zolpidem [Ligand Id: 4348] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL911 (Ambien, Sanval, Zolpidem, Zolpidem civ)
  • GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
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  • 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: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111327] [GtoPdb: 414, 405, 411] [UniProtKB: P18508, P23576, P63138]
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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: 414, 412, 405] [UniProtKB: P18507, P28472, P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138]
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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: 414, 412, 406] [UniProtKB: P18507, P28472, P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat [ChEMBL: CHEMBL2111374] [GtoPdb: 414, 408, 412] [UniProtKB: P18508, P19969, P63079]
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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: 414, 412, 408] [UniProtKB: P18507, P28472, P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111370] [GtoPdb: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445]
  • GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
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  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
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  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903]
  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Rat [ChEMBL: CHEMBL328] [GtoPdb: 406] [UniProtKB: P20236]
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  • GABAA receptor α4 subunit/GABA receptor alpha-4 subunit in Human [ChEMBL: CHEMBL2472] [GtoPdb: 407] [UniProtKB: P48169]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
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  • Translocator protein/Peripheral-type benzodiazepine receptor in Rat [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
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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 β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111392] [GtoPdb: 404, 410, 414] [UniProtKB: P14867, P18505, P18507]
ChEMBL Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells B 7.28 pKi 53 nM Ki J. Med. Chem. (2006) 49: 2526-2533 [PMID:16610795]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 7.68 pKi 20.7 nM Ki Eur J Pharmacol (1995) 291: 301-9 [PMID:8719414];
Eur J Pharmacol (1996) 304: 155-62 [PMID:8813598]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 7.68 pKi 20.7 nM Ki Eur J Pharmacol (1995) 291: 301-9 [PMID:8719414];
Eur J Pharmacol (1996) 304: 155-62 [PMID:8813598]
ChEMBL Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1-beta-2-gamma-2 subunits B 5 pIC50 >=10000 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 2277-2282
ChEMBL Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1-beta-2-gamma-2 subunits B 7.33 pIC50 46.3 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 2277-2282
ChEMBL Positive allosteric modulation of human recombinant GABA-A receptor alpha1beta2gamma2 expressed in HEK293 cells assessed as potentiation of of GABA induced chloride currents treated every 60 secs measured for 7 secs by electrophysiological method B 6.62 pEC50 240 nM EC50 Eur J Med Chem (2016) 124: 456-467 [PMID:27598234]
GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414, 404, 411] [UniProtKB: P18508, P62813, P63138]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2009) 52: 3723-3734 [PMID:19469479]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in HEK293 cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2005) 48: 2936-2943 [PMID:15828832]
ChEMBL Displacement of [3H]flumazenil from rat GABA-Aalpha1 receptor plus beta-2-gamma-2 in HEK293 cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2006) 49: 2489-2495 [PMID:16610792]
ChEMBL Displacement of [3H]flumazenil from rat GABAA alpha-1-beta-2-gamma-2 expressed in HEK293 cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2007) 50: 1627-1634 [PMID:17335185]
ChEMBL Inhibition of [3H]flumazenil specific binding at rat GABA-A alpha-1-beta-2-gamma-2 receptor subunits expressed in HEK293 cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2001) 44: 2286-2297 [PMID:11428922]
ChEMBL Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.57 pKi 26.7 nM Ki J. Med. Chem. (2002) 45: 5710-5720 [PMID:12477354]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.57 pKi 26.7 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
ChEMBL Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.72 pKi 19 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
