohta, S; Endo, Y Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring. Bioorg Med Chem 16: 8022-8 (2008)
- Tng, J; Lim, J; Wu, KC; Lucke, AJ; Xu, W; Reid, RC; Fairlie, DP Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation. J Med Chem 63: 5956-5971 (2020)
- Xu, F; Chen, H; Xu, J; Liang, X; He, X; Shao, B; Sun, X; Li, B; Deng, X; Yuan, M Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH. Bioorg Med Chem 23: 7735-42 (2015)
- Vidaluc, JL; Calmel, F; Bigg, DC; Carilla, E; Briley, M Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation. J Med Chem 38: 2969-73 (1995)
- Wasilewska, A; Sączewski, F; Hudson, AL; Ferdousi, M; Scheinin, M; Laurila, JM; Rybczyńska, A; Boblewski, K; Lehmann, A Fluorinated analogues of marsanidine, a highly α2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities. Eur J Med Chem 87: 386-97 (2014)
- Takeda, K; Terauchi, T; Hashizume, M; Shin, K; Ino, M; Shibata, H; Yonaga, M Design, synthesis, and structure-activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF1 receptor antagonists. Bioorg Med Chem Lett 22: 5372-8 (2012)
- Hu, R; Wang, WL; Yang, YY; Hu, XT; Wang, QW; Zuo, WQ; Xu, Y; Feng, Q; Wang, NY Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor. Eur J Med Chem 227: (2022)
- Han, X; Wang, C; Qin, C; Xiang, W; Fernandez-Salas, E; Yang, CY; Wang, M; Zhao, L; Xu, T; Chinnaswamy, K; Delproposto, J; Stuckey, J; Wang, S Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem 62: 941-964 (2019)
- Yoshida, K; Itoyama, R; Yamahira, M; Tanaka, J; Loaëc, N; Lozach, O; Durieu, E; Fukuda, T; Ishibashi, F; Meijer, L; Iwao, M Synthesis, resolution, and biological evaluation of atropisomeric (aR)- and (aS)-16-methyllamellarins N: unique effects of the axial chirality on the selectivity of protein kinases inhibition. J Med Chem 56: 7289-301 (2013)
- Abduelkarem, AR; Anbar, HS; Zaraei, SO; Alfar, AA; Al-Zoubi, OS; Abdelkarem, EG; El-Gamal, MI Eur J Med Chem 188: (2020)
- Clemens, JJ; Abela, AR; Anderson, CD; Busch, BB; Chen, WG; Cleveland, T; Coon, TR; Frieman, B; Ghirmai, SG; Grootenhuis, P; Gulevich, AV; Hadida Ruah, SS; Hsia, CK; Kang, P; Khatuya, H; McCartney, J; Miller, MT; Paraselli, P; Pierre, F; Swift, SE; Termin, A; Uy, J; Vogel, CV; Zhou, J US Patent US11866450 (2024)
- Lee, S; Ali, AR; Abed, DA; Nguyen, MU; Verzi, MP; Hu, L Eur J Med Chem 265:
- Vu, LY; Luo, D; Johnson, K; Denehy, ED; Songrady, JC; Martin, J; Trivedi, R; Alsum, AR; Shaykin, JD; Chaudhary, CL; Woloshin, EJ; Kornberger, L; Bhuiyan, N; Parkin, S; Jiang, Q; Che, T; Alilain, W; Turner, JR; Bardo, MT; Prisinzano, TE J Med Chem 67: 9173-9193
- Anas, AR; Kisugi, T; Umezawa, T; Matsuda, F; Campitelli, MR; Quinn, RJ; Okino, T J Nat Prod 75: 1546-52 (2012)
- Wilson, KJ; Witter, DJ; Daniels, MH; Angeles, AR; Siliphaivanh, P; Sloman, D; O'Boyle, B; Falcone, D; White, C; Ferguson, R; Zhou, W; Lipford, K; Mansoor, UF; Fevrier, S; Huang, X; Kurukulasuriya, R; Richard, JE; Tang, S; Boyce, C; Kozlowski, J; Bakshi, RK; Karunakaran, GB US Patent US9226922 (2016)
- Wijeratne, EM; Gunaherath, GM; Chapla, VM; Tillotson, J; de la Cruz, F; Kang, M; U'Ren, JM; Araujo, AR; Arnold, AE; Chapman, E; Gunatilaka, AA J Nat Prod 79: 340-52 (2016)
- Moas-Héloire, V; Renault, N; Batalha, V; Arias, AR; Marchivie, M; Yous, S; Deguine, N; Buée, L; Chavatte, P; Blum, D; Lopes, L; Melnyk, P; Agouridas, L Eur J Med Chem 106: 15-25 (2015)
- BELL, AS; BESNARD, J; BRADLEY, AR; GREEN, L; HAAP, W; KOCER, B; KUGLSTATTER, A; LUCAS, X; MATTEI, P; MAZUNIN, D; RIEMER, C; VAN HOORN, WP US Patent US20230382911 (2023)
- Fantini, M; Rivara, M; Zuliani, V; Kalmar, CL; Vacondio, F; Silva, C; Baheti, AR; Singh, N; Merrick, EC; Katari, RS; Cocconcelli, G; Ghiron, C; Patel, MK Bioorg Med Chem 17: 3642-8 (2009)
- Orafaie, A; Sadeghian, H; Bahrami, AR; Rafatpanah, H; Matin, MM Bioorg Med Chem 30: (2021)
- Dixon, DD; Sethumadhavan, D; Benneche, T; Banaag, AR; Tius, MA; Thakur, GA; Bowman, A; Wood, JT; Makriyannis, A J Med Chem 53: 5656-66 (2010)
- Ajmera, S; Bapat, AR; Danenberg, K; Danenberg, PV J Med Chem 27: 11-4 (1984)
- Semple, G; Ryder, H; Kendrick, DA; Batt, AR; Mathews, E; Rooker, DP; Szelke, M; Nishida, A; Miyata, K Bioorg Med Chem Lett 6: 2971-2976 (1996)
- Flipo, M; Willand, N; Lecat-Guillet, N; Hounsou, C; Desroses, M; Leroux, F; Lens, Z; Villeret, V; Wohlkönig, A; Wintjens, R; Christophe, T; Kyoung Jeon, H; Locht, C; Brodin, P; Baulard, AR; Déprez, B J Med Chem 55: 6391-402 (2012)
- Fischer, B; Chulkin, A; Boyer, JL; Harden, KT; Gendron, FP; Beaudoin, AR; Chapal, J; Hillaire-Buys, D; Petit, P J Med Chem 42: 3636-46 (1999)
- Beauglehole, AR; Baker, SP; Scammells, PJ J Med Chem 43: 4973-80 (2001)
- Günther, S; Reinke, PY; Fernández-García, Y; Lieske, J; Lane, TJ; Ginn, HM; Koua, FH; Ehrt, C; Ewert, W; Oberthuer, D; Yefanov, O; Meier, S; Lorenzen, K; Krichel, B; Kopicki, J; Gelisio, L; Brehm, W; Dunkel, I; Seychell, B; Gieseler, H; Norton-Baker, B; Escudero-Pérez, B; Domaracky, M; Saouane, S; Tolstikova, A; White, TA; Hänle, A; Groessler, M; Fleckenstein, H; Trost, F; Galchenkova, M; Gevorkov, Y; Li, C; Awel, S; Peck, A; Barthelmess, M; Schlünzen, F; Xavier, PL; Werner, N; Andaleeb, H; Ullah, N; Falke, S; Srinivasan, V; Franca, BA; Schwinzer, M; Brognaro, H; Rogers, C; Melo, D; Zaitsev-Doyle, JJ; Knoska, J; Peña Murillo, GE; Mashhour, AR; Guicking, F; Hennicke, V; Fischer, P; Hakanpää, J; Meyer, J; Gribbon, P; Ellinger, B; Kuzikov, M; Wolf, M; Beccari, AR; Bourenkov, G; Stetten, D; Pompidor, G; Bento, I; Panneerselvam, S; Karpics, I; Schneider, TR; Garcia Alai, MM; Niebling, S; Günther, C; Schmidt, C; Schubert, R; Han, H; Boger, J; Monteiro, DC; Zhang, L; Sun, X; Pletzer-Zelgert, J; Wollenhaupt, J; Feiler, CG; Weiss, MS; Schulz, E; Mehrabi, P; Karničar, K; Usenik, A; Loboda, J; Tidow, H; Chari, A; Hilgenfeld, R; Uetrecht, C; Cox, R; Zaliani, A; Beck, T; Rarey, M; Günther, S; Turk, D; Hinrichs, W; Chapman, HN; Pearson, AR; Betzel, C; Meents, A bioRxiv 2020: (2020)
- Mansour, TS; Jin, H; Wang, W; Hooker, EU; Ashman, C; Cammack, N; Salomon, H; Belmonte, AR; Wainberg, MA J Med Chem 38: 1-4 (1995)
- Sorrentino, F; Karioti, A; Gratteri, P; Rigobello, MP; Scutari, G; Messori, L; Bindoli, A; Chioccioli, M; Gabbiani, C; Bergonzi, MC; Bilia, AR Bioorg Med Chem 19: 631-41 (2011)
- Blaazer, AR; Lange, JH; van der Neut, MA; Mulder, A; den Boon, FS; Werkman, TR; Kruse, CG; Wadman, WJ Eur J Med Chem 46: 5086-98 (2011)
- Winneroski, LL; Erickson, JA; Green, SJ; Lopez, JE; Stout, SL; Porter, WJ; Timm, DE; Audia, JE; Barberis, M; Beck, JP; Boggs, LN; Borders, AR; Boyer, RD; Brier, RA; Hembre, EJ; Hendle, J; Garcia-Losada, P; Minguez, JM; Mathes, BM; May, PC; Monk, SA; Rankovic, Z; Shi, Y; Watson, BM; Yang, Z; Mergott, DJ Bioorg Med Chem 28: (2020)
- Wu, ES; Cole, TE; Davidson, TA; Dailey, MA; Doring, KG; Fedorchuk, M; Loch, JT; Thomas, TL; Blosser, JC; Borrelli, AR J Med Chem 32: 183-92 (1989)
- Wu, C; Decker, ER; Blok, N; Li, J; Bourgoyne, AR; Bui, H; Keller, KM; Knowles, V; Li, W; Stavros, FD; Holland, GW; Brock, TA; Dixon, RA J Med Chem 44: 1211-6 (2001)
- Zhang, A; Zhang, Y; Branfman, AR; Baldessarini, RJ; Neumeyer, JL J Med Chem 50: 171-81 (2007)
- Liu, Z; Chen, H; Wang, P; Li, Y; Wold, EA; Leonard, PG; Joseph, S; Brasier, AR; Tian, B; Zhou, J J Med Chem 63: 5242-5256 (2020)
- Ray, P; Wright, J; Adam, J; Boucharens, S; Black, D; Brown, AR; Epemolu, O; Fletcher, D; Huggett, M; Jones, P; Laats, S; Lyons, A; de Man, J; Morphy, R; Sherborne, B; Sherry, L; Straten, Nv; Westwood, P; York, M Bioorg Med Chem Lett 21: 1084-8 (2011)
- Guzman-Perez, A; Wester, RT; Allen, MC; Brown, JA; Buchholz, AR; Cook, ER; Day, WW; Hamanaka, ES; Kennedy, SP; Knight, DR; Kowalczyk, PJ; Marala, RB; Mularski, CJ; Novomisle, WA; Ruggeri, RB; Tracey, WR; Hill, RJ Bioorg Med Chem Lett 11: 803-7 (2001)
- Bulusu, AR US Patent US9120808 (2015)
- Benaim, G; Sanders, JM; Garcia-Marchán, Y; Colina, C; Lira, R; Caldera, AR; Payares, G; Sanoja, C; Burgos, JM; Leon-Rossell, A; Concepcion, JL; Schijman, AG; Levin, M; Oldfield, E; Urbina, JA J Med Chem 49: 892-9 (2006)
- Wilson, DM; Apps, J; Bailey, N; Bamford, MJ; Beresford, IJ; Briggs, MA; Calver, AR; Crook, B; Davis, RP; Davis, S; Dean, DK; Harris, L; Heightman, TD; Panchal, T; Parr, CA; Quashie, N; Steadman, JG; Schogger, J; Sehmi, SS; Stean, TO; Takle, AK; Trail, BK; White, T; Witherington, J; Worby, A; Medhurst, AD Bioorg Med Chem Lett 23: 6897-901 (2013)
- Nuti, E; Cantelmo, AR; Gallo, C; Bruno, A; Bassani, B; Camodeca, C; Tuccinardi, T; Vera, L; Orlandini, E; Nencetti, S; Stura, EA; Martinelli, A; Dive, V; Albini, A; Rossello, A J Med Chem 58: 7224-40 (2015)
- Katavic, PL; Venables, DA; Rali, T; Carroll, AR J Nat Prod 70: 866-8 (2007)
- Goodnow, RA; Hicks, A; Sidduri, A; Kowalczyk, A; Dominique, R; Qiao, Q; Lou, JP; Gillespie, P; Fotouhi, N; Tilley, J; Cohen, N; Choudhry, S; Cavallo, G; Tannu, SA; Ventre, JD; Lavelle, D; Tare, NS; Oh, H; Lamb, M; Kurylko, G; Hamid, R; Wright, MB; Pamidimukkala, A; Egan, T; Gubler, U; Hoffman, AF; Wei, X; Li, YL; O'Neil, J; Marcano, R; Pozzani, K; Molinaro, T; Santiago, J; Singer, L; Hargaden, M; Moore, D; Catala, AR; Chao, LC; Hermann, G; Venkat, R; Mancebo, H; Renzetti, LM J Med Chem 53: 3502-16 (2010)
- Shuttleworth, SJ; Tomassi, CD; Cecil, AR; MacCormick, S; Nodes, WJ; Silva, FA US Patent US10150763 (2018)
- Machado, V; Cenci, AR; Teixeira, KF; Sens, L; Tizziani, T; Nunes, RJ; Ferreira, LLG; Yunes, RA; Sandjo, LP; Andricopulo, AD; de Oliveira, AS RSC Med Chem 13: 1644-1656 (2022)
- Goswami, R; Wohlfahrt, G; Törmäkangas, O; Moilanen, A; Lakshminarasimhan, A; Nagaraj, J; Arumugam, KN; Mukherjee, S; Chacko, AR; Krishnamurthy, NR; Jaleel, M; Palakurthy, RK; Samiulla, DS; Ramachandra, M Bioorg Med Chem Lett 25: 5309-14 (2015)
