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Assay Detail

CHEMBL4731052

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity pig brain GABA-AT assessed as inactivation constant using GABA as substrate in presence of NADP+ and alpha-ketoglutarate by SSDH coupled enzyme based UV-Vis spectrophotometry
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

4-aminobutyrate aminotransferase, mitochondrial (CHEMBL2266)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Mechanism-Based Design of 3-Amino-4-Halocyclopentenecarboxylic Acids as Inactivators of GABA Aminotransferase.
Shen S,Doubleday PF,Weerawarna PM,Zhu W,Kelleher NL,Silverman RB
ACS Med Chem Lett (2020) 11 : 1949 -1955
PubMed 33062178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 4.52 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746439 1 5.00
CHEMBL4747359 1 4.58
CHEMBL163117 1 4.28
CHEMBL146927 CPP-115 FREE BASE 1.0 1 4.23
CHEMBL4758952 1 -
CHEMBL4741430 1 -
CHEMBL89598 VIGABATRIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746439 Ki = 10000.0 nM 5.00
CHEMBL4747359 Ki = 26000.0 nM 4.58
CHEMBL163117 Ki = 53000.0 nM 4.28
CHEMBL146927 CPP-115 FREE BASE Ki = 59000.0 nM 4.23
CHEMBL4758952 Ki = 6010000.0 nM -
CHEMBL4741430 Ki = 14260000.0 nM -
CHEMBL89598 VIGABATRIN Ki = 290000.0 nM -