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 Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells B 7.28 pKi 52.1 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells B 7.57 pKi 27 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.57 pKi 27 nM Ki J. Med. Chem. (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells B 7.57 pKi 27 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-1-beta-3-gamma-2 receptor B 7.57 pKi 26.7 nM Ki J. Med. Chem. (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 7.57 pKi 26.7 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting B 7.57 pKi 26.7 nM Ki Bioorg. Med. Chem. (2010) 18: 7548-7564 [PMID:20888240]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 7.68 pKi 20.7 nM Ki Eur J Pharmacol (1995) 291: 301-9 [PMID:8719414];
Eur J Pharmacol (1996) 304: 155-62 [PMID:8813598]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111413] [GtoPdb: 414, 405, 411] [UniProtKB: P18507, P47869, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 6.12 pKi 760.6 nM Ki Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
ChEMBL Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-2-beta-2-gamma-2 receptor expressed in HEK293T cells B 6.39 pKi 408 nM Ki J. Med. Chem. (2008) 51: 7243-7252 [PMID:18973287]
ChEMBL Potentiation of GABA-evoked Cl- currents in Xenopus oocytes expressing human alpha-2-beta-2-gamma-2 subunits F 6.74 pEC50 180 nM EC50 J. Med. Chem. (1997) 40: 3109-3118 [PMID:9301675]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111327] [GtoPdb: 414, 405, 411] [UniProtKB: P18508, P23576, P63138]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A Gamma-aminobutyric acid A receptor alpha-2-beta-2-gamma-2 expressed in HEK293 cells B 6.12 pKi 765 nM Ki J. Med. Chem. (2005) 48: 2936-2943 [PMID:15828832]
ChEMBL Displacement of [3H]flumazenil from rat GABA-Aalpha2 receptor plus beta-2-gamma-2 in HEK293 cells B 6.12 pKi 765 nM Ki J. Med. Chem. (2006) 49: 2489-2495 [PMID:16610792]
ChEMBL Displacement of [3H]flumazenil from rat GABAA alpha-2-beta-2-gamma-2 expressed in HEK293 cells B 6.12 pKi 765 nM Ki J. Med. Chem. (2007) 50: 1627-1634 [PMID:17335185]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells B 6.81 pKi 156 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
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]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 6.12 pKi 760.6 nM Ki Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
ChEMBL Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells B 6.59 pKi 255.1 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells B 6.8 pKi 160 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells B 6.8 pKi 160 nM Ki J. Med. Chem. (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-2-beta-3-gamma-2 receptor B 6.81 pKi 156 nM Ki J. Med. Chem. (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 B 6.81 pKi 156 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting B 6.81 pKi 156 nM Ki Bioorg. Med. Chem. (2010) 18: 7548-7564 [PMID:20888240]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells B 6.99 pKi 103 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414, 406, 411] [UniProtKB: P18507, P34903, P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 5.67 pKi 2149.5 nM Ki Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
ChEMBL Displacement of [3H]Flumazenil from human GABA-Aalpha3 receptor plus beta-2-gamma-2 expressed in HEK293 cells B 5.73 pKi 1850 nM Ki J. Med. Chem. (2006) 49: 2526-2533 [PMID:16610795]
ChEMBL Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-3-beta-2-gamma-2 receptor expressed in HEK293T cells B 6.01 pKi 975 nM Ki J. Med. Chem. (2008) 51: 7243-7252 [PMID:18973287]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111343] [GtoPdb: 414, 406, 411] [UniProtKB: P18508, P20236, P63138]
ChEMBL Inhibition of [3H]-flumazenil binding to rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 6.12 pKi 765 nM Ki J. Med. Chem. (2001) 44: 2286-2297 [PMID:11428922]
ChEMBL Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 6.4 pKi 400 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 6.42 pKi 383 nM Ki J. Med. Chem. (2002) 45: 5710-5720 [PMID:12477354]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 6.42 pKi 383 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
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]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 5.67 pKi 2149.5 nM Ki Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
ChEMBL Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells B 6.22 pKi 608.5 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 6.42 pKi 383 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing GABA alpha-3-beta-3-gamma-2 receptor B 6.42 pKi 383 nM Ki J. Med. Chem. (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting B 6.42 pKi 383 nM Ki Bioorg. Med. Chem. (2010) 18: 7548-7564 [PMID:20888240]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in L(tk-) cells B 6.42 pKi 380 nM Ki J. Med. Chem. (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells B 6.42 pKi 380 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 subtype expressed in L (tk-) cells B 6.61 pKi 246 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111374] [GtoPdb: 414, 408, 412] [UniProtKB: P18508, P19969, P63079]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells B 7.46 pKi 35 nM Ki J. Med. Chem. (2009) 52: 3723-3734 [PMID:19469479]
