flumazenil [Ligand Id: 4192] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL407 (Anexate, Flumazenil, Flumazepil, Lanexat, Mazicon, NSC-759193, RO-15-1788, RO-151788, RO 15-1788/000, RO-151788000, RO-1722, RO-41-8157, Romazicon) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit in Human [GtoPdb: 414, 404, 411] [UniProtKB: P18507, P14867, P47870] | ||||||||
| GtoPdb | Affinity measured using α1β3γ2 receptors. | - | 9.1 | pKi | 0.8 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| 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 | 6.97 | pKi | 106 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| ChEMBL | Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 9.3 | pKi | 0.5 | 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 against alpha-1-beta-3-gamma-2 GABAA/BzR receptor subtype. | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1998) 41: 4130-4142 [PMID:9767648] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Affinity measured using α1β3γ2 receptors. | - | 9.1 | pKi | 0.8 | nM | Ki | 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] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-2-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 8.24 | pKi | 5.7 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GtoPdb | Affinity measured using α2β3γ2 receptors. | - | 9.05 | pKi | 0.9 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| 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 | Binding affinity tested against alpha-2-beta-3-gamma-2 GABAA/BzR receptor subtype. | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1998) 41: 4130-4142 [PMID:9767648] |
| ChEMBL | Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Affinity measured using α2β3γ2 receptors. | - | 9.05 | pKi | 0.9 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| 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] | ||||||||
| ChEMBL | Displacement of [3H]Ro-151788 from benzodiazepine binding site of GABAA alpha-3-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 8.09 | pKi | 8.1 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GtoPdb | Affinity measured using α3β3γ2 receptors. | - | 8.98 | pKi | 1.05 | nM | Ki |
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]; Eur J Pharmacol (2010) 636: 18-27 [PMID:20303942] |
| 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 | Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1994) 37: 4576-4580 [PMID:7799410] |
| 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 | Binding affinity to human GABAA alpha3beta2gamma2 expressed in thymidine kinase-deficient L cells | B | 9.35 | pKd | 0.45 | nM | Kd | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| ChEMBL | Binding affinity against alpha-3-beta-3-gamma-2 GABAA/BzR receptor subtype. | B | 8.98 | pKi | 1.05 | nM | Ki | J Med Chem (1998) 41: 4130-4142 [PMID:9767648] |
| GtoPdb | Affinity measured using α3β3γ2 receptors. | - | 8.98 | pKi | 1.05 | nM | Ki |
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]; Eur J Pharmacol (2010) 636: 18-27 [PMID:20303942] |
| 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] | ||||||||
| GtoPdb | Affinity measured using α5β3γ2 receptors. | - | 9.22 | pKi | 0.6 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| ChEMBL | Binding affinity for Gamma-aminobutyric acid A receptor alpha-5-beta-3-gamma-2 | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1998) 41: 4130-4142 [PMID:9767648] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2 | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit in Human [GtoPdb: 414, 409, 411] [UniProtKB: P18507, Q16445, P47870] | ||||||||
| GtoPdb | Affinity measured using α6β3γ2 receptors. | - | 6.83 | pKi | 148 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| 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 | 7.05 | pKi | 90 | 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 | 7.48 | pKi | 33 | 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 | 7.77 | pKi | 17 | 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 | 7.77 | pKi | 17 | 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 | 7.82 | pKi | 15 | 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 against Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2 | B | 6.83 | pKi | 148 | nM | Ki | J Med Chem (1998) 41: 4130-4142 [PMID:9767648] |
