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 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]