AC261066 [Ligand Id: 4054] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL198997 (AC-261066)
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Mouse [ChEMBL: CHEMBL2792] [GtoPdb: 590] [UniProtKB: P11416]
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
  • Retinoic acid receptor-β/Retinoic acid receptor beta in Mouse [ChEMBL: CHEMBL3266] [GtoPdb: 591] [UniProtKB: P22605]
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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Mouse [ChEMBL: CHEMBL4177] [GtoPdb: 592] [UniProtKB: P18911]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]