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

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ChEMBL ligand: CHEMBL1657 (AGN 190168, AGN-190168, Arazlo, Avage, Fabior, Idp-123, Tazarotene, Tazorac, 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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]