ALRT 1550 [Ligand Id: 2740] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL89241
  • 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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  • RAR-related orphan receptor-β in Human [GtoPdb: 599] [UniProtKB: Q92753]
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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 7.2 pKi 63.5 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha F 7.19 pEC50 65 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha F 8.4 pEC50 4 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
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 7.05 pKi 90 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta B 9.15 pKi 0.7 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta F 7.62 pEC50 24 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta F 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
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 6.91 pKi 124 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma F 7.8 pEC50 16 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma F 9.47 pEC50 0.34 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha B 6.65 pKi 223 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha B 8.34 pKi 4.6 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR alpha F 6.87 pEC50 134 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR beta B 6.25 pKi 560 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR beta B 7.99 pKi 10.2 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta F 7.06 pEC50 87 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma B 6.49 pKi 320 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma F 7.11 pEC50 77 nM EC50 J. Med. Chem. (1996) 39: 2659-2663 [PMID:8709094]
RAR-related orphan receptor-β in Human [GtoPdb: 599] [UniProtKB: Q92753]
GtoPdb - - 6.8 pKi - - - Nat. Struct. Biol. (2003) 10: 820-5 [PMID:12958591]
GtoPdb - - 10.4 pIC50 - - - Nat. Struct. Biol. (2003) 10: 820-5 [PMID:12958591]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]