γ-hydroxybutyrate [Ligand Id: 4711] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1342 (.gamma.-hydroxybutyrate, Gamma hydroxybutyrate, Gamma-hydroxybutyrate, Oxybate, Xyrem)
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  • Gamma-hydroxybutyrate receptor in Rat [ChEMBL: CHEMBL3558] [UniProtKB: Q6RY99]
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  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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  • HCA1 receptor in Human [GtoPdb: 311] [UniProtKB: Q9BXC0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.37 pKi 4300 nM Ki J Med Chem (2019) 62: 2798-2813 [PMID:30763084]
Gamma-hydroxybutyrate receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3558] [UniProtKB: Q6RY99]
ChEMBL Displacement of [3H]NCS-382 (16 nM) from GHB receptor of rat cerebrocortical membranes B 4.6 pIC50 25000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3201-3202 [PMID:15927467]
ChEMBL Binding affinity towards [3H]GHB binding site B 5.18 pIC50 6600 nM IC50 J Med Chem (1988) 31: 893-897 [PMID:3361576]
Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
ChEMBL Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting B 1.81 pKi -1.81 mM pKi Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456]
HCA1 receptor in Human [GtoPdb: 311] [UniProtKB: Q9BXC0]
GtoPdb - - 1.82 pEC50 15300000 nM EC50 J Biol Chem (2009) 284: 2811-22 [PMID:19047060]

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]