gaboxadol [Ligand Id: 4322] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL312443 (MK-0928, LU-02-030, Gaboxadol, LU 02-030, LU-02030)
  • 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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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 Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 4.85 pEC50 14125.38 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
ChEMBL Agonist activity at human GABAA alpha1beta2gamma2S receptor expressed in TSA201 cells after 1 min by FLIPR assay B 4.85 pEC50 14000 nM EC50 J. Med. Chem. (2013) 56: 993-1006 [PMID:23294161]
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 Displacement of [3H]muscimol from GABAA receptor in rat brain synaptic membranes B 6.8 pKi 160 nM Ki J. Med. Chem. (2006) 49: 4442-4446 [PMID:16821803]
ChEMBL Inhibition against Gamma-aminobutyric acid A (GABA-A) receptor B 6.89 pIC50 130 nM IC50 J. Med. Chem. (2000) 43: 4930-4933 [PMID:11150163]
ChEMBL In vitro affinity for GABA binding sites on purified synaptic membranes from rat brain. B 6.89 pIC50 130 nM IC50 J. Med. Chem. (1983) 26: 895-900 [PMID:6304315]
ChEMBL Inhibition of [3H]-GABA binding to GABA-A receptor in rat cerebral cortex homogenates B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (1991) 1: 247-248
ChEMBL Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex B 7.04 pIC50 92 nM IC50 J. Med. Chem. (1995) 38: 3287-3296 [PMID:7650683]
ChEMBL Displacement of [3H]- muscimol in cerebral tissue of male rats B 7.5 pIC50 31.5 nM IC50 J. Med. Chem. (1985) 28: 1109-1111 [PMID:2991521]
GABAB2/GABAB1/GABA B receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111474] [GtoPdb: 241240] [UniProtKB: O88871Q9Z0U4]
ChEMBL Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1995) 38: 3287-3296 [PMID:7650683]

ChEMBL data shown on this page come from version 28:

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]