tazarotene [Ligand Id: 6952] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1657 (Arazlo, AGN-190168, AGN 190168, Tazorac, Tazarotene, Fabior, Avage, Zorac)
  • 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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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
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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]
GtoPdb - - 7.2 pEC50 63 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 7.2 pEC50 63 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 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 9.1 pEC50 0.8 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 489-492 [PMID:19058965]
GtoPdb - - 9.1 pEC50 0.8 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 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 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 489-492 [PMID:19058965]
GtoPdb - - 7.4 pEC50 40 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]