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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 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]