[11C]flumazenil [Ligand Id: 4367] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL407 (Flumazepil, RO-1722, Flumazenil, RO-15-1788, RO-151788, Ro-151788000, RO-41-8157, Mazicon, Anexate, Romazicon)
  • 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: 414404411] [UniProtKB: P18508P62813P63138]
1 CHEMBL407_lig_chart_1 GABA-A receptor; alpha-1/beta-2/gamma-2 Rat
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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: 404414412] [UniProtKB: P14867P18507P28472]
2 CHEMBL407_lig_chart_2 GABA-A receptor; alpha-1/beta-3/gamma-2 Human
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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: 414405411] [UniProtKB: P18507P47869P47870]
  • This target only has 1 pki data point
3 CHEMBL407_lig_chart_3 GABA A receptor alpha-2/beta-2/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
4 CHEMBL407_lig_chart_4 GABA-A receptor; alpha-2/beta-3/gamma-2 Human
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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: 414406411] [UniProtKB: P18507P34903P47870]
  • 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: 414406411] [UniProtKB: P18508P20236P63138]
5 CHEMBL407_lig_chart_5 GABA A receptor alpha-3/beta-2/gamma-2 HumanRat
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414412406] [UniProtKB: P18507P28472P34903]
6 CHEMBL407_lig_chart_6 GABA-A receptor; alpha-3/beta-3/gamma-2 Human
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414412408] [UniProtKB: P18507P28472P31644]
7 CHEMBL407_lig_chart_7 GABA-A receptor; alpha-5/beta-3/gamma-2 Human
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  • 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: 414409411] [UniProtKB: P18508P30191P63138]
8 CHEMBL407_lig_chart_8 GABA A receptor alpha-6/beta-2/gamma-2 Rat
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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: 414412409] [UniProtKB: P18507P28472Q16445]
9 CHEMBL407_lig_chart_9 GABA-A receptor; alpha-6/beta-3/gamma-2 Human
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10 CHEMBL407_lig_chart_10 GABA-A receptor; anion channel HumanBovineRat
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • This target only has 1 pki data point
11 CHEMBL407_lig_chart_11 GABA receptor alpha-1 subunit Human
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  • GABAA receptor α4 subunit/GABA receptor alpha-4 subunit in Human [ChEMBL: CHEMBL2472] [GtoPdb: 407] [UniProtKB: P48169]
  • This target only has 1 pki data point
12 CHEMBL407_lig_chart_12 GABA receptor alpha-4 subunit Human
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
  • This target only has 0 pki data point
13 CHEMBL407_lig_chart_13 GABA receptor alpha-5 subunit Human
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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/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414404411] [UniProtKB: P18508P62813P63138]
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: 404414412] [UniProtKB: P14867P18507P28472]
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]
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: 414405411] [UniProtKB: P18507P47869P47870]
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]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
ChEMBL 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]
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: 414406411] [UniProtKB: P18507P34903P47870]
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]
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: 414406411] [UniProtKB: P18508P20236P63138]
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: 414412406] [UniProtKB: P18507P28472P34903]
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]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094122] [GtoPdb: 414412408] [UniProtKB: P18507P28472P31644]
ChEMBL 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/GABA A receptor alpha-6/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111365] [GtoPdb: 414409411] [UniProtKB: P18508P30191P63138]
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: 414412409] [UniProtKB: P18507P28472Q16445]
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]
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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
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]
GABA-A receptor; anion channel in Bovine (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094107] [UniProtKB: P08219P08220P10063P10064P20237P22300]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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]
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 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 data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]