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: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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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: 404, 414, 412] [UniProtKB: P14867, P18507, P28472]
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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: 414, 408, 412] [UniProtKB: P18508, P19969, P63079]
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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: 404, 414, 411] [UniProtKB: P14867, P18507, P47870]
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]
ChEMBL Antagonist activity at human alpha1beta2gamma2S GABA(A) receptor expressed in human tsA201 cells assessed as inhibition of GABA-induced membrane potential after 16 to 24 hrs by FMP-blue assay B 6.62 pIC50 240 nM IC50 J Med Chem (2019) 62: 2798-2813 [PMID:30763084]
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 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: 414, 408, 412] [UniProtKB: P18508, P19969, P63079]
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: 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]
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: 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 Displacement of [3H]NCS-382 from high-affinity GHB binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting B 4.8 pKi 16000 nM Ki J Med Chem (2019) 62: 2798-2813 [PMID:30763084]
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 Displacement of [3H]muscimol from orthosteric binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting B 7.13 pKi 74 nM Ki J Med Chem (2019) 62: 2798-2813 [PMID:30763084]
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 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]