clonazepam [Ligand Id: 6963] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL452 (NSC-179913, RO-54023, Klonopin, Clonazepam civ, Clonazepam, RO 5-4023, RO-5-4023, Rivotril, Klonopin rapidly disintegrating)
  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
  • Cholecystokinin A receptor in Guinea pig [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
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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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
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: P08219P08220P10063P10064P20237P22300]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]