LG100754 [Ligand Id: 2814] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL109581
  • 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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  • 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
Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha B 5.75 pKi 1791 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL Transcriptional activation of Retinoic acid receptor RAR alpha B 8.4 pEC50 4 nM EC50 J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta B 5.59 pKi 2587 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL Transcriptional activation of Retinoic acid receptor RAR beta B 8 pEC50 10 nM EC50 J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma B 5.22 pKi 6094 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL Transcriptional activation of Retinoic acid receptor RAR gamma B 6.72 pEC50 192 nM EC50 J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Inhibition of [3H]targretin binding to Retinoid X receptor RXR alpha B 8.1 pKi 8 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
GtoPdb - - 8.5 pIC50 - - - Mol Endocrinol (2001) 15: 1360-9 [PMID:11463859]
ChEMBL Transcriptional ativation of Retinoid X receptor RXR alpha B 8.7 pEC50 2 nM EC50 J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR beta B 8.05 pKi 9 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
GtoPdb - - 8 pIC50 - - - Mol Endocrinol (2001) 15: 1360-9 [PMID:11463859];
J Biol Chem (2002) 277: 12503-6 [PMID:11877384];
Nature (1996) 383: 450-3 [PMID:8837780]
ChEMBL Transcriptional activation of Retinoid X receptor RXR beta B 7.89 pEC50 13 nM EC50 J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL Inhibition of [3H]targretin binding to Retinoid X receptor RXR gamma B 7.85 pKi 14 nM Ki J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]
ChEMBL Transcriptional activation of Retinoid X receptor RXR gamma B 8.4 pEC50 4 nM EC50 J. Med. Chem. (1996) 39: 3229-3234 [PMID:8765503]

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]