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ChEMBL ligand: CHEMBL69367 (AM580) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
ChEMBL | Binding affinity for baculovirus-expressed Retinoic acid receptor RAR alpha | B | 7.44 | pKd | 36 | nM | Kd | J Med Chem (1996) 39: 3035-3038 [PMID:8759622] |
ChEMBL | Binding affinity fo retinoic acid receptor RAR alpha | B | 7.44 | pKd | 36 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
ChEMBL | Binding affinity for Retinoic Acid Receptor alpha (RAR alpha) | B | 7.39 | pIC50 | 41 | nM | IC50 | J Med Chem (2000) 43: 409-419 [PMID:10669568] |
ChEMBL | Activity at RARalpha expressed in mouse NIH3T3 cells by R-SAT assay | B | 7.1 | pEC50 | 79.43 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
ChEMBL | Agonist activity at RARalpha by TR-FRET assay | F | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (2011) 54: 788-808 [PMID:21218783] |
ChEMBL | Effective concentration for retinoic acid receptor RAR alpha transcriptional activation | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
GtoPdb | - | - | 9.52 | pEC50 | 0.3 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
ChEMBL | Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 9.52 | pEC50 | 0.3 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
ChEMBL | Binding affinity for retinoic acid receptor RAR beta | B | 5.85 | pKd | 1400 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
ChEMBL | Binding affinity for baculovirus-expressed Retinoic acid receptor RAR beta | B | 5.87 | pKd | 1361 | nM | Kd | J Med Chem (1996) 39: 3035-3038 [PMID:8759622] |
ChEMBL | Transcriptional activity against RARbeta1 | F | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2005) 48: 7517-7519 [PMID:16302793] |
ChEMBL | Activity at RARbeta1 expressed in mouse NIH3T3 cells by R-SAT assay | B | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
ChEMBL | Transcriptional activity against RARbeta2 | F | 7.7 | pEC50 | 19.95 | nM | EC50 | J Med Chem (2005) 48: 7517-7519 [PMID:16302793] |
ChEMBL | Agonist activity at RARbeta2 expressed in mouse NIH3T3 cells by R-SAT assay | F | 7.7 | pEC50 | 19.95 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
ChEMBL | Effective concentration for retinoic acid receptor RAR beta transcriptional activation | F | 8.05 | pEC50 | 9 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
ChEMBL | Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 8.07 | pEC50 | 8.6 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
GtoPdb | - | - | 8.07 | pEC50 | 8.6 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
ChEMBL | Binding affinity for baculovirus-expressed Retinoic acid receptor RAR gamma | B | 5.42 | pKd | 3824 | nM | Kd | J Med Chem (1996) 39: 3035-3038 [PMID:8759622] |
ChEMBL | Binding affinity for retinoic acid receptor RAR gamma | B | 5.42 | pKd | 3800 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
ChEMBL | Activity at RARgamma expressed in mouse NIH3T3 cells by R-SAT assay | B | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
ChEMBL | Effective concentration for retinoic acid receptor RAR gamma transcriptional activation | F | 7.72 | pEC50 | 19 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
ChEMBL | Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
GtoPdb | - | - | 7.89 | pEC50 | 13 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]