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Assay Detail

CHEMBL4013206

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

Binding
Inhibition of recombinant human His-tagged KGA S384A mutant expressed in Escherichia coli BL21(DE3)pLysS using glutamine substrate preincubated for 10 mins followed by substrate addition measured after 60 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, Synthesis, and Evaluation of Thiazolidine-2,4-dione Derivatives as a Novel Class of Glutaminase Inhibitors.
Yeh TK, Kuo CC, Lee YZ, Ke YY, Chu KF, Hsu HY, Chang HY, Liu YW, Song JS, Yang CW, Lin LM, Sun M, Wu SH, Kuo PC, Shih C, Chen CT, Tsou LK, Lee SJ.
J Med Chem (2017) 60 : 5599 -5612
PubMed 28609101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.95 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177757 1 7.19
CHEMBL4090687 1 7.11
CHEMBL4074218 1 7.06
CHEMBL4098413 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177757 IC50 = 65.0 nM 7.19
CHEMBL4090687 IC50 = 78.0 nM 7.11
CHEMBL4074218 IC50 = 87.0 nM 7.06
CHEMBL4098413 IC50 = 361.0 nM 6.44