zolpidem [Ligand Id: 4348] 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: 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • GABAA receptor α4 subunit/GABA receptor alpha-4 subunit in Human [ChEMBL: CHEMBL2472] [GtoPdb: 407] [UniProtKB: P48169]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • Translocator protein/Peripheral-type benzodiazepine receptor in Rat [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
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
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];
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]
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];
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]
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];
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]
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];
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]
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];
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]
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 Mol Pharmacol (1993) 43: 970-5 [PMID:8391122]
ChEMBL Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 2 B 6.13 pEC50 737 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-2-beta-2-gamma-2 receptor expressed in HEK293 cells B 6.12 pKi 765 nM Ki J Med Chem (2009) 52: 3723-3734 [PMID:19469479]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha2 receptor expressed in HEK293 cells after 1 hr B 6.81 pKi 156 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: 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 Inhibition of GABAA receptor alpha3 (unknown origin) B 6.4 pKi 400 nM Ki Eur J Med Chem (2019) 181: 111569-111569 [PMID:31404862]
ChEMBL Effective concentration against gamma-aminobutyric acid (GABA) A receptor, alpha 3 B 5.52 pEC50 >3000 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL328] [GtoPdb: 406] [UniProtKB: P20236]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha3 receptor expressed in HEK293 cells after 1 hr B 6.42 pKi 383 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
GABAA receptor α4 subunit/GABA receptor alpha-4 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2472] [GtoPdb: 407] [UniProtKB: P48169]
ChEMBL Displacement of [3H]Ro-154513 from benzodiazepine binding site of GABAA alpha-4-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 α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
ChEMBL Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-5-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]
ChEMBL Effective concentration against Gamma-aminobutyric acid A receptor, alpha 5 B 5.52 pEC50 >3000 nM EC50 J Med Chem (2002) 45: 5043-5051 [PMID:12408715]
GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
ChEMBL Displacement of [3H]RO15-1788 from recombinant rat GABAalpha5 receptor expressed in HEK293 cells after 1 hr B 5 pKi >10000 nM Ki Eur J Med Chem (2017) 126: 298-352 [PMID:27894044]
Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
ChEMBL Displacement of Ro 5-4864 from peripheral (renal cell) Benzodiazepine receptor B 5.33 pIC50 4700 nM IC50 J Med Chem (1997) 40: 3109-3118 [PMID:9301675]

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]