chlordiazepoxide [Ligand Id: 3370] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL451 (Trakipeal, Chlordiazepoxide, Librium, Clopoxide, Chlordiazepoxide civ, A-Poxide, Chlordiazachel, Lygen, Libritabs, Librelease, Sarlib, Zeisin)
  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404414412] [UniProtKB: P14867P18507P28472]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414412406] [UniProtKB: P18507P28472P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414412408] [UniProtKB: P18507P28472P31644]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • Translocator protein/Peripheral-type benzodiazepine receptor in Rat [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
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  • TRH1 receptor in Mouse [GtoPdb: 363] [UniProtKB: P21761]
  • TRH1 receptor in Rat [GtoPdb: 363] [UniProtKB: Q01717]
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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: 404414412] [UniProtKB: P14867P18507P28472]
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: 414412405] [UniProtKB: P18507P28472P47869]
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: 414412406] [UniProtKB: P18507P28472P34903]
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: 414412408] [UniProtKB: P18507P28472P31644]
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: P08219P08220P10063P10064P20237P22300]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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. U.S.A. (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 27:

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]