- Medina, JR; Becker, CJ; Blackledge, CW; Duquenne, C; Feng, Y; Grant, SW; Heerding, D; Li, WH; Miller, WH; Romeril, SP; Scherzer, D; Shu, A; Bobko, MA; Chadderton, AR; Dumble, M; Gardiner, CM; Gilbert, S; Liu, Q; Rabindran, SK; Sudakin, V; Xiang, H; Brady, PG; Campobasso, N; Ward, P; Axten, JM J Med Chem 54: 1871-95 (2011)
- Lew, A; Chamberlin, AR Bioorg Med Chem Lett 9: 3267-72 (2000)
- Kumar, G; Das, C; Acharya, A; Bhal, S; Joshi, M; Kundu, CN; Choudhury, AR; Guchhait, SK Bioorg Med Chem 67: (2022)
- Sandrini, MP; Shannon, O; Clausen, AR; Björck, L; Piskur, J Antimicrob Agents Chemother 51: 2726-32 (2007)
- Taylor, AM; Côté, A; Hewitt, MC; Pastor, R; Leblanc, Y; Nasveschuk, CG; Romero, FA; Crawford, TD; Cantone, N; Jayaram, H; Setser, J; Murray, J; Beresini, MH; de Leon Boenig, G; Chen, Z; Conery, AR; Cummings, RT; Dakin, LA; Flynn, EM; Huang, OW; Kaufman, S; Keller, PJ; Kiefer, JR; Lai, T; Li, Y; Liao, J; Liu, W; Lu, H; Pardo, E; Tsui, V; Wang, J; Wang, Y; Xu, Z; Yan, F; Yu, D; Zawadzke, L; Zhu, X; Zhu, X; Sims, RJ; Cochran, AG; Bellon, S; Audia, JE; Magnuson, S; Albrecht, BK ACS Med Chem Lett 7: 531-6 (2016)
- Austin, RP; Bennion, C; Bonnert, RV; Cheema, L; Cook, AR; Cox, RJ; Ebden, MR; Gaw, A; Grime, K; Meghani, P; Nicholls, D; Phillips, C; Smith, N; Steele, J; Stonehouse, JP Bioorg Med Chem Lett 25: 1616-20 (2015)
- Egbertson, MS; Moritz, HM; Melamed, JY; Han, W; Perlow, DS; Kuo, MS; Embrey, M; Vacca, JP; Zrada, MM; Cortes, AR; Wallace, A; Leonard, Y; Hazuda, DJ; Miller, MD; Felock, PJ; Stillmock, KA; Witmer, MV; Schleif, W; Gabryelski, LJ; Moyer, G; Ellis, JD; Jin, L; Xu, W; Braun, MP; Kassahun, K; Tsou, NN; Young, SD Bioorg Med Chem Lett 17: 1392-8 (2007)
- Govek, SP; Oshiro, G; Anzola, JV; Beauregard, C; Chen, J; Coyle, AR; Gamache, DA; Hellberg, MR; Hsien, JN; Lerch, JM; Liao, JC; Malecha, JW; Staszewski, LM; Thomas, DJ; Yanni, JM; Noble, SA; Shiau, AK Bioorg Med Chem Lett 20: 2928-32 (2010)
- Jobson, NK; Crawford, AR; Dewar, D; Pimlott, SL; Sutherland, A Bioorg Med Chem Lett 18: 4940-3 (2008)
- Dana, D; Davalos, AR; De, S; Rathod, P; Gamage, RK; Huestis, J; Afzal, N; Zavlanov, Y; Paroly, SS; Rotenberg, SA; Subramaniam, G; Mark, KJ; Chang, EJ; Kumar, S Bioorg Med Chem 21: 2975-87 (2013)
- Navidpour, L; Shadnia, H; Shafaroodi, H; Amini, M; Dehpour, AR; Shafiee, A Bioorg Med Chem 15: 1976-82 (2007)
- Gagnon, H; Beauchemin, S; Kwiatkowska, A; Couture, F; D'Anjou, F; Levesque, C; Dufour, F; Desbiens, AR; Vaillancourt, R; Bernard, S; Desjardins, R; Malouin, F; Dory, YL; Day, R J Med Chem 57: 29-41 (2014)
- Sanner, MA; Chappie, TA; Dunaiskis, AR; Fliri, AF; Desai, KA; Zorn, SH; Jackson, ER; Johnson, CG; Morrone, JM; Seymour, PA; Majchrzak, MJ; Faraci, WS; Collins, JL; Duignan, DB; Prete Di, CC; Lee, JS; Trozzi, A Bioorg Med Chem Lett 8: 725-30 (1999)
- Arnold, NJ; Arnold, R; Beer, D; Bhalay, G; Collingwood, SP; Craig, S; Devereux, N; Dodds, M; Dunstan, AR; Fairhurst, RA; Farr, D; Fullerton, JD; Glen, A; Gomez, S; Haberthuer, S; Hatto, JD; Howes, C; Jones, D; Keller, TH; Leuenberger, B; Moser, HE; Muller, I; Naef, R; Nicklin, PA; Sandham, DA; Turner, KL; Tweed, MF; Watson, SJ; Zurini, M Bioorg Med Chem Lett 17: 2376-9 (2007)
- Kumar, B; Kumar, V; Prashar, V; Saini, S; Dwivedi, AR; Bajaj, B; Mehta, D; Parkash, J; Kumar, V Eur J Med Chem 177: 221-234 (2019)
- Ravindranathan, KP; Mandiyan, V; Ekkati, AR; Bae, JH; Schlessinger, J; Jorgensen, WL J Med Chem 53: 1662-72 (2010)
- El Sayed, MT; El-Sharief, MAMS; Zarie, ES; Morsy, NM; Elsheakh, AR; Voronkov, A; Berishvili, V; Hassan, GS Bioorg Med Chem Lett 28: 952-957 (2018)
- Greenspan, PD; Main, AJ; Bhagwat, SS; Barsky, LI; Doti, RA; Engle, AR; Frey, LM; Zhou, H; Lipson, KE; Chin, MH; Jackson, RH; Uziel-Fusi, S Bioorg Med Chem Lett 7: 949-954 (1997)
- Hemmerling, M; Nilsson, S; Edman, K; Eirefelt, S; Russell, W; Hendrickx, R; Johnsson, E; Kärrman Mårdh, C; Berger, M; Rehwinkel, H; Abrahamsson, A; Dahmén, J; Eriksson, AR; Gabos, B; Henriksson, K; Hossain, N; Ivanova, S; Jansson, AH; Jensen, TJ; Jerre, A; Johansson, H; Klingstedt, T; Lepistö, M; Lindsjö, M; Mile, I; Nikitidis, G; Steele, J; Tehler, U; Wissler, L; Hansson, T J Med Chem 60: 8591-8605 (2017)
- Hiremathad, A; Keri, RS; Esteves, AR; Cardoso, SM; Chaves, S; Santos, MA Eur J Med Chem 148: 255-267 (2018)
- Rose, Y; Ciblat, S; Reddy, R; Belley, AC; Dietrich, E; Lehoux, D; McKay, GA; Poirier, H; Far, AR; Delorme, D Bioorg Med Chem Lett 16: 891-6 (2006)
- Fathi, AR; Krautheim, A; Kaap, S; Eger, K; Steinfelder, HJ Bioorg Med Chem Lett 10: 1605-8 (2000)
- Galasiti Kankanamalage, AC; Kim, Y; Damalanka, VC; Rathnayake, AD; Fehr, AR; Mehzabeen, N; Battaile, KP; Lovell, S; Lushington, GH; Perlman, S; Chang, KO; Groutas, WC Eur J Med Chem 150: 334-346 (2018)
- Heidtmann, CV; Fejer, AR; Stærk, K; Pedersen, M; Asmussen, MG; Hertz, FB; Prabhala, BK; Frimodt-Møller, N; Klitgaard, JK; Andersen, TE; Nielsen, CU; Nielsen, P J Med Chem 67: 3692-3710
- Baud, MGJ; Bauer, MR; Verduci, L; Dingler, FA; Patel, KJ; Horil Roy, D; Joerger, AC; Fersht, AR Eur J Med Chem 152: 101-114 (2018)
- Kennedy, BJ; Lato, AM; Fisch, AR; Burke, SJ; Kirkland, JK; Prevatte, CW; Dunlap, LE; Smith, RT; Vogiatzis, KD; Collier, JJ; Campagna, SR ACS Med Chem Lett 12: 1568-1577 (2021)
- Flynn, AR; Mays, SG; Ortlund, EA; Jui, NT ACS Med Chem Lett 9: 1051-1056 (2018)
- Lowder, LL; Powell, M; Miller, SE; Kishton, RJ; Kelly, CB; Cribb, CB; Mastro-Kishton, K; Chelvanambi, M; Do, PT; Govindapur, RR; Wardell, SE; McDonnell, DP; Bartolotti, LJ; Akkaraju, GR; Frampton, AR; Varadarajan, S J Med Chem 64: 12651-12669 (2021)
- Hennessy, MR; Gutridge, AM; French, AR; Rhoda, ES; Meqbil, YJ; Gill, M; Kashyap, Y; Appourchaux, K; Paul, B; Wang, ZJ; van Rijn, RM; Riley, AP J Med Chem 66: 3312-3326 (2023)
- Venkatesh, R; Ramaiah, MJ; Gaikwad, HK; Janardhan, S; Bantu, R; Nagarapu, L; Sastry, GN; Ganesh, AR; Bhadra, M Eur J Med Chem 94: 87-101 (2015)
- Sperandio, D; Gangloff, AR; Litvak, J; Goldsmith, R; Hataye, JM; Wang, VR; Shelton, EJ; Elrod, K; Janc, JW; Clark, JM; Rice, K; Weinheimer, S; Yeung, KS; Meanwell, NA; Hernandez, D; Staab, AJ; Venables, BL; Spencer, JR Bioorg Med Chem Lett 12: 3129-33 (2002)
- Geanes, AR; Cho, HP; Nance, KD; McGowan, KM; Conn, PJ; Jones, CK; Meiler, J; Lindsley, CW Bioorg Med Chem Lett 26: 4487-4491 (2016)
- Genady, AR; Janzen, N; Banevicius, L; El-Gamal, M; El-Zaria, ME; Valliant, JF J Med Chem 59: 2660-73 (2016)
- Bentley, JM; Adams, DR; Bebbington, D; Benwell, KR; Bickerdike, MJ; Davidson, JE; Dawson, CE; Dourish, CT; Duncton, MA; Gaur, S; George, AR; Giles, PR; Hamlyn, RJ; Kennett, GA; Knight, AR; Malcolm, CS; Mansell, HL; Misra, A; Monck, NJ; Pratt, RM; Quirk, K; Roffey, JR; Vickers, SP; Cliffe, IA Bioorg Med Chem Lett 14: 2367-70 (2004)
- Germain, AR; Carmody, LC; Nag, PP; Morgan, B; Verplank, L; Fernandez, C; Donckele, E; Feng, Y; Perez, JR; Dandapani, S; Palmer, M; Lander, ES; Gupta, PB; Schreiber, SL; Munoz, B Bioorg Med Chem Lett 23: 1834-8 (2013)
- Paul, B; Rahaman, O; Roy, S; Pal, S; Satish, S; Mukherjee, A; Ghosh, AR; Raychaudhuri, D; Bhattacharya, R; Goon, S; Ganguly, D; Talukdar, A Eur J Med Chem 159: 187-205 (2018)
- Gomes, AR; Varela, CL; Tavares-da-Silva, EJ; Roleira, FMF Eur J Med Chem 201: (2020)
- Voight, EA; Gomtsyan, AR; Daanen, JF; Perner, RJ; Schmidt, RG; Bayburt, EK; DiDomenico, S; McDonald, HA; Puttfarcken, PS; Chen, J; Neelands, TR; Bianchi, BR; Han, P; Reilly, RM; Franklin, PH; Segreti, JA; Nelson, RA; Su, Z; King, AJ; Polakowski, JS; Baker, SJ; Gauvin, DM; Lewis, LR; Mikusa, JP; Joshi, SK; Faltynek, CR; Kym, PR; Kort, ME J Med Chem 57: 7412-24 (2014)
- Thomenius, MJ; Totman, J; Harvey, D; Mitchell, LH; Riera, TV; Cosmopoulos, K; Grassian, AR; Klaus, C; Foley, M; Admirand, EA; Jahic, H; Majer, C; Wigle, T; Jacques, SL; Gureasko, J; Brach, D; Lingaraj, T; West, K; Smith, S; Rioux, N; Waters, NJ; Tang, C; Raimondi, A; Munchhof, M; Mills, JE; Ribich, S; Porter Scott, M; Kuntz, KW; Janzen, WP; Moyer, M; Smith, JJ; Chesworth, R; Copeland, RA; Boriack-Sjodin, PA PLoS ONE 13:
- Katharine Holloway, M; McGaughey, GB; Coburn, CA; Stachel, SJ; Jones, KG; Stanton, EL; Gregro, AR; Lai, MT; Crouthamel, MC; Pietrak, BL; Munshi, SK Bioorg Med Chem Lett 17: 823-7 (2007)
- Namballa, HK; Dorogan, M; Gudipally, AR; Okafor, S; Gadhiya, S; Harding, WW J Med Chem 66: 10060-10079 (2023)
- Street, LJ; Baker, R; Davey, WB; Guiblin, AR; Jelley, RA; Reeve, AJ; Routledge, H; Sternfeld, F; Watt, AP; Beer, MS J Med Chem 38: 1799-810 (1995)
- Hajipour, AR; Fontanilla, D; Chu, UB; Arbabian, M; Ruoho, AE Bioorg Med Chem 18: 4397-404 (2010)
- Han, AR; Kim, JA; Lantvit, DD; Kardono, LB; Riswan, S; Chai, H; Carcache de Blanco, EJ; Farnsworth, NR; Swanson, SM; Kinghorn, AD J Nat Prod 72: 2028-31 (2009)
- Zhu, C; Hansen, AR; Bateman, T; Chen, Z; Holt, TG; Hubert, JA; Karanam, BV; Lee, SJ; Pan, J; Qian, S; Reddy, VB; Reitman, ML; Strack, AM; Tong, V; Weingarth, DT; Wolff, MS; MacNeil, DJ; Weber, AE; Duffy, JL; Edmondson, SD Bioorg Med Chem Lett 18: 4393-6 (2008)
- Warshawsky, AM; Alt, CA; Brozinick, JT; Harkness, AR; Hawkins, ED; Henry, JR; Matthews, DP; Miller, AR; Misener, EA; Montrose-Rafizadeh, C; Rhodes, GA; Shen, Q; Vance, JA; Udodong, UE; Wang, M; Zhang, TY; Zink, RW Bioorg Med Chem Lett 16: 6328-33 (2006)
- Goldberg, FW; Ting, AKT; Beattie, D; Lamont, GM; Fallan, C; Finlay, MRV; Williamson, B; Schimpl, M; Harmer, AR; Adeyemi, OB; Nordell, P; Cronin, AS; Vazquez-Chantada, M; Barratt, D; Ramos-Montoya, A; Cadogan, EB; Davies, BR ACS Med Chem Lett 13: 1295-1301 (2022)
