HX 531 [Ligand Id: 8079] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL326525
  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
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  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
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  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Antagonist activity at human RXRalpha expressed in EK293 cells assessed as inhibition of LG-100268-induced transactivation F 5.92 pIC50 1200 nM IC50 Bioorg Med Chem Lett (2007) 17: 4808-4811 [PMID:17651969]
ChEMBL Antagonist activity at human RXRalpha expressed in EK293 cells assessed as inhibition of 9-cis-retinoic acid-induced transactivation F 6.05 pIC50 900 nM IC50 Bioorg Med Chem Lett (2007) 17: 4808-4811 [PMID:17651969]
GtoPdb Measuring inhibition of agonist-induced activation of RXRα. - 6.05 pIC50 900 nM IC50 Bioorg Med Chem Lett (2007) 17: 4808-11 [PMID:17651969]
ChEMBL Antagonist activity at RXRalpha expressed in african green monkey COS1 cells assessed as inhibition of LGD-1069-induced agonist activity F 6.54 pIC50 290 nM IC50 Bioorg Med Chem Lett (2009) 19: 1001-1003 [PMID:19095448]
ChEMBL Antagonist activity at RXRalpha (unknown origin) B 6 pEC50 1000 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL Antagonist activity at RXRbeta expressed in african green monkey COS1 cells assessed as inhibition of LGD-1069-induced agonist activity F 7.36 pIC50 44 nM IC50 Bioorg Med Chem Lett (2009) 19: 1001-1003 [PMID:19095448]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL Antagonist activity at RXRgamma expressed in african green monkey COS1 cells assessed as inhibition of LGD-1069-induced agonist activity F 6.42 pIC50 380 nM IC50 Bioorg Med Chem Lett (2009) 19: 1001-1003 [PMID:19095448]

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]