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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
