vigabatrin [Ligand Id: 4821] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL89598 (5-hexenoic acid, 4-amino-, CPP-109, Gamma vinyl gaba, Gamma-vinyl gaba, MDL 71,754, MDL-71754, RMI-71754, Sabril, Vigabatrin, Vinyl gamma-aminobutyric acid)
  • 4-aminobutyrate aminotransferase in Human [GtoPdb: 2464] [UniProtKB: P80404]
  • 4-aminobutyrate aminotransferase/4-aminobutyrate aminotransferase, mitochondrial in Mouse [ChEMBL: CHEMBL4523258] [GtoPdb: 2464] [UniProtKB: P61922]
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  • 4-aminobutyrate aminotransferase in Human [GtoPdb: 2464] [UniProtKB: P80404]
  • 4-aminobutyrate aminotransferase/Gamma-amino-N-butyrate transaminase in Rat [ChEMBL: CHEMBL3148] [GtoPdb: 2464] [UniProtKB: P50554]
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  • Vesicular inhibitory amino acid transporter in Human [GtoPdb: 1133] [UniProtKB: Q9H598]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
4-aminobutyrate aminotransferase in Human [GtoPdb: 2464] [UniProtKB: P80404]
GtoPdb - - 3.07 pKi 850000 nM Ki Eur J Biochem (1977) 74: 441-5 [PMID:856582];
J Med Chem (2012) 55: 567-75 [PMID:22168767]
4-aminobutyrate aminotransferase/4-aminobutyrate aminotransferase, mitochondrial in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523258] [GtoPdb: 2464] [UniProtKB: P61922]
ChEMBL Inhibition of GABA aminotransferase in mouse brain homogenates using GABA and alpha-ketoglutarate as substrates preincubated for 30 mins followed by beta-NADP addition and measured for 20 mins by spectrophotometric method B 4.4 pIC50 39720 nM IC50 Bioorg Med Chem Lett (2019) 29: 1825-1830 [PMID:31084949]
4-aminobutyrate aminotransferase in Human [GtoPdb: 2464] [UniProtKB: P80404]
GtoPdb - - 3.07 pKi 850000 nM Ki Eur J Biochem (1977) 74: 441-5 [PMID:856582];
J Med Chem (2012) 55: 567-75 [PMID:22168767]
4-aminobutyrate aminotransferase/Gamma-amino-N-butyrate transaminase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3148] [GtoPdb: 2464] [UniProtKB: P50554]
ChEMBL Inhibition of Rattus norvegicus (rat) brain gamma-amino butyrate aminotransferase using gamma-amino butyrate as substrate assessed as decrease in NADPH generation after 30 min by spectrophotometric analysis B 4.38 pIC50 41210 nM IC50 Med Chem Res (2013) 22: 134-146
Vesicular inhibitory amino acid transporter in Human [GtoPdb: 1133] [UniProtKB: Q9H598]
GtoPdb - - 2.1 pIC50 7500000 nM IC50 Nature (1997) 389: 870-6 [PMID:9349821]

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]