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, Kigabeq, MDL 71,754, MDL-71754, RMI-71754, Sabril, Vigabatrin, Vigabatrina, Vigabatrine, 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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]