AC261066 [Ligand Id: 4054] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL198997 (AC-261066) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
| ChEMBL | Activity at RARalpha expressed in mouse NIH3T3 cells by R-SAT assay | B | 6.2 | pEC50 | 630.96 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2792] [GtoPdb: 590] [UniProtKB: P11416] | ||||||||
| ChEMBL | Transactivation of GAL4-fused mouse RARalpha-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay | B | 7.15 | pEC50 | 70 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 995-1000 [PMID:30792038] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Activity at RARbeta1 expressed in mouse NIH3T3 cells by R-SAT assay | B | 6.4 | pEC50 | 398.11 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| ChEMBL | Transcriptional activity against RARbeta2 | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2005) 48: 7517-7519 [PMID:16302793] |
| GtoPdb | - | - | 8.1 | pEC50 | - | - | - | J Med Chem (2005) 48: 7517-9 [PMID:16302793] |
| ChEMBL | Agonist activity at RARbeta2 expressed in mouse NIH3T3 cells by R-SAT assay | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3266] [GtoPdb: 591] [UniProtKB: P22605] | ||||||||
| ChEMBL | Transactivation of GAL4-fused mouse RARbeta-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay | B | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 995-1000 [PMID:30792038] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
| ChEMBL | Activity at RARgamma expressed in mouse NIH3T3 cells by R-SAT assay | B | 6.3 | pEC50 | 501.19 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4177] [GtoPdb: 592] [UniProtKB: P18911] | ||||||||
| ChEMBL | Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay | B | 8.24 | pEC50 | 5.8 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 995-1000 [PMID:30792038] |
ChEMBL data shown on this page come from version 33:
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]
