AC55649 [Ligand Id: 4055] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL425027 (AC-55649)
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
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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 5.6 pEC50 2511.89 nM EC50 J. Med. Chem. (2009) 52: 1540-1545 [PMID:19239230]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Transcriptional activity against RARbeta1 F 5 pEC50 >10000 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 5.7 pEC50 1995.26 nM EC50 J. Med. Chem. (2009) 52: 1540-1545 [PMID:19239230]
ChEMBL Transcriptional activity against RARbeta2 F 6.9 pEC50 125.89 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 6.9 pEC50 125.89 nM EC50 J. Med. Chem. (2009) 52: 1540-1545 [PMID:19239230]
GtoPdb Affinity for RARβ2 isoform. - 7.3 pEC50 - - - J Med Chem (2005) 48: 7517-9 [PMID:16302793];
J Med Chem (2009) 52: 1540-5 [PMID:19239230]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]