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]
Created with Highcharts 10.3.3ValuesChart context menuRetinoic acid receptor alphapKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
Created with Highcharts 10.3.3ValuesChart context menuRetinoic acid receptor betapKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
Created with Highcharts 10.3.3ValuesChart context menuRetinoic acid receptor gammapKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
Created with Highcharts 10.3.3ValuesChart context menuRetinoid X receptor alphapKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
Created with Highcharts 10.3.3ValuesChart context menuRetinoid X receptor betapKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
Created with Highcharts 10.3.3ValuesChart context menuRetinoid X receptor gammapKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
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 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]