- Harper, AR; Le, AT; Mather, T; Burgett, A; Berry, W; Summers, JA Bioorg Med Chem 26: 5766-5779 (2018)
- McAllister, LA; Butler, CR; Mente, S; O'Neil, SV; Fonseca, KR; Piro, JR; Cianfrogna, JA; Foley, TL; Gilbert, AM; Harris, AR; Helal, CJ; Johnson, DS; Montgomery, JI; Nason, DM; Noell, S; Pandit, J; Rogers, BN; Samad, TA; Shaffer, CL; da Silva, RG; Uccello, DP; Webb, D; Brodney, MA J Med Chem 61: 3008-3026 (2018)
- Prazeres, VF; Tizón, L; Otero, JM; Guardado-Calvo, P; Llamas-Saiz, AL; van Raaij, MJ; Castedo, L; Lamb, H; Hawkins, AR; González-Bello, C J Med Chem 53: 191-200 (2010)
- Annand, JR; Henderson, AR; Cole, KS; Maurais, AJ; Becerra, J; Liu, Y; Weerapana, E; Koehler, AN; Mapp, AK; Schindler, CS ACS Med Chem Lett 11: 1913-1918 (2020)
- Kokatla, HP; Sil, D; Malladi, SS; Balakrishna, R; Hermanson, AR; Fox, LM; Wang, X; Dixit, A; David, SA J Med Chem 56: 6871-85 (2013)
- Burnett, JC; Ruthel, G; Stegmann, CM; Panchal, RG; Nguyen, TL; Hermone, AR; Stafford, RG; Lane, DJ; Kenny, TA; McGrath, CF; Wipf, P; Stahl, AM; Schmidt, JJ; Gussio, R; Brunger, AT; Bavari, S J Biol Chem 282: 5004-14 (2007)
- Horswill, AR; Gordon, CP J Med Chem 63: 2705-2730 (2020)
- Dollinger, LM; Howell, AR Bioorg Med Chem Lett 8: 977-8 (1998)
- Ardecky, RJ; Hudson, AR; Phillips, DP; Tyhonas, JS; Deckhut, C; Lau, TL; Li, Y; Martinborough, EA; Roach, SL; Higuchi, RI; Lopez, FJ; Marschke, KB; Miner, JN; Karanewsky, DS; Negro-Vilar, A; Zhi, L Bioorg Med Chem Lett 17: 4158-62 (2007)
- Aicher, TD; Van Huis, CA; Hurd, AR; Skalitzky, DJ; Taylor, CB; Beleh, OM; Glick, G; Toogood, PL; Yang, B; Zheng, T; Huo, C; Gao, J; Qiao, C; Tian, X; Zhang, J; Demock, K; Hao, LY; Lesch, CA; Morgan, RW; Moisan, J; Wang, Y; Scatina, J; Paulos, CM; Zou, W; Carter, LL; Hu, X J Med Chem 64: 13410-13428 (2021)
- Jacobson, AR; Tam, SW; Sayre, LM J Med Chem 34: 2816-21 (1991)
- Karche, NP; Bhonde, M; Sinha, N; Jana, G; Kukreja, G; Kurhade, SP; Jagdale, AR; Tilekar, AR; Hajare, AK; Jadhav, GR; Gupta, NR; Limaye, R; Khedkar, N; Thube, BR; Shaikh, JS; Rao Irlapati, N; Phukan, S; Gole, G; Bommakanti, A; Khanwalkar, H; Pawar, Y; Kale, R; Kumar, R; Gupta, R; Praveen Kumar, VR; Wahid, S; Francis, A; Bhat, T; Kamble, N; Patil, V; Nigade, PB; Modi, D; Pawar, S; Naidu, S; Volam, H; Pagdala, V; Mallurwar, S; Goyal, H; Bora, P; Ahirrao, P; Singh, M; Kamalakannan, P; Naik, KR; Kumar, P; Powar, RG; Shankar, RB; Bernstein, PR; Gundu, J; Nemmani, K; Narasimham, L; George, KS; Sharma, S; Bakhle, D; Kamboj, RK; Palle, VP Bioorg Med Chem 28: (2020)
- Black, SL; Jales, AR; Brandt, W; Lewis, JW; Husbands, SM J Med Chem 46: 314-7 (2003)
- Ahmad, VU; Hussain, H; Jassbi, AR; Hussain, J; Bukhari, IA; Yasin, A; Aziz, N; Choudhary, MI J Nat Prod 66: 1221-4 (2003)
- Jesus, AR; Vila-Viçosa, D; Machuqueiro, M; Marques, AP; Dore, TM; Rauter, AP J Med Chem 60: 568-579 (2017)
- Thao, NP; Luyen, BT; Kim, JH; Jo, AR; Dat, NT; Kiem, PV; Minh, CV; Kim, YH Bioorg Med Chem 24: 3125-32 (2016)
- Joaquim, AR; Gionbelli, MP; Gosmann, G; Fuentefria, AM; Lopes, MS; Fernandes de Andrade, S J Med Chem 64: 16349-16379 (2021)
- Fauber, BP; Gobbi, A; Savy, P; Burton, B; Deng, Y; Everett, C; La, H; Johnson, AR; Lockey, P; Norman, M; Wong, H Bioorg Med Chem Lett 25: 4109-13 (2015)
- Slavov, SH; Radzvilovits, M; LeFrancois, S; Stoyanova-Slavova, IB; Soti, F; Kem, WR; Katritzky, AR Eur J Med Chem 45: 2433-46 (2010)
- Shtyrlin, NV; Kayumov, AR; Agafonova, MN; Garipov, MR; Gatina, AE; Pugachev, MV; Bulatova, ES; Grishaev, DY; Iksanova, AG; Khaziev, RM; Ganiev, IM; Aimaletdinov, AM; Gnezdilov, OI; Shtyrlin, YG Eur J Med Chem 261:
- Grychowska, K; Olejarz-Maciej, A; Blicharz, K; Pietruś, W; Karcz, T; Kurczab, R; Koczurkiewicz, P; Doroz-Płonka, A; Latacz, G; Keeri, AR; Piska, K; Satała, G; Pęgiel, J; Trybała, W; Jastrzębska-Więsek, M; Bojarski, AJ; Lamaty, F; Partyka, A; Walczak, M; Krawczyk, M; Malikowska-Racia, N; Popik, P; Zajdel, P Eur J Med Chem 236: (2022)
- Keimowitz, AR; Martin, BR; Razdan, RK; Crocker, PJ; Mascarella, SW; Thomas, BF J Med Chem 43: 59-70 (2000)
- Bussenius, J; Blazey, CM; Aay, N; Anand, NK; Arcalas, A; Baik, T; Bowles, OJ; Buhr, CA; Costanzo, S; Curtis, JK; DeFina, SC; Dubenko, L; Heuer, TS; Huang, P; Jaeger, C; Joshi, A; Kennedy, AR; Kim, AI; Lara, K; Lee, J; Li, J; Lougheed, JC; Ma, S; Malek, S; Manalo, JC; Martini, JF; McGrath, G; Nicoll, M; Nuss, JM; Pack, M; Peto, CJ; Tsang, TH; Wang, L; Womble, SW; Yakes, M; Zhang, W; Rice, KD Bioorg Med Chem Lett 22: 5396-404 (2012)
- Reuberson, J; Horsley, H; Franklin, RJ; Ford, D; Neuss, J; Brookings, D; Huang, Q; Vanderhoydonck, B; Gao, LJ; Jang, MY; Herdewijn, P; Ghawalkar, A; Fallah-Arani, F; Khan, AR; Henshall, J; Jairaj, M; Malcolm, S; Ward, E; Shuttleworth, L; Lin, Y; Li, S; Louat, T; Waer, M; Herman, J; Payne, A; Ceska, T; Doyle, C; Pitt, W; Calmiano, M; Augustin, M; Steinbacher, S; Lammens, A; Allen, R J Med Chem 61: 6705-6723 (2018)
- Hyvönen, MT; Keinänen, TA; Khomutov, M; Simonian, A; Weisell, J; Kochetkov, SN; Vepsäläinen, J; Alhonen, L; Khomutov, AR J Med Chem 54: 4611-8 (2011)
- King, AR; Dotsey, EY; Lodola, A; Jung, KM; Ghomian, A; Qiu, Y; Fu, J; Mor, M; Piomelli, D Chem Biol 16: 1045-52 (2009)
- Nie, S; Yao, Y; Wu, F; Wu, X; Zhao, J; Hua, Y; Wu, J; Huo, T; Lin, YL; Kneubehl, AR; Vogt, MB; Ferreon, J; Rico-Hesse, R; Song, Y J Med Chem 64: 2777-2800 (2021)
- Foloppe, N; Allen, NH; Bentley, CH; Brooks, TD; Kennett, G; Knight, AR; Leonardi, S; Misra, A; Monck, NJ; Sellwood, DM Bioorg Med Chem Lett 18: 1199-206 (2008)
- Schepetkin, IA; Khlebnikov, AI; Potapov, AS; Kovrizhina, AR; Matveevskaya, VV; Belyanin, ML; Atochin, DN; Zanoza, SO; Gaidarzhy, NM; Lyakhov, SA; Kirpotina, LN; Quinn, MT Eur J Med Chem 161: 179-191 (2019)
- Welch, WM; Kraska, AR; Sarges, R; Koe, BK J Med Chem 27: 1508-15 (1984)
- Kulkarni, PM; Kulkarni, AR; Korde, A; Tichkule, RB; Laprairie, RB; Denovan-Wright, EM; Zhou, H; Janero, DR; Zvonok, N; Makriyannis, A; Cascio, MG; Pertwee, RG; Thakur, GA J Med Chem 59: 44-60 (2016)
- Wang, L; Doherty, GA; Judd, AS; Tao, ZF; Hansen, TM; Frey, RR; Song, X; Bruncko, M; Kunzer, AR; Wang, X; Wendt, MD; Flygare, JA; Catron, ND; Judge, RA; Park, CH; Shekhar, S; Phillips, DC; Nimmer, P; Smith, ML; Tahir, SK; Xiao, Y; Xue, J; Zhang, H; Le, PN; Mitten, MJ; Boghaert, ER; Gao, W; Kovar, P; Choo, EF; Diaz, D; Fairbrother, WJ; Elmore, SW; Sampath, D; Leverson, JD; Souers, AJ ACS Med Chem Lett 11: 1829-1836 (2020)
- Punthasee, P; Laciak, AR; Cummings, AH; Ruddraraju, KV; Lewis, SM; Hillebrand, R; Singh, H; Tanner, JJ; Gates, KS Biochemistry 56: 2051-2060 (2017)
- Wall, ID; Leach, AR; Salt, DW; Ford, MG; Essex, JW J Med Chem 42: 5142-52 (2000)
- Heinrich, T; Peterson, C; Schneider, R; Garg, S; Schwarz, D; Gunera, J; Seshire, A; Kötzner, L; Schlesiger, S; Musil, D; Schilke, H; Doerfel, B; Diehl, P; Böpple, P; Lemos, AR; Sousa, PMF; Freire, F; Bandeiras, TM; Carswell, E; Pearson, N; Sirohi, S; Hooker, M; Trivier, E; Broome, R; Balsiger, A; Crowden, A; Dillon, C; Wienke, D J Med Chem 65: 9206-9229 (2022)
- Johnson, MG; Liu, JJ; Li, AR; van Lengerich, B; Wang, S; Medina, JC; Collins, TL; Danao, J; Seitz, L; Willee, A; D'Souza, W; Budelsky, AL; Fan, PW; Wong, SG Bioorg Med Chem Lett 24: 2877-80 (2014)
- Lin, Z; Zachariah, MM; Marett, L; Hughen, RW; Teichert, RW; Concepcion, GP; Haygood, MG; Olivera, BM; Light, AR; Schmidt, EW J Nat Prod 77: 1224-30 (2014)
- Kim, RM; Chang, J; Lins, AR; Brady, E; Candelore, MR; Dallas-Yang, Q; Ding, V; Dragovic, J; Iliff, S; Jiang, G; Mock, S; Qureshi, S; Saperstein, R; Szalkowski, D; Tamvakopoulos, C; Tota, L; Wright, M; Yang, X; Tata, JR; Chapman, K; Zhang, BB; Parmee, ER Bioorg Med Chem Lett 18: 3701-5 (2008)
- Wise, JG; Nanayakkara, AK; Aljowni, M; Chen, G; De Oliveira, MC; Ammerman, L; Olengue, K; Lippert, AR; Vogel, PD J Med Chem 62: 10645-10663 (2019)
- Faria, RX; Oliveira, FH; Salles, JP; Oliveira, AS; von Ranke, NL; Bello, ML; Rodrigues, CR; Castro, HC; Louvis, AR; Martins, DL; Ferreira, VF Eur J Med Chem 143: 1361-1372 (2018)
- NIROGI, R; SHINDE, AK; MOHAMMED, AR; GOYAL, VK; PANDEY, SK; BENADE, VS; GOURA, V; JASTI, V US Patent US20250019386 (2025)
- Al-Suwaidan, IA; Alanazi, AM; El-Azab, AS; Al-Obaid, AM; ElTahir, KE; Maarouf, AR; Abu El-Enin, MA; Abdel-Aziz, AA Bioorg Med Chem Lett 23: 2601-5 (2013)
- Middleton, DS; MacKenzie, AR; Newman, SD; Corless, M; Warren, A; Marchington, AP; Jones, B Bioorg Med Chem Lett 15: 3957-61 (2005)
- Paquin, I; Raeppel, S; Leit, S; Gaudette, F; Zhou, N; Moradei, O; Saavedra, O; Bernstein, N; Raeppel, F; Bouchain, G; Fréchette, S; Woo, SH; Vaisburg, A; Fournel, M; Kalita, A; Robert, MF; Lu, A; Trachy-Bourget, MC; Yan, PT; Liu, J; Rahil, J; MacLeod, AR; Besterman, JM; Li, Z; Delorme, D Bioorg Med Chem Lett 18: 1067-71 (2008)
- Gaudette, F; Raeppel, S; Nguyen, H; Beaulieu, N; Beaulieu, C; Dupont, I; Macleod, AR; Besterman, JM; Vaisburg, A Bioorg Med Chem Lett 20: 848-52 (2010)
- Maddirala, AR; Klein, R; Pinkner, JS; Kalas, V; Hultgren, SJ; Janetka, JW J Med Chem 62: 467-479 (2019)
- Mahajan, D; Sen, S; Kuila, B; Sharma, A; Arora, R; Sagar, M; Mahapatra, AR; Gawade, LB; Dugar, S J Med Chem 63: 11121-11130 (2020)
- Villadsen, JS; Stephansen, HM; Maolanon, AR; Harris, P; Olsen, CA J Med Chem 56: 6512-20 (2013)
- Nikam, SS; Martin, AR; Nelson, DL J Med Chem 31: 1965-8 (1988)
