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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL312443 (Gaboxadol, LU 02-030, LU-02-030, LU-02030, MK-0928, NSC-759585)
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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 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: 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]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: 241, 240] [UniProtKB: O88871, Q9Z0U4]
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 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]