AGN193109 [Ligand Id: 2640] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL358145
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
There should be some charts here, you may need to enable JavaScript!
  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
There should be some charts here, you may need to enable JavaScript!
  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
There should be some charts here, you may need to enable JavaScript!
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 Binding affinity towards retinoic acid receptor alpha was determined using [3H]ATRA (5 nM) as radioligand B 7.77 pKd 17 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
ChEMBL Ability to displace 3[H](all-E)-retinoic acid (5 nM) from alpha retinoic acid receptor (alpha RAR) using transactivation assay B 7.8 pKd 16 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 573-576 [PMID:10098666]
ChEMBL Binding constant for baculovirus-expressed Retinoic acid receptor RAR alpha B 8.7 pKd 2 nM Kd J. Med. Chem. (1995) 38: 4764-4767 [PMID:7490725]
ChEMBL Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor alpha F 7.51 pIC50 31 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
GtoPdb - - 8.7 pIC50 - - - J Biol Chem (1996) 271: 22692-6 [PMID:8798442];
J Biol Chem (2000) 275: 19401-8 [PMID:10777502];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Binding affinity towards retinoic acid receptor beta was determined using [3H]ATRA (5 nM) as radioligand B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
ChEMBL Ability to displace 3[H](all-E)-retinoic acid (5 nM) from beta retinoic acid receptor (beta RAR) using transactivation assay B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 573-576 [PMID:10098666]
ChEMBL Binding constant for baculovirus-expressed Retinoic acid receptor RAR beta B 8.7 pKd 2 nM Kd J. Med. Chem. (1995) 38: 4764-4767 [PMID:7490725]
ChEMBL Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor beta F 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
GtoPdb - - 8.7 pIC50 - - - J Biol Chem (1996) 271: 22692-6 [PMID:8798442];
J Biol Chem (2000) 275: 19401-8 [PMID:10777502];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Ability to displace 3[H](all-E)-retinoic acid (5 nM) from Retinoic acid receptor gamma using transactivation assay B 8.15 pKd 7 nM Kd Bioorg. Med. Chem. Lett. (1999) 9: 573-576 [PMID:10098666]
ChEMBL Binding affinity towards retinoic acid receptor gamma was determined using [3H]ATRA (5 nM) as radioligand B 8.22 pKd 6 nM Kd Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]
ChEMBL Binding constant for baculovirus-expressed Retinoic acid receptor RAR gamma B 8.52 pKd 3 nM Kd J. Med. Chem. (1995) 38: 4764-4767 [PMID:7490725]
GtoPdb - - 8.5 pIC50 - - - J Biol Chem (1996) 271: 22692-6 [PMID:8798442];
J Biol Chem (2000) 275: 19401-8 [PMID:10777502];
Curr Pharm Des (2000) 6: 25-58 [PMID:10637371]
ChEMBL Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor gamma F 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 765-768 [PMID:11277515]

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]