- Günther, S; Reinke, PY; Fernández-García, Y; Lieske, J; Lane, TJ; Ginn, HM; Koua, FH; Ehrt, C; Ewert, W; Oberthuer, D; Yefanov, O; Meier, S; Lorenzen, K; Krichel, B; Kopicki, J; Gelisio, L; Brehm, W; Dunkel, I; Seychell, B; Gieseler, H; Norton-Baker, B; Escudero-Pérez, B; Domaracky, M; Saouane, S; Tolstikova, A; White, TA; Hänle, A; Groessler, M; Fleckenstein, H; Trost, F; Galchenkova, M; Gevorkov, Y; Li, C; Awel, S; Peck, A; Barthelmess, M; Schlünzen, F; Xavier, PL; Werner, N; Andaleeb, H; Ullah, N; Falke, S; Srinivasan, V; Franca, BA; Schwinzer, M; Brognaro, H; Rogers, C; Melo, D; Zaitsev-Doyle, JJ; Knoska, J; Peña Murillo, GE; Mashhour, AR; Guicking, F; Hennicke, V; Fischer, P; Hakanpää, J; Meyer, J; Gribbon, P; Ellinger, B; Kuzikov, M; Wolf, M; Beccari, AR; Bourenkov, G; Stetten, D; Pompidor, G; Bento, I; Panneerselvam, S; Karpics, I; Schneider, TR; Garcia Alai, MM; Niebling, S; Günther, C; Schmidt, C; Schubert, R; Han, H; Boger, J; Monteiro, DC; Zhang, L; Sun, X; Pletzer-Zelgert, J; Wollenhaupt, J; Feiler, CG; Weiss, MS; Schulz, E; Mehrabi, P; Karničar, K; Usenik, A; Loboda, J; Tidow, H; Chari, A; Hilgenfeld, R; Uetrecht, C; Cox, R; Zaliani, A; Beck, T; Rarey, M; Günther, S; Turk, D; Hinrichs, W; Chapman, HN; Pearson, AR; Betzel, C; Meents, A bioRxiv 2020: (2020)
- McCarthy, AR; Pirrie, L; Hollick, JJ; Ronseaux, S; Campbell, J; Higgins, M; Staples, OD; Tran, F; Slawin, AM; Lain, S; Westwood, NJ Bioorg Med Chem 20: 1779-93 (2012)
- Poon, SF; Stock, N; Payne, JE; McGuire, AR; Stearns, B; Yang, X; Chen, W; Munoz, B; Smith, ND Bioorg Med Chem Lett 15: 2259-63 (2005)
- Karkare, S; Chung, TT; Collin, F; Mitchenall, LA; McKay, AR; Greive, SJ; Meyer, JJ; Lall, N; Maxwell, A J Biol Chem 288: 5149-56 (2013)
- Green, OM; McKenzie, AR; Shapiro, AB; Otterbein, L; Ni, H; Patten, A; Stokes, S; Albert, R; Kawatkar, S; Breed, J Bioorg Med Chem Lett 22: 1510-9 (2012)
- Egleton, JE; Thinnes, CC; Seden, PT; Laurieri, N; Lee, SP; Hadavizadeh, KS; Measures, AR; Jones, AM; Thompson, S; Varney, A; Wynne, GM; Ryan, A; Sim, E; Russell, AJ Bioorg Med Chem 22: 3030-54 (2014)
- de Souza, MM; Andreolla, MC; Ribeiro, TC; Gonçalves, AE; Medeiros, AR; de Souza, AS; Ferreira, LLG; Andricopulo, AD; Yunes, RA; de Oliveira, AS RSC Med Chem 11: 307-316 (2020)
- Brant, MG; Goodwin-Tindall, J; Stover, KR; Stafford, PM; Wu, F; Meek, AR; Schiavini, P; Wohnig, S; Weaver, DF ACS Med Chem Lett 9: 131-136 (2018)
- Mezo, AR; McDonnell, KA; Castro, A; Fraley, C Bioorg Med Chem 16: 6394-405 (2008)
- Hamdouchi, C; Maiti, P; Warshawsky, AM; DeBaillie, AC; Otto, KA; Wilbur, KL; Kahl, SD; Patel Lewis, A; Cardona, GR; Zink, RW; Chen, K; Cr, S; Lineswala, JP; Neathery, GL; Bouaichi, C; Diseroad, BA; Campbell, AN; Sweetana, SA; Adams, LA; Cabrera, O; Ma, X; Yumibe, NP; Montrose-Rafizadeh, C; Chen, Y; Miller, AR J Med Chem 61: 934-945 (2018)
- Mohamed, AR; Mostafa, A; El Hassab, MA; Hedeab, GM; Mahmoud, SH; George, RF; Georgey, HH; Abdel Gawad, NM; El-Ashrey, MK RSC Med Chem 14: 899-920 (2023)
- Nirogi, R; Mohammed, AR; Shinde, AK; Ravella, SR; Bogaraju, N; Subramanian, R; Mekala, VR; Palacharla, RC; Muddana, N; Thentu, JB; Bhyrapuneni, G; Abraham, R; Jasti, V J Med Chem 63: 2833-2853 (2020)
- Aghazadeh Tabrizi, M; Baraldi, PG; Saponaro, G; Moorman, AR; Romagnoli, R; Preti, D; Baraldi, S; Ruggiero, E; Tintori, C; Tuccinardi, T; Vincenzi, F; Borea, PA; Varani, K J Med Chem 56: 4482-96 (2013)
- Collibee, SE; Romero, A; Muci, AR; Hwee, DT; Chuang, C; Hartman, JJ; Motani, AS; Ashcraft, L; DeRosier, A; Grillo, M; Lu, Q; Malik, FI; Morgan, BP J Med Chem 67: 7859-7869
- D'yakonov, VA; Dzhemileva, LU; Makarov, AA; Mulukova, AR; Baev, DS; Khusnutdinova, EK; Tolstikova, TG; Dzhemilev, UM Bioorg Med Chem Lett 25: 2405-8 (2015)
- Palani, A; Nawrocki, AR; Orvieto, F; Bianchi, E; Mandić, E; Pessi, A; Huang, C; Deng, Q; Toussaint, N; Walsh, E; Reddy, V; Ashley, E; He, H; Mumick, S; Hawes, B; Marsh, D; Erion, M; Nargund, R; Carrington, PE ACS Med Chem Lett 13: 1248-1254 (2022)
- Nesaragi, AR; Kamble, RR; Dixit, S; Kodasi, B; Hoolageri, SR; Bayannavar, PK; Dasappa, JP; Vootla, S; Joshi, SD; Kumbar, VM Bioorg Med Chem Lett 43: (2021)
- Davie, RL; Edwards, HJ; Evans, DM; Hodgson, ST; Miller, I; Novak, AR; Smith, AJ; Stocks, MJ US Patent US9533987 (2017)
- Tsai, WC; Gilbert, NC; Ohler, A; Armstrong, M; Perry, S; Kalyanaraman, C; Yasgar, A; Rai, G; Simeonov, A; Jadhav, A; Standley, M; Lee, HW; Crews, P; Iavarone, AT; Jacobson, MP; Neau, DB; Offenbacher, AR; Newcomer, M; Holman, TR Bioorg Med Chem 46: (2021)
- Shim, S; Krishnaiah, M; Sankham, MR; Kim, I; Lee, Y; Shin, I; Oh, AR; Lee, HJ; Vu, TNL; Park, J; Choi, S; Park, S; Kwon, Y; Fang, S; Kim, DK J Med Chem 65: 9974-10000 (2022)
- Cheung, AW; Banner, B; Bose, J; Kim, K; Li, S; Marcopulos, N; Orzechowski, L; Sergi, JA; Thakkar, KC; Wang, BB; Yun, W; Zwingelstein, C; Berthel, S; Olivier, AR Bioorg Med Chem Lett 22: 7518-22 (2012)
- Checa, A; Ortiz, AR; de Pascual-Teresa, B; Gago, F J Med Chem 40: 4136-45 (1998)
- Bazan, HA; Bhattacharjee, S; Burgos, C; Recio, J; Abet, V; Pahng, AR; Jun, B; Heap, J; Ledet, AJ; Gordon, WC; Edwards, S; Paul, D; Alvarez-Builla, J; Bazan, NG Eur J Med Chem 202: (2020)
- Pickett, JE; Nagakura, K; Pasternak, AR; Grinnell, SG; Majumdar, S; Lewis, JS; Pasternak, GW Bioorg Med Chem Lett 23: 4347-50 (2013)
- Jeong, LS; Lee, HW; Kim, HO; Tosh, DK; Pal, S; Choi, WJ; Gao, ZG; Patel, AR; Williams, W; Jacobson, KA; Kim, HD Bioorg Med Chem Lett 18: 1612-6 (2008)
- Günther, S; Reinke, PY; Fernández-García, Y; Lieske, J; Lane, TJ; Ginn, HM; Koua, FH; Ehrt, C; Ewert, W; Oberthuer, D; Yefanov, O; Meier, S; Lorenzen, K; Krichel, B; Kopicki, J; Gelisio, L; Brehm, W; Dunkel, I; Seychell, B; Gieseler, H; Norton-Baker, B; Escudero-Pérez, B; Domaracky, M; Saouane, S; Tolstikova, A; White, TA; Hänle, A; Groessler, M; Fleckenstein, H; Trost, F; Galchenkova, M; Gevorkov, Y; Li, C; Awel, S; Peck, A; Barthelmess, M; Schlünzen, F; Xavier, PL; Werner, N; Andaleeb, H; Ullah, N; Falke, S; Srinivasan, V; Franca, BA; Schwinzer, M; Brognaro, H; Rogers, C; Melo, D; Zaitsev-Doyle, JJ; Knoska, J; Peña Murillo, GE; Mashhour, AR; Guicking, F; Hennicke, V; Fischer, P; Hakanpää, J; Meyer, J; Gribbon, P; Ellinger, B; Kuzikov, M; Wolf, M; Beccari, AR; Bourenkov, G; Stetten, D; Pompidor, G; Bento, I; Panneerselvam, S; Karpics, I; Schneider, TR; Garcia Alai, MM; Niebling, S; Günther, C; Schmidt, C; Schubert, R; Han, H; Boger, J; Monteiro, DC; Zhang, L; Sun, X; Pletzer-Zelgert, J; Wollenhaupt, J; Feiler, CG; Weiss, MS; Schulz, E; Mehrabi, P; Karničar, K; Usenik, A; Loboda, J; Tidow, H; Chari, A; Hilgenfeld, R; Uetrecht, C; Cox, R; Zaliani, A; Beck, T; Rarey, M; Günther, S; Turk, D; Hinrichs, W; Chapman, HN; Pearson, AR; Betzel, C; Meents, A bioRxiv 2020: (2020)
- Gutiérrez, M; Pereira, AR; Debonsi, HM; Ligresti, A; Di Marzo, V; Gerwick, WH J Nat Prod 74: 2313-7 (2011)
- Armani, E; Rizzi, A; Capaldi, C; De Fanti, R; Delcanale, M; Villetti, G; Marchini, G; Pisano, AR; Pitozzi, V; Pittelli, MG; Trevisani, M; Salvadori, M; Cenacchi, V; Puccini, P; Amadei, F; Pappani, A; Civelli, M; Patacchini, R; Baker-Glenn, CAG; Van de Poël, H; Blackaby, WP; Nash, K; Amari, G J Med Chem 64: 9100-9119 (2021)
- Avalon, NE; Nafie, J; De Marco Verissimo, C; Warrensford, LC; Dietrick, SG; Pittman, AR; Young, RM; Kearns, FL; Smalley, T; Binning, JM; Dalton, JP; Johnson, MP; Woodcock, HL; Allcock, AL; Baker, BJ J Nat Prod 85: 1315-1323 (2022)
- Rejman, D; Rabatinová, A; Pombinho, AR; Kovačková, S; Pohl, R; Zborníková, E; Kolář, M; Bogdanová, K; Nyč, O; Sanderová, H; Látal, T; Bartůněk, P; Krásný, L J Med Chem 54: 7884-98 (2011)
- Porcari, AR; Devivar, RV; Kucera, LS; Drach, JC; Townsend, LB J Med Chem 41: 1252-62 (1998)
- Bago, R; Malik, N; Munson, MJ; Prescott, AR; Davies, P; Sommer, E; Shpiro, N; Ward, R; Cross, D; Ganley, IG; Alessi, DR Biochem J 463: 413-27
- Liu, Y; Zhang, W; Li, L; Salvador, LA; Chen, T; Chen, W; Felsenstein, KM; Ladd, TB; Price, AR; Golde, TE; He, J; Xu, Y; Li, Y; Luesch, H J Med Chem 55: 10749-65 (2012)
- Zhao, H; Prosser, AR; Liotta, DC; Wilson, LJ Bioorg Med Chem Lett 25: 4950-5 (2015)
- Cardillo, G; Gentilucci, L; Tolomelli, A; Spinosa, R; Calienni, M; Qasem, AR; Spampinato, S J Med Chem 47: 5198-203 (2004)
- Lintnerová, L; García-Caballero, M; Gregán, F; Melichercík, M; Quesada, AR; Dobiaš, J; Lác, J; Sališová, M; Bohác, A Eur J Med Chem 72: 146-59 (2014)
- Sirisha, B; Narsaiah, B; Yakaiah, T; Gayatri, G; Sastry, GN; Prasad, MR; Rao, AR Eur J Med Chem 45: 1739-45 (2010)
- Rosati, RL; Da Silva Jardine, P; Cameron, KO; Thompson, DD; Ke, HZ; Toler, SM; Brown, TA; Pan, LC; Ebbinghaus, CF; Reinhold, AR; Elliott, NC; Newhouse, BN; Tjoa, CM; Sweetnam, PM; Cole, MJ; Arriola, MW; Gauthier, JW; Crawford, DT; Nickerson, DF; Pirie, CM; Qi, H; Simmons, HA; Tkalcevic, GT J Med Chem 41: 2928-31 (1998)
- Corte, JR; Fang, T; Pinto, DJ; Orwat, MJ; Rendina, AR; Luettgen, JM; Rossi, KA; Wei, A; Ramamurthy, V; Myers, JE; Sheriff, S; Narayanan, R; Harper, TW; Zheng, JJ; Li, YX; Seiffert, DA; Wexler, RR; Quan, ML Bioorg Med Chem 24: 2257-72 (2016)
- Ferreira, RS; Bryant, C; Ang, KK; McKerrow, JH; Shoichet, BK; Renslo, AR J Med Chem 52: 5005-8 (2010)
- Salimbeni, A; Canevotti, R; Paleari, F; Bonaccorsi, F; Renzetti, AR; Belvisi, L; Bravi, G; Scolastico, C J Med Chem 37: 3928-38 (1994)
- Cameron, KO; Kung, DW; Kalgutkar, AS; Kurumbail, RG; Miller, R; Salatto, CT; Ward, J; Withka, JM; Bhattacharya, SK; Boehm, M; Borzilleri, KA; Brown, JA; Calabrese, M; Caspers, NL; Cokorinos, E; Conn, EL; Dowling, MS; Edmonds, DJ; Eng, H; Fernando, DP; Frisbie, R; Hepworth, D; Landro, J; Mao, Y; Rajamohan, F; Reyes, AR; Rose, CR; Ryder, T; Shavnya, A; Smith, AC; Tu, M; Wolford, AC; Xiao, J J Med Chem 59: 8068-81 (2016)
- Matić, J; Akladios, F; Battisti, UM; Håversen, L; Nain-Perez, A; Füchtbauer, AF; Kim, W; Monjas, L; Rivero, AR; Borén, J; Mardinoglu, A; Uhlen, M; Grøtli, M Eur J Med Chem 269:
