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 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]
