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Assay Detail

CHEMBL3369280

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Binding
Competitive inhibition of human GSTA1 activity by double reciprocal Lineweaver-Burk graph
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutathione S-transferase A1 (CHEMBL3409)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,2'-Dihydroxybenzophenones and their carbonyl N-analogues as inhibitor scaffolds for MDR-involved human glutathione transferase isoenzyme A1-1.
Perperopoulou FD, Tsoungas PG, Thireou TN, Rinotas VE, Douni EK, Eliopoulos EE, Labrou NE, Clonis YD.
Bioorg Med Chem (2014) 22 : 3957 -3970
PubMed 25002233 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.11 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3310888 1 6.44
CHEMBL3310887 1 6.42
CHEMBL3310886 1 5.83
CHEMBL3310889 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3310888 Ki = 360.0 nM 6.44
CHEMBL3310887 Ki = 380.0 nM 6.42
CHEMBL3310886 Ki = 1470.0 nM 5.83
CHEMBL3310889 Ki = 1750.0 nM 5.76