- Hayes, KE; Batsomboon, P; Chen, WC; Johnson, BD; Becker, A; Eschrich, S; Yang, Y; Robart, AR; Dudley, GB; Geldenhuys, WJ; Hazlehurst, LA Bioorg Med Chem 27: 1479-1488 (2019)
- Murray, CM; Hutchinson, R; Bantick, JR; Belfield, GP; Benjamin, AD; Brazma, D; Bundick, RV; Cook, ID; Craggs, RI; Edwards, S; Evans, LR; Harrison, R; Holness, E; Jackson, AP; Jackson, CG; Kingston, LP; Perry, MW; Ross, AR; Rugman, PA; Sidhu, SS; Sullivan, M; Taylor-Fishwick, DA; Walker, PC; Whitehead, YM; Wilkinson, DJ; Wright, A; Donald, DK Nat Chem Biol 1: 371-6 (2005)
- Eccles, W; Hack, MD; Jones, WM; Krawczuk, PJ; Lebsack, AD; Pippel, DJ; Rovira, AR; Wolin, RL US Patent US20240199605 (2024)
- Ruwe, AR; Koikov, L; Abdel-Malek, Z; Haskell-Luevano, C; Dirain, ML; Portillo, F; Xiang, Z; Wortman, M; Knittel, JJ Bioorg Med Chem Lett 19: 5176-81 (2009)
- Sabnis, RW; Sabnis, AR ACS Med Chem Lett 14: 1165-1166 (2023)
- Shahripour, A; Para, KS; Plummer, MS; Lunney, EA; Holland, DR; Rubin, JR; Humblet, C; Fergus, JH; Marks, JS; Saltiel, AR; Sawyer, TK Bioorg Med Chem Lett 7: 1107-1112 (1997)
- Cosentino, L; Redondo-Horcajo, M; Zhao, Y; Santos, AR; Chowdury, KF; Vinader, V; Abdallah, QM; Abdel-Rahman, H; Fournier-Dit-Chabert, J; Shnyder, SD; Loadman, PM; Fang, WS; Díaz, JF; Barasoain, I; Burns, PA; Pors, K J Med Chem 55: 11062-6 (2012)
- Hatcher, JM; Zwirek, M; Sarhan, AR; Vatsan, PS; Tonelli, F; Alessi, DR; Davies, P; Gray, NS Bioorg Med Chem Lett 94: (2023)
- Yu, Z; Sawkar, AR; Whalen, LJ; Wong, CH; Kelly, JW J Med Chem 50: 94-100 (2007)
- Griffith, DA; Edmonds, DJ; Fortin, JP; Kalgutkar, AS; Kuzmiski, JB; Loria, PM; Saxena, AR; Bagley, SW; Buckeridge, C; Curto, JM; Derksen, DR; Dias, JM; Griffor, MC; Han, S; Jackson, VM; Landis, MS; Lettiere, D; Limberakis, C; Liu, Y; Mathiowetz, AM; Patel, JC; Piotrowski, DW; Price, DA; Ruggeri, RB; Tess, DA J Med Chem 65: 8208-8226 (2022)
- Schneekloth, AR; Pucheault, M; Tae, HS; Crews, CM Bioorg Med Chem Lett 18: 5904-8 (2008)
- Brand, M; Clayton, J; Moroglu, M; Schiedel, M; Picaud, S; Bluck, JP; Skwarska, A; Bolland, H; Chan, AKN; Laurin, CMC; Scorah, AR; See, L; Rooney, TPC; Andrews, KH; Fedorov, O; Perell, G; Kalra, P; Vinh, KB; Cortopassi, WA; Heitel, P; Christensen, KE; Cooper, RI; Paton, RS; Pomerantz, WCK; Biggin, PC; Hammond, EM; Filippakopoulos, P; Conway, SJ J Med Chem 64: 10102-10123 (2021)
- Shalabi, AR; Yu, Z; Zhou, X; Jounaidi, Y; Chen, H; Dai, J; Kent, DE; Feng, HJ; Forman, SA; Cohen, JB; Bruzik, KS; Miller, KW Eur J Med Chem 194: (2020)
- Liu, J; Shikhman, AR; Lotz, MK; Wong, CH Chem Biol 8: 701-11 (2001)
- Woods, KW; Lai, C; Miyashiro, JM; Tong, Y; Florjancic, AS; Han, EK; Soni, N; Shi, Y; Lasko, L; Leverson, JD; Johnson, EF; Shoemaker, AR; Penning, TD Bioorg Med Chem Lett 22: 1940-3 (2012)
- Palin, R; Clark, JK; Evans, L; Feilden, H; Fletcher, D; Hamilton, NM; Houghton, AK; Jones, PS; McArthur, D; Montgomery, B; Ratcliffe, PD; Smith, AR; Sutherland, A; Weston, MA; Wishart, G Bioorg Med Chem Lett 19: 6441-6 (2009)
- Martin, KR; Celano, SL; Solitro, AR; Gunaydin, H; Scott, M; O'Hagan, RC; Shumway, SD; Fuller, P; MacKeigan, JP iScience 8: 74-84
- Cox, B; Hutson, JL; Keeling, SE; Kirk, BE; Srikantha, AR; Watson, NS Bioorg Med Chem Lett 4: 1931-1936 (1994)
- Hassett, MR; Sternberg, AR; Roepe, PD Biochemistry 56: 4326-4334
- Stoit, AR; den Hartog, AP; Mons, H; van Schaik, S; Barkhuijsen, N; Stroomer, C; Coolen, HK; Reinders, JH; Adolfs, TJ; van der Neut, M; Keizer, H; Kruse, CG Bioorg Med Chem Lett 18: 188-93 (2008)
- Mishra, SJ; Ghosh, S; Stothert, AR; Dickey, CA; Blagg, BS ACS Chem Biol 12: 244-253 (2017)
- Volynets, GP; Bdzhola, VG; Golub, AG; Synyugin, AR; Chekanov, MA; Kukharenko, OP; Yarmoluk, SM Eur J Med Chem 61: 104-15 (2013)
- Panyain, N; Godinat, A; Thawani, AR; Lachiondo-Ortega, S; Mason, K; Elkhalifa, S; Smith, LM; Harrigan, JA; Tate, EW RSC Med Chem 12: 1935-1943 (2021)
- Sinha, N; Karche, NP; Verma, MK; Walunj, SS; Nigade, PB; Jana, G; Kurhade, SP; Hajare, AK; Tilekar, AR; Jadhav, GR; Thube, BR; Shaikh, JS; Balgude, S; Singh, LB; Mahimane, V; Adurkar, SK; Hatnapure, G; Raje, F; Bhosale, Y; Bhanage, D; Sachchidanand, S; Dixit, R; Gupta, R; Bokare, AM; Dandekar, M; Bharne, A; Chatterjee, M; Desai, S; Koul, S; Modi, D; Mehta, M; Patil, V; Singh, M; Gundu, J; Goel, RN; Shah, C; Sharma, S; Bakhle, D; Kamboj, RK; Palle, VP J Med Chem 63: 944-960 (2020)
- Oliveira, IA; Gonçalves, AS; Neves, JL; von Itzstein, M; Todeschini, AR J Biol Chem 289: 423-36 (2014)
- Zhao, Y; Ren, J; Fry, EE; Xiao, J; Townsend, AR; Stuart, DI J Med Chem 61: 4938-4945 (2018)
- Caleffi, GS; Rosa, AS; de Souza, LG; Avelar, JLS; Nascimento, SMR; de Almeida, VM; Tucci, AR; Ferreira, VN; da Silva, AJM; Santos-Filho, OA; Miranda, MD; Costa, PRR J Nat Prod 86: 1536-1549 (2023)
- Press, NJ; Taylor, RJ; Fullerton, JD; Tranter, P; McCarthy, C; Keller, TH; Brown, L; Cheung, R; Christie, J; Haberthuer, S; Hatto, JD; Keenan, M; Mercer, MK; Press, NE; Sahri, H; Tuffnell, AR; Tweed, M; Fozard, JR Bioorg Med Chem Lett 15: 3081-5 (2005)
- Muddana, HS; Varnado, CD; Bielawski, CW; Urbach, AR; Isaacs, L; Geballe, MT; Gilson, MK J Comput Aided Mol Des 26: 475-87 (2012)
- Reshma, RS; Jeankumar, VU; Kapoor, N; Saxena, S; Bobesh, KA; Vachaspathy, AR; Kolattukudy, PE; Sriram, D Bioorg Med Chem 25: 2761-2771 (2017)
- Vaino, AR; Grattan, VT; Prensky, Z US Patent US10259786 (2019)
- Sliedregt, LA; Rensen, PC; Rump, ET; van Santbrink, PJ; Bijsterbosch, MK; Valentijn, AR; van der Marel, GA; van Boom, JH; van Berkel, TJ; Biessen, EA J Med Chem 42: 609-18 (1999)
- Brear, P; De Fusco, C; Atkinson, EL; Iegre, J; Francis-Newton, NJ; Venkitaraman, AR; Hyvönen, M; Spring, DR RSC Med Chem 13: 1420-1426 (2022)
- Poe, MM; Methuku, KR; Li, G; Verma, AR; Teske, KA; Stafford, DC; Arnold, LA; Cramer, JW; Jones, TM; Cerne, R; Krambis, MJ; Witkin, JM; Jambrina, E; Rehman, S; Ernst, M; Cook, JM; Schkeryantz, JM J Med Chem 59: 10800-10806 (2016)
- MCKERRALL, SJ; WONG, AR; CRAWFORD, JJ; LEE, W; LAI, KW; PELLETIER, G; ROY, S; WINTER, DK; OKUMURA, M; Dorel, R US Patent US20240174696 (2024)
- Smith, PW; Sollis, SL; Howes, PD; Cherry, PC; Cobley, KN; Taylor, H; Whittington, AR; Scicinski, J; Bethell, RC; Taylor, N; Skarzynski, T; Cleasby, A; Singh, O; Wonacott, A; Varghese, J; Colman, P Bioorg Med Chem Lett 6: 2931-2936 (1996)
- Dinnell, K; Chicchi, GG; Dhar, MJ; Elliott, JM; Hollingworth, GJ; Kurtz, MM; Ridgill, MP; Rycroft, W; Tsao, KL; Williams, AR; Swain, CJ Bioorg Med Chem Lett 11: 1237-40 (2001)
- Giblin, GM; O'Shaughnessy, CT; Naylor, A; Mitchell, WL; Eatherton, AJ; Slingsby, BP; Rawlings, DA; Goldsmith, P; Brown, AJ; Haslam, CP; Clayton, NM; Wilson, AW; Chessell, IP; Wittington, AR; Green, R J Med Chem 50: 2597-600 (2007)
- Dorel, R; Wong, AR; Crawford, JJ ACS Med Chem Lett 14: 233-243 (2023)
- Huang, KH; Veal, JM; Fadden, RP; Rice, JW; Eaves, J; Strachan, JP; Barabasz, AF; Foley, BE; Barta, TE; Ma, W; Silinski, MA; Hu, M; Partridge, JM; Scott, A; DuBois, LG; Freed, T; Steed, PM; Ommen, AJ; Smith, ED; Hughes, PF; Woodward, AR; Hanson, GJ; McCall, WS; Markworth, CJ; Hinkley, L; Jenks, M; Geng, L; Lewis, M; Otto, J; Pronk, B; Verleysen, K; Hall, SE J Med Chem 52: 4288-305 (2009)
- Salah El Dine, R; Abdel Monem, AR; El-Halawany, AM; Hattori, M; Abdel-Sattar, E J Nat Prod 74: 943-8 (2011)
- East, JE; Kennedy, AJ; Tomsig, JL; De Leon, AR; Lynch, KR; Macdonald, TL Bioorg Med Chem Lett 20: 7132-6 (2010)
- Lin, R; Connolly, PJ; Lu, Y; Chiu, G; Li, S; Yu, Y; Huang, S; Li, X; Emanuel, SL; Middleton, SA; Gruninger, RH; Adams, M; Fuentes-Pesquera, AR; Greenberger, LM Bioorg Med Chem Lett 17: 4297-302 (2007)
- Shuttleworth, SJ; Liam Cecil, AR; Hill, TJ; Silva, FA US Patent US9938290 (2018)
- Bague, D; Wang, R; Hodge, D; Mikati, MO; Roma, JS; Boshoff, HI; Dailey, AL; Girma, M; Couch, RD; Odom John, AR; Dowd, CS RSC Med Chem 15: 2422-2439
- Rodríguez, YA; Gutiérrez, M; Ramírez, D; Alzate-Morales, J; Bernal, CC; Güiza, FM; Romero Bohórquez, AR Chem Biol Drug Des 88: 498-510 (2016)
- Van Dyke, AR; Etemad, LS; Vessicchio, MJ; Naclerio, GA; Jedson, V Chembiochem 17: 1602-5 (2016)
- Mayorov, AV; Cai, M; Chandler, KB; Petrov, RR; Van Scoy, AR; Yu, Z; Tanaka, DK; Trivedi, D; Hruby, VJ J Med Chem 49: 1946-52 (2006)
- Leite, FHA; Santiago, PBGDS; Froes, TQ; da Silva Filho, J; da Silva, SG; Ximenes, RM; de Faria, AR; Brondani, DJ; de Albuquerque, JFC; Castilho, MS Eur J Med Chem 123: 639-648 (2016)
- Eccles, W; Blevitt, JM; Booker, JN; Chrovian, CC; Crawford, S; de Leon, AR; Deng, X; Fourie, AM; Grice, CA; Herman, K; Karlsson, L; Kearney, AM; Lee-Dutra, A; Liang, J; Luna, R; Pippel, D; Rao, N; Riley, JP; Santillán, A; Savall, B; Tanis, VM; Xue, X; Young, AL Bioorg Med Chem Lett 23: 811-5 (2013)
- Lorenzo, P; Alvarez, R; Ortiz, MA; Alvarez, S; Piedrafita, FJ; de Lera, AR J Med Chem 51: 5431-40 (2008)
- Swier, LJ; Monjas, L; Guskov, A; de Voogd, AR; Erkens, GB; Slotboom, DJ; Hirsch, AK Chembiochem 16: 819-26 (2015)
- González-Naranjo, P; Pérez-Macias, N; Campillo, NE; Pérez, C; Arán, VJ; Girón, R; Sánchez-Robles, E; Martín, MI; Gómez-Cañas, M; García-Arencibia, M; Fernández-Ruiz, J; Páez, JA Eur J Med Chem 73: 56-72 (2014)
- Kánai, K; Arányi, P; Böcskei, Z; Ferenczy, G; Harmat, V; Simon, K; Bátori, S; Náray-Szabo, G; Hermecz, I J Med Chem 51: 7514-22 (2009)
- García, M; Virgili, M; Alonso, M; Alegret, C; Farran, J; Fernández, B; Bordas, M; Pascual, R; Burgueño, J; Vidal-Torres, A; Fernández de Henestrosa, AR; Ayet, E; Merlos, M; Vela, JM; Plata-Salamán, CR; Almansa, C J Med Chem 63: 15508-15526 (2020)
