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Assay Detail

CHEMBL2189066

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

Binding
Uncompetitive inhibition of human kidney glutaminase (124 to 669) assessed as reduction of glutamine hydrolysis by double-reciprocal plot analysis
1
Total Activities
1
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

Glutaminase kidney isoform, mitochondrial (CHEMBL2146302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.
Shukla K, Ferraris DV, Thomas AG, Stathis M, Duvall B, Delahanty G, Alt J, Rais R, Rojas C, Gao P, Xiang Y, Dang CV, Slusher BS, Tsukamoto T.
J Med Chem (2012) 55 : 10551 -10563
PubMed 23151085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.70 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178393 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178393 Ki = 2000.0 nM 5.70