chlordiazepoxide [Ligand Id: 3370] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL451 (A-Poxide, Chlordiazachel, Chlordiazepoxide, Chlordiazepoxide civ, Clopoxide, Librelease, Libritabs, Librium, Lygen, Sarlib, Trakipeal, Zeisin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404, 414, 412] [UniProtKB: P14867, P18507, P28472] | ||||||||
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-1-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes | B | 6.11 | pKi | 770 | nM | Ki | J Med Chem (2004) 47: 2176-2179 [PMID:15084116] |
| ChEMBL | Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 | B | 6.22 | pKi | 605 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2871-2875 [PMID:15125950] |
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-1-beta-3-gamma-2 expressed in L(tk-) cells | B | 6.22 | pKi | 605 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-1-beta-3-gamma-2) stably expressed in L(tk-) cells. | B | 6.25 | pKi | 560 | nM | Ki | J Med Chem (2002) 45: 1887-1900 [PMID:11960500] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414, 412, 405] [UniProtKB: P18507, P28472, P47869] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 stably expressed in L(tk-) cells | B | 6.34 | pKi | 460 | nM | Ki | J Med Chem (2002) 45: 1887-1900 [PMID:11960500] |
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-2-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes | B | 6.34 | pKi | 460 | nM | Ki | J Med Chem (2004) 47: 2176-2179 [PMID:15084116] |
| ChEMBL | Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 | B | 6.41 | pKi | 392 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2871-2875 [PMID:15125950] |
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-) cells | B | 6.41 | pKi | 392 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414, 412, 406] [UniProtKB: P18507, P28472, P34903] | ||||||||
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-3-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes | B | 6.13 | pKi | 740 | nM | Ki | J Med Chem (2004) 47: 2176-2179 [PMID:15084116] |
| ChEMBL | Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 | B | 6.33 | pKi | 471 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2871-2875 [PMID:15125950] |
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-) cells | B | 6.33 | pKi | 471 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
| ChEMBL | Binding affinity by displacement of [3H]Ro-151788 from recombinant human gamma-aminobutyric-acid A receptor alpha3,beta3,gamma2 stably expressed in L cells | B | 6.56 | pKi | 275 | nM | Ki | J Med Chem (2002) 45: 1887-1900 [PMID:11960500] |
| GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414, 412, 408] [UniProtKB: P18507, P28472, P31644] | ||||||||
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human GABA-A alpha-5-beta-3-gamma-2 receptor subunits expressed in Xenopus oocytes | B | 6.28 | pKi | 520 | nM | Ki | J Med Chem (2004) 47: 2176-2179 [PMID:15084116] |
| ChEMBL | Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 | B | 6.43 | pKi | 368 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 2871-2875 [PMID:15125950] |
| ChEMBL | Displacement of [3H]-Ro- 15-1788 from human gamma-aminobutyric-acid GABA-A receptor alpha-5-beta-3-gamma-2 expressed in L(tk-) cells | B | 6.43 | pKi | 368 | nM | Ki | J Med Chem (2004) 47: 5829-5832 [PMID:15537339] |
| ChEMBL | Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-5-beta-3-gamma-2) stably expressed in L(tk-) cells. | B | 6.49 | pKi | 320 | nM | Ki | J Med Chem (2002) 45: 1887-1900 [PMID:11960500] |
| GABA-A receptor; anion channel in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094107] [UniProtKB: P08219, P08220, P10063, P10064, P20237, P22300] | ||||||||
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A central Benzodiazepine receptor of bovine brain membranes | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (1985) 28: 506-509 [PMID:2984422] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to benzodiazepine receptor in bovine brain membrane | B | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (1988) 31: 1-3 [PMID:2826782] |
| 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]flunitrazepam from GABA-A benzodiazepine receptor in synaptic membranes of rat cerebral cortex | B | 6.04 | pIC50 | 910 | nM | IC50 | J Med Chem (1985) 28: 683-685 [PMID:2985787] |
| ChEMBL | Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cerebral cortex membrane | B | 6.15 | pIC50 | 710 | nM | IC50 | J Med Chem (1991) 34: 2993-3006 [PMID:1681105] |
| ChEMBL | Inhibition of binding of tritiated 3[H]diazepam radioligand to rat brain homogenates | B | 6.35 | pIC50 | 442 | nM | IC50 | J Med Chem (1983) 26: 845-850 [PMID:6304314] |
| ChEMBL | Inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortex | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (1989) 32: 2561-2573 [PMID:2573731] |
| ChEMBL | In vitro for inhibition of [3H]diazepam towards Benzodiazepine receptor from rat | B | 6.61 | pIC50 | 248 | nM | IC50 | J Med Chem (1981) 24: 592-600 [PMID:6113284] |
| ChEMBL | Inhibition of specific binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptors | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1990) 33: 196-202 [PMID:1967311] |
| ChEMBL | Concentration that inhibits binding of 1.5 nM [3H]diazepam to rat brain benzodiazepine receptor | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1989) 32: 1020-1024 [PMID:2540330] |
| ChEMBL | Inhibitory concentration against specific binding of [3H]diazepam to Benzodiazepine receptor in rat brain | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1990) 33: 1910-1914 [PMID:2163452] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 6.68 | pKi | 208 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) | B | 5.75 | pIC50 | 1795 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
| ChEMBL | Binding affinity against rat benzodiazepine (BZD) receptor | B | 6.36 | pKi | 438 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3219-3222 [PMID:12372538] |
| TRH1 receptor in Mouse [GtoPdb: 363] [UniProtKB: P21761] | ||||||||
| GtoPdb | - | - | 4.7 | pKi | 20000 | nM | Ki | Proc Natl Acad Sci USA (1990) 87: 9514-8 [PMID:2175902] |
| TRH1 receptor in Rat [GtoPdb: 363] [UniProtKB: Q01717] | ||||||||
| GtoPdb | - | - | 4.82 | pKi | 15000 | nM | Ki | Ann N Y Acad Sci (1989) 553: 197-204 [PMID:2566295] |
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]