- Günther, S; Reinke, PY; Fernández-García, Y; Lieske, J; Lane, TJ; Ginn, HM; Koua, FH; Ehrt, C; Ewert, W; Oberthuer, D; Yefanov, O; Meier, S; Lorenzen, K; Krichel, B; Kopicki, J; Gelisio, L; Brehm, W; Dunkel, I; Seychell, B; Gieseler, H; Norton-Baker, B; Escudero-Pérez, B; Domaracky, M; Saouane, S; Tolstikova, A; White, TA; Hänle, A; Groessler, M; Fleckenstein, H; Trost, F; Galchenkova, M; Gevorkov, Y; Li, C; Awel, S; Peck, A; Barthelmess, M; Schlünzen, F; Xavier, PL; Werner, N; Andaleeb, H; Ullah, N; Falke, S; Srinivasan, V; Franca, BA; Schwinzer, M; Brognaro, H; Rogers, C; Melo, D; Zaitsev-Doyle, JJ; Knoska, J; Peña Murillo, GE; Mashhour, AR; Guicking, F; Hennicke, V; Fischer, P; Hakanpää, J; Meyer, J; Gribbon, P; Ellinger, B; Kuzikov, M; Wolf, M; Beccari, AR; Bourenkov, G; Stetten, D; Pompidor, G; Bento, I; Panneerselvam, S; Karpics, I; Schneider, TR; Garcia Alai, MM; Niebling, S; Günther, C; Schmidt, C; Schubert, R; Han, H; Boger, J; Monteiro, DC; Zhang, L; Sun, X; Pletzer-Zelgert, J; Wollenhaupt, J; Feiler, CG; Weiss, MS; Schulz, E; Mehrabi, P; Karničar, K; Usenik, A; Loboda, J; Tidow, H; Chari, A; Hilgenfeld, R; Uetrecht, C; Cox, R; Zaliani, A; Beck, T; Rarey, M; Günther, S; Turk, D; Hinrichs, W; Chapman, HN; Pearson, AR; Betzel, C; Meents, A bioRxiv 2020: (2020)
- Olesen, PH; Sørensen, AR; Ursø, B; Kurtzhals, P; Bowler, AN; Ehrbar, U; Hansen, BF J Med Chem 46: 3333-41 (2003)
- Gökhan-Kelekçi, N; Koyunoqlu, S; Yabanoqlu, S; Yesilada, K; Ozgen, O; Uçar, G; Erol, K; Kendi, E; Yesilada, A Bioorg Med Chem 17: 675-89 (2009)
- Vara Salazar, YI; Aldaba Arévalo, E; Bello Iglesias, T; Roberts, RS; Simón Buela, L; Brea, JM; Carracedo, null; Loza García, MI US Patent US12202823 (2025)
- Fardella Bello, CE; Lagos Arévalo, CF; Vecchiola Cárdenas, AP; Allende Sanzana, FA; Diethelm Varela, BM; Recabarren Gajardo, GI; González Cisterna, PM US Patent US12304894 (2025)
- Díaz, JL; Christmann, U; Fernández, A; Luengo, M; Bordas, M; Enrech, R; Carro, M; Pascual, R; Burgueño, J; Merlos, M; Benet-Buchholz, J; Cerón-Bertran, J; Ramírez, J; Reinoso, RF; Fernández de Henestrosa, AR; Vela, JM; Almansa, C J Med Chem 56: 3656-65 (2013)
- PASTOR FERNÁNDEZ, J; MARTÍNEZ GONZÁLEZ, S; BLANCO APARICIO, C; GARCÍA GARCÍA, AB; RODRÍGUEZ ARÍSTEGUI, S; GÓMEZ DE LA OLIVA, CA; ALBARRÁN SANTIÑO, MI; CEBRIÁ GÓMEZ, A; MALUMBRES MARTÍNEZ, M US Patent US20240199630 (2024)
- Martínez González, S; Hernández, AI; Varela, C; Rodríguez-Arístegui, S; Lorenzo, M; Rodríguez, A; Rivero, V; Martín, JI; Saluste, CG; Ramos-Lima, F; Cendón, E; Cebrián, D; Aguirre, E; Gomez-Casero, E; Albarrán, M; Alfonso, P; García-Serelde, B; Oyarzabal, J; Rabal, O; Mulero, F; Gonzalez-Granda, T; Link, W; Fominaya, J; Barbacid, M; Bischoff, JR; Pizcueta, P; Pastor, J Bioorg Med Chem Lett 22: 3460-6 (2012)
- Pastor Fernández, J; Fernández-Capetillo Ruiz, O; Martínez González, S; Blanco Aparicio, C; Rico Ferreira, M; Toledo Lázaro, LI; Rodríguez Arísteguí, S; Murga Costa, M; Varela Busto, C; Lopez Contreras, AJ; Renner, O; Nieto Soler, M; Cebrián Muñoz, DA US Patent US9453031 (2016)
- ChEMBL_616797 (CHEMBL1103121) Inhibition of AR
- ChEMBL_1473107 (CHEMBL3421436) Inhibition of human AR
- ChEMBL_2292709 Inhibition of AR (unknown origin)
- ChEMBL_332775 (CHEMBL859226) Inhibitory activity against AR
- ChEMBL_447644 (CHEMBL896651) Binding affinity at AR
- ChEMBL_458140 (CHEMBL925473) Binding affinity at AR
- ChEMBL_634773 (CHEMBL1119509) Binding affinity to AR
- ChEMBL_728119 (CHEMBL1687061) Binding affinity to AR
- ChEMBL_785832 (CHEMBL1921048) Antagonist activity at AR
- ChEMBL_1473103 (CHEMBL3421432) Inhibition of AR (unknown origin)
- ChEMBL_1475554 (CHEMBL3424580) Binding affinity to human AR
- ChEMBL_1620824 (CHEMBL3863107) Binding affinity to human AR
- ChEMBL_31458 (CHEMBL643940) Inhibition of Aldose reductase (AR)
- ChEMBL_428792 (CHEMBL916225) Binding affinity to rat AR
- ChEMBL_438312 (CHEMBL887414) Agonist activity at human AR
- ChEMBL_438313 (CHEMBL887415) Binding affinity to human AR
- ChEMBL_1678019 (CHEMBL4028162) Binding affinity to AR (unknown origin)
- ChEMBL_792912 (CHEMBL1929758) Displacement of [3H]testosterone from AR
- ChEMBL_986494 (CHEMBL2434575) Binding affinity at human alpha2C AR
- ChEMBL_986495 (CHEMBL2434576) Binding affinity at human alpha2B AR
- ChEMBL_986496 (CHEMBL2434577) Binding affinity at human alpha2A AR
- ChEMBL_986497 (CHEMBL2434578) Agonist activity at human alpha2C AR
- ChEMBL_986498 (CHEMBL2434579) Agonist activity at human alpha2B AR
- ChEMBL_1473106 (CHEMBL3421435) Inhibition of human AR by fluorescence assay
- ChEMBL_2279105 Inhibition of AR LBD in human LNCaP cells
- ChEMBL_2323232 Induction of AR degradation in human LNCaP cells
- ChEMBL_2323233 Induction of AR degradation in human VCaP cells
- ChEMBL_36112 (CHEMBL648077) Antagonist activity against the Androgen Receptor (AR)
- ChEBML_1625701 Binding affinity to AR (unknown origin) by FP assay
- ChEMBL_2293004 Inhibition of AR (unknown origin) assessed as glycation activity
- ChEMBL_32092 (CHEMBL643668) Inhibitory activity against rat lens aldose reductase(AR).
- ChEMBL_603516 (CHEMBL1068435) Antagonist activity at AR by reporter gene assay
- ChEMBL_1853777 (CHEMBL4354401) Inhibition of R1881 induced-AR transcriptional activity in AR-positive human 22Rv1 cells harboring ARE14 construct after 24 hrs by luciferase assay
- ChEBML_36310 In vitro antagonist activity against rat prostatic androgen receptor (AR)
- ChEMBL_1625701 (CHEMBL3868170) Binding affinity to AR (unknown origin) by FP assay
- ChEMBL_2279104 Induction of degradation of AR LBD in human LNCaP cells
- ChEMBL_38909 (CHEMBL652012) Inhibitory activity against human beta-3 adrenergic receptor (AR)
- Reporter Assay The compounds were subjected to tests using an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells were engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells were also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer.
- ChEMBL_1671470 (CHEMBL4021499) Displacement of [3H]mibolerone from human AR after 3 hrs
- ChEMBL_2235581 (CHEMBL5149353) Agonist activity at human AR expressed in CHO-K1 cells
- ChEMBL_29597 (CHEMBL640255) Inhibition of [3H]-DPCPX binding to adenosine A1 receptor (AR).
- ChEMBL_29598 (CHEMBL640256) Inhibition of [3H]-DPCPX binding to adenosine A1 receptor (AR).
- ChEMBL_36310 (CHEMBL652259) In vitro antagonist activity against rat prostatic androgen receptor (AR)
- ChEMBL_631366 (CHEMBL1109118) Inhibition of aldose reductase from calf lense by AR assay
- ChEMBL_2260974 (CHEMBL5215985) Binding affinity to alpha2C AR (unknown origin) assessed as inhibition constant
- ChEMBL_32102 (CHEMBL644303) Tested for in vitro inhibition activity against rat Aldose reductase (AR)
- ChEMBL_32104 (CHEMBL644305) In vitro inhibition of Aldose reductase (AR) from rat lens (RL)
- ChEMBL_32128 (CHEMBL643708) Inhibition of [3H]ZM-241385 binding to adenosine A2A receptor(AR).
- ChEMBL_359728 (CHEMBL869334) Inhibition of rat AR-mediated reporter gene expression in COS7 cells
- ChEMBL_585097 (CHEMBL1054363) Binding affinity to AR by fluorescence polarization based competition binding assay
- SPA Binding Assay (IC50) and Coactivator Peptide Competitive FP Assay (IC50/EC50) A radiolabeled ligand competition scintillation proximity assay (SPA) for the androgen receptor (AR) using Ni-coated 384-well FlashPlates. It measures [3H]-DHT displacement from AR-LBD protein. AR functionality was determined by fluorescence polarization (excitation @485 nm, emission @ 530 nm) assay, which measures fluorescently labeled SRC2-3 peptide displacement from DHT-bound AR-LBD.
- ChEMBL_1621367 (CHEMBL3863650) Displacement of [18F]-FDHT from androgen receptor in human LNCAP/AR cells
- ChEMBL_1735708 (CHEMBL4151244) Antagonist activity at human AR assessed as reduction in DHT-induced transactivation
- ChEMBL_2227449 (CHEMBL5140962) Antagonist activity at Androgen receptor (unknown origin) assessed as downregulation of AR
- ChEMBL_2279099 Binding affinity to GST tagged AR LBD (unknown orign) by radioligand binding assay
- ChEMBL_2496598 Antagonist activity at AR (unknown origin) expressed in chemically activated Luciferase expression system
- ChEMBL_306188 (CHEMBL830982) Inhibition of AR-dimerization in CHO-K1 cells expressing human androgen receptor
- ChEMBL_31784 (CHEMBL643110) Tested for in vitro inhibition activity against human Aldose reductase (human AR)
- ChEMBL_32141 (CHEMBL646351) Dissociation constant of [3H]ZM-241385 binding to adenosine A2A receptor(AR)
- ChEMBL_41529 (CHEMBL858101) Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
- ChEMBL_41535 (CHEMBL654942) Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
- ChEMBL_41547 (CHEMBL654954) Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
- ChEMBL_41678 (CHEMBL858100) Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
- ChEMBL_41699 (CHEMBL654141) Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
- ChEMBL_41706 (CHEMBL654148) Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells.
- ChEMBL_449233 (CHEMBL899495) Displacement of [3H]DHT from human recombinant AR expressed in Sf9 cells
- ChEMBL_643540 (CHEMBL1212404) Displacement of [3H]DHT from AR in human MDA-MB-453 cells
- ChEMBL_964273 (CHEMBL2395387) Displacement of [3H]R1881 from AR in human MDA-MB-453 cells
- ChEMBL_1339118 (CHEMBL3243253) Binding affinity to human AR NTD (1 to 561 aa) expressed in CV1 cells coexpressing human AR-LBD (644-919 aa) assessed as N/C-termini interaction by androgenic assay
- SPA Binding Assay (IC50) A radiolabeled ligand competition scintillation proximity assay (SPA) for the androgen receptor (AR) using Ni-coated 384-well FlashPlates. It measures [3H]-DHT displacement from AR-LBD protein.
