clonazepam [Ligand Id: 6963] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL452 (Clonazepam, Clonazepam civ, Klonopin, Klonopin rapidly disintegrating, NSC-179913, Ravotril, Rivatril, Rivotril, RO 5-4023, RO-5-4023, RO-54023) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551] | ||||||||
| ChEMBL | Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1988) 31: 2235-2246 [PMID:2848124] |
| Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931] | ||||||||
| ChEMBL | Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1987) 30: 1229-1239 [PMID:2885419] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α3β1γ2. | - | 8.7 | pKi | 2 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α2β1γ2. | - | 8.77 | pKi | 1.7 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| GtoPdb | Assay using recombinant GABAA channels with subunit composition; α1β1γ2. | - | 8.9 | pKi | 1.27 | nM | Ki | Science (1989) 245: 1389-92 [PMID:2551039] |
| ChEMBL | Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2005) 48: 2936-2943 [PMID:15828832] |
| GABA-A receptor; anion channel in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094107] [UniProtKB: P08219, P08220, P10063, P10064, P20237, P22300] | ||||||||
| ChEMBL | In vitro inhibition of [3H]-Ro- 15-1788 binding to GABA-A Benzodiazepine receptor of bovine brain membranes | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (1998) 41: 3821-3830 [PMID:9748357] |
| ChEMBL | Inhibition of [3H]- flumazenil binding to benzodiazepine receptor in bovine brain membranes | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2001) 44: 2286-2297 [PMID:11428922] |
| ChEMBL | Displacement of [3H]- Ro.15-1788 from GABA-A central Benzodiazepine receptor (BzR) of Bovine cerebral cortex membrane | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2000) 43: 96-102 [PMID:10633040] |
| GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14] | ||||||||
| ChEMBL | Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (1987) 30: 1229-1239 [PMID:2885419] |
| ChEMBL | Inhibition of [3H]diazepam binding to GABA-A benzodiazepine receptor of rat brain | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (1988) 31: 2235-2246 [PMID:2848124] |
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]
