basmisanil [Ligand Id: 10427] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3681419 (Basmisanil, Rg1662, RG-1662, RG1662, RO-5186582, RO5186582) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Binding affinity to GABA-A alpha1 (unknown origin) | B | 6.01 | pKi | 985 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869] | ||||||||
| ChEMBL | Binding affinity to GABA-A alpha2 (unknown origin) | B | 6.3 | pKi | 502 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903] | ||||||||
| ChEMBL | Binding affinity to GABA-A alpha3 (unknown origin) | B | 6.31 | pKi | 489 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644] | ||||||||
| ChEMBL | Radioligand Binding Assay: Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell memebranes, [3H]flumazenil at a concentration of 1 nM for α1, α2, α3 subunits and 0.5 nM for α5 subunits and the test compound in the range of 10-10−3x10−6 M. Nonspecific binding was defined by 10−5 M diazepam and typically represented less than 5% of the total binding. Assays were incubated to equilibrium for 1 hour at 4 C. and harvested onto GF/C uni-filters (Packard) by filtration using a Packard harvester and washing with ice-cold wash buffer (50 mM Tris; pH 7.5). After drying, filter-retained radioactivity was detected by liquid scintillation counting. | B | 8.33 | pKi | 4.7 | nM | Ki | US-8846719-B2. Isoxazolo-pyridine derivatives (2014) |
| ChEMBL | Binding affinity to GABA-A alpha5 (unknown origin) | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2020) 63: 3425-3446 [PMID:31738537] |
| GtoPdb | Binding affinity determined in a radioligand displacement assay: test compound competition for [3H]flumazenil at α5β3γ2 GABAA channels transiently expressed in HEK293 cells. | - | 8.33 | pKi | 4.7 | nM | Ki | WO2009071476A1. Isoxazolo-pyridine derivatives (2009) |
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]