- ChEBML_31798 Inhibitory concentration against porcine lens aldose reductase (AR) with DL-glyceraldehyde as the substrate
- ChEBML_41541 Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
- ChEBML_41682 Agonistic activity against cloned human beta1-AR (beta-2-adrenergic receptor) in CHO cells
- ChEBML_41707 Agonistic activity against cloned human beta3-AR (beta-3-adrenergic receptor) in CHO cells
- ChEMBL_2227442 (CHEMBL5140955) Antagonist activity at human Androgen receptor measured by AR-mediated transcriptional activation assay
- ChEMBL_2285082 Binding affinity to AR (unknown origin) incubated for 4 hrs by fluorescence polarization assay
- ChEMBL_726892 (CHEMBL1686598) Displacement of [3H]testosterone from Sprague-Dawley rat AR by liquid scintillation counting
- Coactivator Peptide Competitive FP Assay (IC50/EC50) AR functionality was determined by fluorescence polarization (excitation @485 nm, emission @ 530 nm) assay, which measures fluorescently labeled SRC2-3 peptide displacement from DHT-bound AR-LBD.
- ChEBML_218131 Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
- ChEMBL_2070692 (CHEMBL4726226) Displacement of [3H]-mibolerone from GST-tagged human AR-LBD expressed in HEK293 cells
- ChEMBL_29602 (CHEMBL640260) Dissociation constant of [3H]DPCPX binding to adenosine A1 receptor (AR) at 0.05 nM
- ChEMBL_29603 (CHEMBL640261) Dissociation constant of [3H]-DPCPX binding to adenosine A1 receptor (AR) at 0.1 nM
- ChEMBL_29604 (CHEMBL640262) Dissociation constant of [3H]DPCPX binding to adenosine A1 receptor (AR) at 100 nM
- ChEMBL_29605 (CHEMBL640263) Dissociation constant of [3H]DPCPX binding to adenosine A1 receptor (AR) at 200 nM
- ChEMBL_29606 (CHEMBL640264) Dissociation constant of [3H]DPCPX binding to adenosine A1 receptor (AR) at 5 nM
- ChEMBL_29607 (CHEMBL640265) Dissociation constant of [3H]-DPCPX binding to adenosine A1 receptor(AR) at 0.05 nM
- ChEMBL_29724 (CHEMBL646657) Dissociation constant of [3H]DPCPX binding to adenosine A1 receptor(AR) at 0.1 nM
- ChEMBL_29725 (CHEMBL646658) Dissociation constant of [3H]-DPCPX binding to adenosine A1 receptor(AR) at 100 nM
- ChEMBL_29726 (CHEMBL646659) Dissociation constant of [3H]DPCPX binding to adenosine A1 receptor(AR) at 5 nM
- ChEMBL_306281 (CHEMBL828424) Inhibition of [3H]mibolerone binding to human Androgen receptor of PC3/AR Cell Lysate
- ChEMBL_37248 (CHEMBL651569) Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
- ChEMBL_38172 (CHEMBL650243) Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
- ChEMBL_38262 (CHEMBL646905) Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
- ChEMBL_449234 (CHEMBL899496) Antagonist activity at human AR in MDA-MB453-MMTV-luci cells by functional assay
- ChEMBL_2111616 (CHEMBL4820466) Antagonist activity at VP16-AR wild-type (unknown origin) transfected in human HepG2 cells cotransfected with ARE-LUC incubated for 48 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay
- ChEBML_1695282 Inhibition of AR in Sprague-Dawley rat lens using DL-glyceraldehyde as substrate by spectrophotometric analysis
- ChEMBL_1864064 (CHEMBL4365039) Displacement of [3H]methyltrienolone from recombinant human AR after 1440 mins by scintillation counting analysis
- ChEMBL_2070690 (CHEMBL4726224) SARD activity at AR-LBD T877A mutant (unknown origin) after 4 hrs by luciferase assay
- ChEMBL_2070691 (CHEMBL4726225) SARD activity at AR-LBD F876L mutant (unknown origin) after 4 hrs by luciferase assay
- ChEMBL_218131 (CHEMBL822565) Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
- ChEMBL_2421887 Antagonist activity at AR in human LNCaP cells incubated for 24 hrs by Western blotting analysis
- ChEMBL_643543 (CHEMBL1212407) Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay
- ChEMBL_788156 (CHEMBL1919237) Antagonist activity at human AR overexpressed in human LNCAP cells by luciferase reporter gene assay
- ChEMBL_2111624 (CHEMBL4820474) Antagonist activity at AR F877L mutant (unknown origin) transfected in human LNCAP cells cotransfected with ARE-LUC incubated for 20 to 24 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay
- ChEMBL_2111625 (CHEMBL4820475) Antagonist activity at AR wild-type (unknown origin) transfected in human LNCAP cells cotransfected with ARE-LUC incubated for 20 to 24 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay
- ChEMBL_2453378 Antagonist activity at AR in human LNCaP cells assessed as reduction in R1881-induced AR transcriptional activity preincubated for 60 mins followed by R1881 addition and measured after 24 hrs by Steady-Glo reagent based luciferase assay
- ChEMBL_1689766 (CHEMBL4040336) Androgenic activity at human androgen receptor expressed in African green monkey CV-1 cells assessed as increase in interaction between VP16-fused AR-NTD and GAL4-fused AR-LBD after 17 hrs by luciferase reporter gene assay
- ChEBML_39070 Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
- ChEMBL_2337100 Antagonist activity at AR transcription in human 22Rv1 cells incubated for 24 hrs in presence of R1881
- ChEMBL_2453393 Displacement of fluormone AL green from AR-LBD (unknown origin) incubated for 3 hrs by PolarScreen assay
- ChEMBL_36123 (CHEMBL647749) Inhibition of 1.0 nM [3H]mibolerone binding to human androgen receptor of PC3/AR cell lysate
- ChEMBL_38269 (CHEMBL646912) In vitro agonistic activity against cAMP accumulation level in CHO cells expressing human beta-AR receptor
- ChEMBL_41530 (CHEMBL654937) Concentration that causes 50% inhibition of human beta 1 adrenergic receptor (AR), expressed in CHO cells.
- ChEMBL_41548 (CHEMBL858099) Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
- ChEMBL_634399 (CHEMBL1118176) Displacement of [3H]DHT from human AR expressed in baculovirus Sf9 cells system by scintillation counting
- ChEMBL_771288 (CHEMBL1839476) Inhibition of human recombinant MMP2 assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771363 (CHEMBL1839744) Inhibition of human recombinant MMP14 assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771364 (CHEMBL1839745) Inhibition of human recombinant MMP9 assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771365 (CHEMBL1839746) Inhibition of human recombinant MMP1 assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771366 (CHEMBL1839747) Inhibition of human recombinant MMP3 assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771367 (CHEMBL1839748) Inhibition of human recombinant MMP7 assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEBML_37242 Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
- ChEBML_38164 Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
- ChEMBL_1339117 (CHEMBL3243252) Agonist activity at human AR expressed in CV1 cells after 17 hrs by luciferase reporter gene assay
- ChEMBL_1442061 (CHEMBL3373429) Inhibition of human recombinant MMP1 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442062 (CHEMBL3373430) Inhibition of human recombinant MMP2 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442063 (CHEMBL3373431) Inhibition of human recombinant MMP3 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442064 (CHEMBL3373432) Inhibition of human recombinant MMP7 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442065 (CHEMBL3373433) Inhibition of human recombinant MMP8 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442066 (CHEMBL3373434) Inhibition of human recombinant MMP9 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442067 (CHEMBL3373435) Inhibition of human recombinant MMP10 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1442068 (CHEMBL3374019) Inhibition of human recombinant MMP14 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_1989103 (CHEMBL4622650) Antagonistic activity at AR in human 22Rv1 cells assessed as reduction in cell number by CCK8 assay
- ChEMBL_36124 (CHEMBL649556) Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells
- ChEMBL_39070 (CHEMBL651141) Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
- ChEMBL_629233 (CHEMBL1121347) Antagonist activity at AR in human LNCAP cells assessed as effect on cell proliferation after 6 days
- ChEMBL_643541 (CHEMBL1212405) Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay
- ChEMBL_964272 (CHEMBL2395386) Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis
- ChEMBL_971947 (CHEMBL2405557) Antagonist activity at human pSG5-AR assessed as inhibition of dihydrotestosterone-induced effect by reporter gene assay
- ChEMBL_977682 (CHEMBL2423840) Displacement of [3H]-Testosterone from human AR expressed in 293 cells after 16 hrs by scintillation counting
- ChEMBL_991126 (CHEMBL2446582) Inhibition of human recombinant MMP-2 using MOCAcPLGLA2pr(Dnp)AR-NH2 as substrate by fluorescence spectrophotometric analysis
- AR Antagonism Antagonism of test compounds for AR was measured by reporter gene assay in human embryonic kidney (HEK293) cells stably transfected with an expression vector encoding full-length human AR and androgen responsive luciferase reporter gene construct (hAR/HEK293 cells). To determine antagonism for hAR, the cells were treated simultaneously with increasing concentrations of the test compound and submaximal concentration of testosterone (usually 0.45 nM). The final DMSO concentration was 1%. All test compounds were studied in triplicates. The cells were incubated for 24 before measurement of luciferase activity using Luciferase Assay System (Promega Corporation).Agonism of test compounds in AR overexpressing cells was measured by reporter gene assay in HEK293 cells stably transfected with an expression vector encoding full-length human AR and androgen responsive luciferase reporter gene construct. A clone expressing high levels of androgen receptor (5 times more than AR levels in AR-HEK293 cells) was selected to study agonism in AR overexpressing cells. To determine agonism, the cells were treated with increasing concentrations of the test compound. The final DMSO concentration was 1%. The test compounds were studied in triplicates and luciferase activity was determined as described above.
- ChEBML_41520 In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
- ChEBML_41689 In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta3-AR receptor
- ChEMBL_1431418 (CHEMBL3388707) Inhibition of human recombinant MMP13 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431419 (CHEMBL3388708) Inhibition of human recombinant MMP1 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431420 (CHEMBL3388709) Inhibition of human recombinant MMP2 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431421 (CHEMBL3388710) Inhibition of human recombinant MMP3 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431422 (CHEMBL3388711) Inhibition of human recombinant MMP7 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431423 (CHEMBL3388712) Inhibition of human recombinant MMP8 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431424 (CHEMBL3388713) Inhibition of human recombinant MMP9 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1431425 (CHEMBL3389268) Inhibition of human recombinant MMP10 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1624955 (CHEMBL3867367) Antagonist activity at human AR expressed in HEK293 cells measured after 24 hrs by luciferase reporter gene assay
- ChEMBL_1929381 (CHEMBL4432557) Inhibition of BRD4 in human LNCAP cells assessed as down regulation of nuclear AR level by immunofluorescence assay
- ChEMBL_1934449 (CHEMBL4480101) Inhibition of AR transcriptional activity in human ARR2PB-eGFP expressing LNCaP cells after 3 days by fluorescence assay
- ChEMBL_2022762 (CHEMBL4676575) Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method
- ChEMBL_2172741 (CHEMBL5057875) Inhibition of AR transcriptional activity in human LNCaP cells harboring ARR2PB-eGFP assessed as decrease in PSA level
- ChEMBL_629229 (CHEMBL1121343) Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting
- ChEMBL_771289 (CHEMBL1839477) Inhibition of human recombinant MMP9 catalytic domain assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771362 (CHEMBL1839743) Inhibition of human recombinant MMP14 catalytic domain assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- ChEMBL_771372 (CHEMBL1839753) Inhibition of human recombinant MMP3 catalytic domain assessed as hydrolysis of MOCAcPLGLA2pr(Dnp)AR-NH2 by fluorescence spectrofluorometry
- Inhibition Assay The binding of ligands to wild-type beta-AR was measured by competition with 35 pM 125I-CYP.
- ChEBML_37249 Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR) at a concentration of 10000 nm
- ChEBML_38910 Compound was evaluated for its inhibitory activity against human beta-3 adrenergic receptor (AR) at a concentration of 100 nM
- ChEMBL_1442057 (CHEMBL3373425) Inhibition of human recombinant MMP13 catalytic domain using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
- ChEMBL_2172739 (CHEMBL5057873) Binding affinity to GST-tagged AR ligand binding domain (unknown origin) measured after 4 hrs by fluorescence polarization assay
- ChEMBL_2172740 (CHEMBL5057874) Inhibition of AR transcriptional activity in human LNCaP cells harboring ARR2PB-eGFP incubated for 72 hrs by fluorescence assay
- ChEMBL_2264848 Inhibition of androgen receptor in human LNCaP cells assessed as inhibition of AR transcription activity by dual-luciferase reporter assays
- ChEMBL_38788 (CHEMBL653162) Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
- ChEMBL_41521 (CHEMBL654503) In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
- ChEMBL_629235 (CHEMBL1121349) Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
- ChEMBL_687031 (CHEMBL1291551) Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
- ChEMBL_990996 (CHEMBL2445794) Inhibition of human recombinant MMP-8 catalytic domain using McaKPLGL9(Dpa)AR-NH2 as substrate by fluorescence spectrophotometric analysis
- ChEMBL_991001 (CHEMBL2445799) Inhibition of human recombinant MMP-14 catalytic domain using MOCAcPLGLA2pr(Dnp)AR-NH2 as substrate by fluorescence spectrophotometric analysis
- ChEMBL_991125 (CHEMBL2446581) Inhibition of human recombinant MMP-9 catalytic domain using MOCAcPLGLA2pr(Dnp)AR-NH2 as substrate by fluorescence spectrophotometric analysis
- ChEMBL_1339116 (CHEMBL3243251) Displacement of [3H]mibolerone from full length human AR expressed in COS cells after 3.5 hrs by liquid scintillation counting
- ChEMBL_1431426 (CHEMBL3389269) Inhibition of human recombinant GST-tagged MMP14 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate after 40 mins by spectrofluorimetry
- ChEMBL_1508767 (CHEMBL3603106) Inhibition of human SIRT5 using CH3CONH-AR-(Nepsilon-succinyl-lysine)-ST-CONH2 as substrate after 5 mins by HPLC analysis
- ChEMBL_1648530 (CHEMBL3997586) Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
- ChEMBL_1648531 (CHEMBL3997587) Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method
- ChEMBL_1671471 (CHEMBL4021500) Agonist activity at human AR expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay
- ChEMBL_1736257 (CHEMBL4151793) Agonist activity at AR (unknown origin) expressed in human LNCaP cells incubated for 20 hrs by luciferase reporter gene assay
- ChEMBL_1858221 (CHEMBL4358950) Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry
- ChEMBL_37249 (CHEMBL651570) Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR) at a concentration of 10000 nm
- ChEMBL_766306 (CHEMBL1826238) Displacement of SRC2-3 peptide from human AR ligand binding site expressed in Escherichia coli BL21 by AF2 FP assay
- ChEMBL_766307 (CHEMBL1826239) Inhibition of human AR AF2 site expressed in human LNCap cells coexpressing eGFP -ARR2PB assessed as inhibition of transcriptional activity
- ChEMBL_959632 (CHEMBL2382702) Inhibition of MMP-14 (unknown origin) using Mca-PLGLDpa-AR-NH2 as substrate preincubated for 30 mins by fluorescence assay
- ChEMBL_959635 (CHEMBL2382705) Inhibition of MMP-7 (unknown origin) using Mca-PLGLDpa-AR-NH2 as substrate preincubated for 30 mins by fluorescence assay
- Luciferase Reporter Assay Activities of the test compounds to inhibit androgen receptor mediated transcription induced by DHT were evaluated using stable transfected AR/CHO#3 cells plated onto 96-well luminoplates. After cells were lysed, cell extracts were prepared for luciferase assay. The luciferase activity was measured with a ML3000 luminometer. AR antagonist activities were calculated. The concentration of compounds showing 50% AR antagonist activity, the IC50 values, were obtained through nonlinear analysis using the statistical analysis system (SAS).