| ChEMBL | Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-6-beta-3-gamma-2 | B | 6.83 | pKi | 148 | nM | Ki | J Med Chem (2000) 43: 71-95 [PMID:10633039] |
| GtoPdb | Affinity measured using α6β3γ2 receptors. | - | 6.83 | pKi | 148 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| 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: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| GtoPdb | Affinity measured using α6β3γ2 receptors. | - | 6.83 | pKi | 148 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| GtoPdb | Affinity measured using α3β3γ2 receptors. | - | 8.98 | pKi | 1.05 | nM | Ki |
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]; Eur J Pharmacol (2010) 636: 18-27 [PMID:20303942] |
| ChEMBL | Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2002) 45: 5710-5720 [PMID:12477354] |
| ChEMBL | Displacement of [3H]flumazenil from bovine benzodiazepine receptor GABA-A channel of brain membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2005) 48: 2936-2943 [PMID:15828832] |
| GtoPdb | Affinity measured using α2β3γ2 receptors. | - | 9.05 | pKi | 0.9 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| GtoPdb | Affinity measured using α1β3γ2 receptors. | - | 9.1 | pKi | 0.8 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| GtoPdb | Affinity measured using α5β3γ2 receptors. | - | 9.22 | pKi | 0.6 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| GABA-A receptor; anion channel in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094107] [UniProtKB: P08219, P08220, P10063, P10064, P20237, P22300] | ||||||||
| ChEMBL | In vitro inhibition of [3H]-Ro- 15-1788 binding to GABA-A Benzodiazepine receptor of bovine brain membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1998) 41: 3821-3830 [PMID:9748357] |
| ChEMBL | Inhibition of [3H]flumazenil binding to GABA-A benzodiazepine receptor of bovine brain membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2001) 44: 2286-2297 [PMID:11428922] |
| ChEMBL | Displacement of [3H]flumazenil from GABA-A receptor in bovine brain membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2006) 49: 2489-2495 [PMID:16610792] |
| ChEMBL | In vitro inhibition of [3H]flunitrazepam binding to GABA-A benzodiazepine receptor of bovine cerebral cortical membranes at 10 uM | B | 9.42 | pKi | 0.38 | nM | Ki | J Med Chem (1992) 35: 2214-2220 [PMID:1319492] |
| ChEMBL | Displacement of [3H]- Ro.15-1788 from GABA-A central Benzodiazepine receptor (BzR) of Bovine cerebral cortex membrane | B | 10.05 | pKi | 0.09 | nM | Ki | J Med Chem (2000) 43: 96-102 [PMID:10633040] |
| ChEMBL | Affinity to displace [3H]flunitrazepam from Benzodiazepine receptor in bovine brain membrane | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (1990) 33: 2646-2651 [PMID:2167984] |
| 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] | ||||||||
| GtoPdb | Antagonism of complexes containing α4β2γ2 subunits heterologously expressed in vitro. | - | 7.03 | pKi | 94 | nM | Ki | J Med Chem (1994) 37: 4576-80 [PMID:7799410] |
| ChEMBL | Binding affinity against Diazepam insensitive (DI) Gamma-aminobutyric acid A receptor | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1995) 38: 1679-1688 [PMID:7752192] |
| ChEMBL | Binding affinity for Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1993) 36: 1001-1006 [PMID:8386769] |
| ChEMBL | Binding affinity for Diazepam insensitive (DI) isoform of the benzodiazepine (Bz) binding site on GABAA receptors | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1993) 36: 1820-1830 [PMID:8390574] |
| ChEMBL | Displacement of [3H]flunitrazepam at GABA-A benzodiazepine receptor in rat brain cortical membranes | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (1996) 39: 2915-2921 [PMID:8709126] |
| ChEMBL | In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand | B | 8.71 | pKi | 1.94 | nM | Ki | J Med Chem (1985) 28: 1314-1319 [PMID:2993620] |