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 Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells B 4.82 pKi >15000 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 B 5 pKi >10000 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity towards human alpha-5-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells B 5 pKi >10000 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 B 5 pKi >10000 nM Ki J. Med. Chem. (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-5-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting B 5 pKi >10000 nM Ki Bioorg. Med. Chem. (2010) 18: 7548-7564 [PMID:20888240]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-5-beta-3-gamma-2 subtype expressed in L (tk-) cells B 5.48 pKi >3333 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111370] [GtoPdb: 414, 411, 409] [UniProtKB: P18507, P47870, Q16445]
ChEMBL Displacement of [3H]Ro-154513 from benzodiazepine binding site of GABAA alpha-6-beta-2-gamma-2 receptor expressed in HEK293T cells B 4.82 pKi >15000 nM Ki J. Med. Chem. (2008) 51: 7243-7252 [PMID:18973287]
GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111365] [GtoPdb: 414, 409, 411] [UniProtKB: P18508, P30191, P63138]
ChEMBL Binding affinity for rat GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his)-beta-2-gamma-2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr)beta2gamma2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly,val)beta2gamma2 subunits expressed in HEK293 cells B 5.85 pKi 1400 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-6-(his,thr,gly)beta2gamma2 subunits expressed in HEK293 cells B 6.01 pKi 980 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095190] [GtoPdb: 414, 412, 409] [UniProtKB: P18507, P28472, Q16445]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 B 5 pKi >10000 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Binding affinity measured using LtK- cell membranes expressing Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 B 5 pKi >10000 nM Ki J. Med. Chem. (1998) 41: 2537-2552 [PMID:9651158]
ChEMBL Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-6-beta-3-gamma-2 receptor expressed in HEK cells by liquid scintillation counting B 5 pKi >10000 nM Ki Bioorg. Med. Chem. (2010) 18: 7548-7564 [PMID:20888240]
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 in Human [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O00591, P18505, O14764, P18507, P31644, P34903, Q8N1C3, P47869, P48169, Q99928, Q16445, P14867, P28472, P47870, P78334]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 5.67 pKi 2149.5 nM Ki Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 6.12 pKi 760.6 nM Ki Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 7.68 pKi 20.7 nM Ki Eur J Pharmacol (1995) 291: 301-9 [PMID:8719414];
Eur J Pharmacol (1996) 304: 155-62 [PMID:8813598]
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 Binding affinity was determined by displacement of [3H]flumazenil from rat cortex homogenates F 7.32 pKi 48 nM Ki J. Med. Chem. (2002) 45: 5043-5051 [PMID:12408715]
ChEMBL Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor B 7.6 pKi 25 nM Ki J. Med. Chem. (1994) 37: 758-768 [PMID:8145225]
ChEMBL Displacement of [3H]flunitrazepam from rat brain GABA-A Benzodiazepine receptor B 7.32 pIC50 48 nM IC50 J. Med. Chem. (1997) 40: 3109-3118 [PMID:9301675]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
ChEMBL Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 receptor expressed in HEK293T cells B 7.21 pKi 61.9 nM Ki J. Med. Chem. (2008) 51: 7243-7252 [PMID:18973287]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β3γ2. - 7.68 pKi 20.7 nM Ki Eur J Pharmacol (1995) 291: 301-9 [PMID:8719414];
Eur J Pharmacol (1996) 304: 155-62 [PMID:8813598]
ChEMBL Inhibition of GABAA receptor alpha1 (unknown origin) B 7.7 pKi 20 nM Ki Eur J Med Chem (2019) 181: 111569-111569 [PMID:31404862]
ChEMBL Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1 subunit in spinal cord B 6.89 pIC50 130 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 2277-2282
ChEMBL Inhibition of [3H]flumazenil binding to recombinant GABA-A receptor alpha-1 subunit in cerebellum B 7.85 pIC50 14 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 2277-2282
ChEMBL Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 1 B 6.7 pEC50 198 nM EC50 J. Med. Chem. (2002) 45: 5043-5051 [PMID:12408715]
ChEMBL Activity at rat wild type GABAA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as GABA-elicited response by two electrode voltage clamp method relative to control B 6.72 pEC50 191 nM EC50 J. Biol. Chem. (2007) 282: 26316-26325 [PMID:17626010]
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha1 receptor expressed in HEK293 cells after 1 hr B 7.57 pKi 26.7 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 6.12 pKi 760.6 nM Ki