- ChEMBL_1923008 (CHEMBL4425964) Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
- ChEMBL_2330382 Activation of Gal-DBD and NHRLBD fused AR (unknown origin) transfected in African green monkey CV-1 cells by luciferase reporter assay
- ChEMBL_2447508 Inhibition of human Cathepsin D using MCA-PLGL-Dap(Dnp)-AR-NH2 as substrate incubated for 10 mins by FRET-enzymatic assay
- Biological Assay The N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides described herein exhibit androgen receptor (AR) inhibiting properties. This AR inhibiting activity was measured in a transactivation test by the dissociation constants KdR (rest), KdA (active), and Kdapp (apparent).A compound may be said to be an AR inhibitor if it has a dissociation constant, Kdapp, of less than or equal to 1 μM, and a KdR/KdA ratio of less than or equal to 10 in a transactivation test.Preferred AR type receptor inhibitors have a dissociation constant of less than or equal to 500 nM, and more preferably less than or equal to 100 nM.
- ChEMBL_1614152 (CHEMBL3855952) Agonist activity at human alpha2a-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
- ChEMBL_1614153 (CHEMBL3855953) Agonist activity at human alpha2b-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
- ChEMBL_1614154 (CHEMBL3855954) Agonist activity at human alpha2c-AR expressed in CHO cells assessed as rate of acidification after 240 mins by cytosensor microphysiometric analysis
- ChEMBL_1625928 (CHEMBL3868397) Inhibition of recombinant human AMPA-activated MMP13 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625929 (CHEMBL3868398) Inhibition of recombinant human AMPA-activated MMP1 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625930 (CHEMBL3868399) Inhibition of recombinant human AMPA-activated MMP2 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625931 (CHEMBL3868400) Inhibition of recombinant human AMPA-activated MMP3 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625932 (CHEMBL3868401) Inhibition of recombinant human AMPA-activated MMP7 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625933 (CHEMBL3868402) Inhibition of recombinant human AMPA-activated MMP8 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625934 (CHEMBL3868403) Inhibition of recombinant human AMPA-activated MMP9 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625935 (CHEMBL3868404) Inhibition of recombinant human AMPA-activated MMP10 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625936 (CHEMBL3868405) Inhibition of recombinant human AMPA-activated MMP12 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1625937 (CHEMBL3868406) Inhibition of recombinant human GST-tagged MMP14 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1668159 (CHEMBL4018047) Inhibition of APMA-activated recombinant human MMP2 expressed in CHO cells using Mca-PLGL-(DapDnp)-AR-NH2 as substrate by fluorescence assay
- ChEMBL_1668164 (CHEMBL4018052) Inhibition of APMA-activated recombinant human MMP9 expressed in CHO cells using Mca-PLGL-(DapDnp)-AR-NH2 as substrate by fluorescence assay
- ChEMBL_1742330 (CHEMBL4158080) Antagonist activity at AR in mouse SC3 cells assessed as inhibition of DHT-induced cell proliferation after 3 days by CCK8 assay
- ChEMBL_1803399 (CHEMBL4275691) Displacement of Fluormone-DHT from rat GST-tagged rat AR LBD expressed in insect cells after 4 hrs by fluorescence polarization assay
- ChEMBL_2329557 Displacement of [3H]mibolerone from GST-tagged wild type AR ligand binding domain (unknown origin) incubated for 16 hrs by scintillation counting analysis
- ChEMBL_2501841 Binding affinity to full length human recombinant MMP-13 using Mca-PLGL-Dpa-AR-NH2 as fluorogenic peptide substrate assessed as inhibition constant
- ChEMBL_1621743 (CHEMBL3864026) Displacement of fluormone-DHT green from His/GST-tagged rat AR ligand binding domain after 4 to 8 hrs by fluorescence polarization assay
- ChEMBL_1648532 (CHEMBL3997588) Displacement of [3H]DHA from beta2-AR (unknown origin) expressed in baculovirus infected sf9 cell membranes after 1 hr by scintillation counting method
- ChEMBL_1648545 (CHEMBL3997601) Partial agonist activity at human beta2-AR expressed in CHOK1 cells assessed as inhibition of cimaterol-induced CRE-SPAP production after 5 hrs
- ChEMBL_1668165 (CHEMBL4018053) Inhibition of APMA-activated recombinant human MMP13 expressed in mouse NS0 cells using Mca-PLGL-(DapDnp)-AR-NH2 as substrate by fluorescence assay
- ChEMBL_1803383 (CHEMBL4275675) Inhibition of R1881-induced full length AR transcriptional activity in human LNCAP cells harboring AR2PB-eGFP construct after 72 hrs by fluorescence assay
- ChEMBL_2160327 (CHEMBL5045077) Antagonist activity at human AR AF2 assessed as inhibition of fluorescent-labelled D11-FxxLF peptide Co-activator to receptor by TR-FRET assay
- ChEMBL_2227466 (CHEMBL5140979) Antagonist activity at Androgen receptor (unknown origin) assessed as inhibition of activation function 1 (AF-1) of AR N-terminal transactivation domain (NTD)
- ChEMBL_2227483 (CHEMBL5140996) Antagonist activity at Androgen receptor in human LNCaP cells assessed as inhibition of Binding Function 3 (BF3) of AR measured by luciferase assay
- ChEMBL_41534 (CHEMBL654941) Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
- ChEMBL_41677 (CHEMBL655820) Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
- ChEMBL_41698 (CHEMBL858102) Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
- ChEMBL_41705 (CHEMBL654147) Ability to cause cAMP accumulation in CHO cells expressing human beta-3 AR expressed as the negative logarithm of the molar drug concentration
- Competitive Radioligand Displacement Assay and AR-Mediated Transcription Activation Assay The Ki values were determined by the application of the Cheng-Prusoff equation: Ki = (IC50 x Kd)/(Kd+[L]) where [L] is the concentration of [3H]MIB (1 nM ) and Kd is the dissociation constant of the [3H]MIB determined in the saturation analysis, IC50 is determined by computer fitting data for the competitive binding of each AR ligand. EC50 is the lowest concentration of the ligand capable of maximally stimulating AR-mediated transcription during transfection experiments.
- ChEMBL_1651669 (CHEMBL4000924) Inhibition of APMA-activated recombinant human MMP-13 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651670 (CHEMBL4000925) Inhibition of APMA-activated recombinant human MMP-2 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651671 (CHEMBL4000926) Inhibition of APMA-activated recombinant human MMP-8 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651672 (CHEMBL4000927) Inhibition of APMA-activated recombinant human MMP-10 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651675 (CHEMBL4000930) Inhibition of APMA-activated recombinant human MMP-1 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651676 (CHEMBL4000931) Inhibition of APMA-activated recombinant human MMP-3 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651677 (CHEMBL4000932) Inhibition of APMA-activated recombinant human MMP-7 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1651678 (CHEMBL4000933) Inhibition of APMA-activated recombinant human MMP-9 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1803354 (CHEMBL4275646) Antagonist activity at AR in human LNCAP cells assessed as reduction in DHT-induced transcriptional activation after 24 hrs by luciferase reporter gene assay
- ChEMBL_2160325 (CHEMBL5045075) Binding affinity to human AR LBD (663 to 920 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by biolayer interferometry assay
- Androgen Receptor Binding Assay The competitive radio-ligand binding analysis was performed on human AR extracts from transfected Sf9 cells in the presence or absence of differing concentrations of test compound and a fixed concentration of 3H-dihydrotestosterone (3H-DHT) as tracer. AR bound 3H-DHT levels are determined in the presence of compounds and compared to levels of receptor specific binding when no competitor is present. Compound binding affinity to the human AR is expressed as the concentration of compound at which 50% of the maximum specific binding is inhibited (IC50).
- ChEMBL_1923009 (CHEMBL4425965) Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting
- ChEMBL_1934683 (CHEMBL4480335) Inhibition of MMP1 (unknown origin) using Mca-PLGL-Dpa-AR as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
- ChEMBL_1934684 (CHEMBL4480336) Inhibition of MMP3 (unknown origin) using Mca-PLGL-Dpa-AR as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
- ChEMBL_1934685 (CHEMBL4480337) Inhibition of MMP9 (unknown origin) using Mca-PLGL-Dpa-AR as substrate preincubated for 20 mins followed by substrate addition by fluorescence plate reader analysis
- ChEMBL_2239506 (CHEMBL5153402) Inhibition of full length human AR stably expressed in human HEK293 cells assessed as luciferase activity incubated for 24 hrs by microplate luminometer luciferase assay
- ChEMBL_38259 (CHEMBL884032) Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
- ChEMBL_38260 (CHEMBL646903) Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-1 adrenergic receptor (AR) in the presence of [125I]iodocyanopindolol
- ChEMBL_38263 (CHEMBL646906) Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
- ChEMBL_38313 (CHEMBL647876) Compound was evaluated for its inhibitory activity against CHO cells expressing the cloned human beta-2 adrenergic receptor (AR) in the presence of [125I]-iodocyanopindolol
- ChEMBL_474428 (CHEMBL934261) Antagonist activity at human AR ligand binding domain expressed in african green monkey COS7 cells in presence of 5-alpha-dihydrotestosterone by Gal4 hybrid assay
- ChEMBL_687028 (CHEMBL1291499) Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
- ChEMBL_1651679 (CHEMBL4000934) Inhibition of APMA-activated recombinant human GST-tagged MMP-14 using Cy3-PLGLK(Cy5Q)AR-NH2 peptide as substrate measured after 40 mins by spectrofluorimetric method
- ChEMBL_1735695 (CHEMBL4151231) Antagonist activity at human CMX-AR expressed in HEK293 cells assessed as reduction in dihydrotestosterone-induced transactivation activity after 24 hrs by luciferase reporter gene assay
- ChEMBL_1735784 (CHEMBL4151320) Inhibition of recombinant human MMP1 catalytic domain (Phe100 to Gln268 residues) expressed in Escherichia coli using McaKPLGL-Dpa-AR-NH2 as substrate by fluorescence spectrophotometric method
- ChEMBL_1735788 (CHEMBL4151324) Inhibition of recombinant human MMP8 catalytic domain (Phe99 to Gln269 residues) expressed in Escherichia coli using McaKPLGL-Dpa-AR-NH2 as substrate by fluorescence spectrophotometric method
- ChEMBL_1803361 (CHEMBL4275653) Antagonist activity at AR in human LNCAP cells assessed as reduction in DHT-induced cell growth treated for every 2 days for 4 days by hemocytometry
- ChEMBL_1847878 (CHEMBL4348419) Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay
- ChEMBL_1922603 (CHEMBL4425559) Inhibition of human MMP1 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922604 (CHEMBL4425560) Inhibition of human MMP2 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922605 (CHEMBL4425561) Inhibition of human MMP3 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922606 (CHEMBL4425562) Inhibition of human MMP7 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922607 (CHEMBL4425563) Inhibition of human MMP9 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922608 (CHEMBL4425564) Inhibition of human MMP13 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922609 (CHEMBL4425565) Inhibition of human MMP14 using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_1922610 (CHEMBL4425566) Inhibition of human TACE using Mca-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH as substrate measured after 2 to 4 hrs by fluorescence analysis
- ChEMBL_2014864 (CHEMBL4668442) Inhibition of recombinant human MMP2 expressed in human HeLaS3 cells using MOCAcPLGLA2pr(Dnp)-AR-NH2 as substrate incubated for 15 to 30 mins by fluorescence method
- ChEMBL_2014865 (CHEMBL4668443) Inhibition of recombinant human MMP9 expressed in human HeLaS3 cells using MOCAcPLGLA2pr(Dnp)-AR-NH2 as substrate incubated for 15 to 30 mins by fluorescence method
- ChEMBL_2160328 (CHEMBL5045078) Antagonist activity against human androgen receptor expressed in human LNCap cells trasfected with ARR2PB-eGFP cells incubated for 3 days by fluorescence based AR transcription assay
- ChEMBL_624727 (CHEMBL1113403) Antagonist activity at AR in human MDA-kb2 cells co-transfected with MMTV-luc assessed as decrease in DHT-induced luciferase activity by reporter gene assay
- ChEMBL_1663587 (CHEMBL4013268) Inhibition of human MMP3 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopropionyl)-AR-OH as substrate after 2 to 4 hrs by fluorescence assay
- ChEMBL_1663588 (CHEMBL4013269) Inhibition of human MMP12 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopropionyl)-AR-OH as substrate after 2 to 4 hrs by fluorescence assay
- ChEMBL_1663590 (CHEMBL4013271) Inhibition of human MMP14 using Mca-PQGL-(3-[2, 4-dinitrophenyl]-L-2, 3-diaminopropionyl)-AR-OH as substrate after 2 to 4 hrs by fluorescence assay
- ChEMBL_1784000 (CHEMBL4255517) Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
- ChEMBL_1826850 (CHEMBL4326724) Inhibition of recombinant human MMP-2 preincubated for 10 mins followed by Mca-PLGL-Dpa-AR-NH2 substrate addition and measured for 5 mins by fluorescence assay
- ChEMBL_2227484 (CHEMBL5140997) Antagonist activity at Androgen receptor in human LNCaP cells assessed as inhibition of DNA binding domain of AR measured by enhanced green fluorescent protein transcriptional (eGFPT) assay
- ChEMBL_841247 (CHEMBL2089650) Antagonist activity at wild type AR LBD assessed as inhibition of DHT-induced fluorescent labeled D11-FxxLF recruitment after 2 to 4 hrs by TR-FRET assay