| ChEMBL | In vitro affinity against Benzodiazepine receptor binding to rat cortical membranes (using [3H]- flumazenil as radioligand). | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1999) 42: 4343-4350 [PMID:10543878] |
| ChEMBL | Binding affinity for Diazepam sensitive (DS) isoform of the benzodiazepine (Bz) binding site on GABAA receptors | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1993) 36: 1820-1830 [PMID:8390574] |
| ChEMBL | Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1993) 36: 1001-1006 [PMID:8386769] |
| ChEMBL | Binding affinity against Diazepam sensitive (DS) Gamma-aminobutyric acid A receptor in rat cerebellum. | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1995) 38: 1679-1688 [PMID:7752192] |
| ChEMBL | Inhibition of radiolabeled antagonist [3H]-Ro- 15-1788 binding to benzodiazepine receptor from rat cortical membranes | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (1989) 32: 2282-2291 [PMID:2552115] |
| ChEMBL | Agonistic activity against specific binding of radioligand [3H]Ro-151788 to GABA-A Benzodiazepine receptor in rat cortex | B | 8.74 | pIC50 | 1.82 | nM | IC50 | J Med Chem (1993) 36: 1669-1673 [PMID:8388472] |
| GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Binding affinity to GABAA alpha-1-beta-2-gamma-2 receptor | B | 8.7 | pKd | 2 | nM | Kd | J Med Chem (2008) 51: 3788-3803 [PMID:18537233] |
| ChEMBL | Displacement of [3H]Ro15-1788 from benzodiazepine binding site of GABAA alpha-1-beta-2-gamma-2 receptor expressed in HEK293T cells | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GtoPdb | Affinity measured using α1β3γ2 receptors. | - | 9.1 | pKi | 0.8 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| ChEMBL | Binding affinity to GABBA alpha1 (unknown origin) | B | 9.1 | pKi | 0.79 | nM | Ki | J Nat Prod (2021) 84: 713-723 [PMID:32870011] |
| GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4956] [GtoPdb: 405] [UniProtKB: P47869] | ||||||||
| GtoPdb | Affinity measured using α2β3γ2 receptors. | - | 9.05 | pKi | 0.9 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| ChEMBL | Binding affinity to GABBA alpha2 (unknown origin) | B | 9.1 | pKi | 0.79 | nM | Ki | J Nat Prod (2021) 84: 713-723 [PMID:32870011] |
| GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3026] [GtoPdb: 406] [UniProtKB: P34903] | ||||||||
| GtoPdb | Affinity measured using α3β3γ2 receptors. | - | 8.98 | pKi | 1.05 | nM | Ki |
Pharmacol Rev (2018) 70: 836-878 [PMID:30275042]; Eur J Pharmacol (2010) 636: 18-27 [PMID:20303942] |
| ChEMBL | Binding affinity to GABBA alpha3 (unknown origin) | B | 9 | pKi | 1 | nM | Ki | J Nat Prod (2021) 84: 713-723 [PMID:32870011] |
| 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 | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2008) 51: 7243-7252 [PMID:18973287] |
| GABAA receptor α4 subunit in Rat [GtoPdb: 407] [UniProtKB: P28471] | ||||||||
| GtoPdb | Antagonism of complexes containing α4β2γ2 subunits heterologously expressed in vitro. | - | 7.03 | pKi | 94 | nM | Ki | J Med Chem (1994) 37: 4576-80 [PMID:7799410] |
| GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644] | ||||||||
| ChEMBL | Binding affinity to GABAA alpha-5-beta-2-gamma-2 receptor | B | 9.3 | pKd | 0.5 | nM | Kd | J Med Chem (2008) 51: 3788-3803 [PMID:18537233] |
| ChEMBL | Binding affinity to GABBA alpha5 (unknown origin) | B | 9.2 | pKi | 0.63 | nM | Ki | J Nat Prod (2021) 84: 713-723 [PMID:32870011] |
| GtoPdb | Affinity measured using α5β3γ2 receptors. | - | 9.22 | pKi | 0.6 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
| GABAA receptor α6 subunit/GABA receptor alpha-6 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2579] [GtoPdb: 409] [UniProtKB: Q16445] | ||||||||
| ChEMBL | Binding affinity to GABBA alpha6 (unknown origin) | B | 6.8 | pKi | 158.49 | nM | Ki | J Nat Prod (2021) 84: 713-723 [PMID:32870011] |
| GtoPdb | Affinity measured using α6β3γ2 receptors. | - | 6.83 | pKi | 148 | nM | Ki | Pharmacol Rev (2018) 70: 836-878 [PMID:30275042] |
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]
