AGN194204 [Ligand Id: 2811] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL69091
  • 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]
  • Retinoid X receptor-β in Mouse [GtoPdb: 611] [UniProtKB: P28704]
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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 Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 5.02 pKd 9530 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed retinoic acid receptor RAR-alpha B 5.02 pKd 9500 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 6.25 pKd 556 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor alpha using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor alpha using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
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 baculovirus expressed retinoic acid receptor RAR-beta B 4.69 pKd 20500 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 4.69 pKd 20472 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 6 pKd >1000 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor beta using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor beta using transactivation assay B 6.47 pEC50 340 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 4.8 pKd 15942 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed retinoic acid receptor RAR-gamma B 4.8 pKd 15900 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor B 6 pKd >1000 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor gamma using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor gamma using transactivation assay B 6.7 pEC50 200 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]-9-cis-RA as a radioligand in baculovirus expressed receptor B 6 pKd >1000 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-alpha B 8.82 pKd 1.5 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]-9-cis-RA as a radioligand in baculovirus expressed receptor B 8.82 pKd 1.5 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
GtoPdb - - 9.4 pIC50 - - - J Med Chem (2001) 44: 2298-303 [PMID:11428923]
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor alpha using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor alpha using transactivation assay B 8.82 pEC50 1.5 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor B 6 pKd >1000 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-beta B 8.6 pKd 2.5 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor B 8.6 pKd 2.5 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor beta using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor beta using transactivation assay B 8.7 pEC50 2 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
Retinoid X receptor-β in Mouse [GtoPdb: 611] [UniProtKB: P28704]
GtoPdb - - 8.44 pIC50 - - - J Med Chem (2001) 44: 2298-303 [PMID:11428923]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor B 6 pKd >1000 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-gamma B 8.74 pKd 1.8 nM Kd J. Med. Chem. (2001) 44: 2298-2303 [PMID:11428923]
ChEMBL Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor B 8.74 pKd 1.8 nM Kd Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor gamma using transactivation assay B 6 pEC50 >1000 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218
ChEMBL Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor gamma using transactivation assay B 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 213-218

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]