gabazine [Ligand Id: 4197] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL32503 (Gabazine)
  • 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: 404414411] [UniProtKB: P14867P18507P47870]
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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]
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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: 414408412] [UniProtKB: P18508P19969P63079]
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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 γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
ChEMBL Antagonist activity at human recombinant GABA A receptor alpha1beta2gamma2S expressed in HEK293 cells assessed as inhibition of GABA-induced current by patch clamp electrophysiology F 6.46 pIC50 349 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4252-4254 [PMID:21664131]
ChEMBL Antagonist activity at human alpha1beta2gamma2S GABA-A receptor expressed in tsA201 cells assessed as inhibition of GABA-induced effect after 30 mins by FLIPR membrane potential blue assay B 6.62 pIC50 240 nM IC50 J. Med. Chem. (2013) 56: 6536-6540 [PMID:23855889]
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 at human GABAA alpha-1-beta-3-gamma-2S expressed in Xenopus oocytes by voltage-clamp electrophysiology F 6.62 pKi 240 nM Ki J. Med. Chem. (2006) 49: 1388-1396 [PMID:16480274]
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: 414408412] [UniProtKB: P18508P19969P63079]
ChEMBL Displacement of [3H]muscimol from GABAA alpha-1-beta-3-gamma-2S in rat brain membrane B 7.13 pKi 74 nM Ki J. Med. Chem. (2006) 49: 1388-1396 [PMID:16480274]
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 in vivo for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]-GABA agonist from rat brain preparations after iv injection. B 6.85 pIC50 140 nM IC50 J. Med. Chem. (1992) 35: 4092-4097 [PMID:1331456]
ChEMBL Affinity for gamma-aminobutyric-acid A receptor measured by its ability to displace [3H]gabazine antagonist from rat brain preparations. F 8.1 pIC50 8 nM IC50 J. Med. Chem. (1992) 35: 4092-4097 [PMID:1331456]
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 In vitro inhibition of [3H]muscimol to rat brain synaptic membranes B 7.13 pKi 74 nM Ki J. Med. Chem. (2000) 43: 4930-4933 [PMID:11150163]
ChEMBL Inhibition of Gamma-aminobutyric acid A (GABA-A) receptor in vitro by whole-cell patch-clamp recording in cultured cerebral cortical neurones F 6.62 pIC50 240 nM IC50 J. Med. Chem. (2000) 43: 4930-4933 [PMID:11150163]

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]