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Evaluation of Compounds as Inhibitors of GABA-AT from US Patent US10800753: "Tetrahydrothiophene-based GABA aminotransferase inactivators and analogs thereof for treating neurological disorders"
Assay data:7 Tested
SummaryRelated BioAssays by Target
Biochemical assay from US Patent US10189807: "Tetrahydrothiophene-based GABA aminotransferase inactivators"
Binding affinity to pig brain GABA-AT assessed as adduct formation by measuring change in protein mass by LC-MS/MS analysis
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by Target
Substrate activity at pig brain GABA-AT assessed as formation of M7' by measuring molecular weight in presence of PLP by LC-MS/MS analysis
Assay data:1 Tested
Inactivation of pig brain GABA-AT assessed as percentage of compound underwent fluoride ion elimination assessed per inactivation event in presence of varying levels of NaF and 10 uM fluoride ions by fluoride electrode based analytical method
Inactivation of pig brain GABA-AT assessed as number of fluoride ions released per inactivation event in presence of varying levels of NaF and 10 uM fluoride ions by fluoride electrode based analytical method
Substrate activity at pig brain GABA-AT assessed as halide ion elimination by measuring formation of M3' in presence of PLP by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of M6' by measuring molecular weight in presence of PLP by LC-MS/MS analysis
Inactivation of pig brain GABA-AT assessed as partition ratio by measuring number of molecules required for enzyme inactivation
Assay data:2 Tested
Inactivation of pig brain GABA-AT assessed as kinact/Ki ratio using GABA as substrate in presence of NADP+, alpha-ketoglutarate and SSDH by SSDH coupled enzyme based UV-Vis spectrophotometry relative to (1R,3S,4S)-3-amino-4-fluorocyclopentanecarboxylic acid
Irreversible inhibition of pig brain GABA-AT assessed as regeneration of enzyme activity at 10 to 40 equiv measured after 4 days in presence of excess PLP and alpha-ketoglutarate by dialysis method
Potency index, ratio of (1R,3S,4S)-3-amino-4-fluorocyclopentanecarboxylic acid Ki to test compound Ki for binding affinity to pig brain GABA-AT assessed as inhibition constant using GABA as substrate in presence of NADP+, alpha-ketoglutarate by SSDH coupled enzyme based UV-Vis spectrophotometry
Substrate activity at pig brain GABA-AT assessed as formation of (S)-3-((3-hydroxy-2-methyl-5-(phosphonooxymethyl)pyridin-4-yl)methyleneamino)cyclopent-3-enecarboxylic acid by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of (1R,3S)-3-fluoro-4-((3-hydroxy-2-methyl-5-(phosphonooxymethyl)pyridin-4(1H)-ylidene)methylimino)cyclopentanecarboxylic acid by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of M5 in presence of PLP by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of PLP-bound M8 by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of (1R,3S)-3-fluoro-4-oxocyclopentanecarboxylic acid by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of (S)-3-oxocyclopentanecarboxylic acid by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of (S)-3-iminocyclopentanecarboxylic acid by LC-MS/MS analysis
Substrate activity at pig brain GABA-AT assessed as formation of M4 by LC-MS/MS analysis
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