Ro 40-6055 [Ligand Id: 2647] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL69367 (AM580)
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
  • This target only has 0 pki data point
  • 0
1 CHEMBL69367_lig_chart_1 Retinoic acid receptor alpha Human
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
  • This target only has 0 pki data point
  • 0
2 CHEMBL69367_lig_chart_2 Retinoic acid receptor beta Human
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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
  • This target only has 0 pki data point
  • 0
3 CHEMBL69367_lig_chart_3 Retinoic acid receptor gamma Human
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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 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 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]