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ChEMBL ligand: CHEMBL312443 (Gaboxadol, LU 02-030, LU-02-030, LU-02030, MK-0928, NSC-759585) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]