AGN193109 [Ligand Id: 2640] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL358145 |
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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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
