clonazepam [Ligand Id: 6963] 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: CHEMBL452 (Clonazepam, Clonazepam civ, Klonopin, Klonopin rapidly disintegrating, NSC-179913, Ravotril, Rivatril, Rivotril, RO 5-4023, RO-5-4023, RO-54023) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| Peripheral-type benzodiazepine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2419] [UniProtKB: P30535] | ||||||||
| ChEMBL | Binding affinity to bovine brain membrane BzR assessed as inhibition constant | B | 9.07 | pKi | 0.85 | nM | Ki | J Med Chem (2021) 64: 3508-3545 [PMID:33764065] |
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]
