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Assay Detail

CHEMBL4193353

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

Binding
Activation of recombinant human liver glucokinase 2 assessed as assessed as reduction in Km for glucose in presence of 5 mM glucose by G6PDH coupled assay
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

Hexokinase-4 (CHEMBL3820)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation.
Wang Z, Shi X, Zhang H, Yu L, Cheng Y, Zhang H, Zhang H, Zhou J, Chen J, Shen X, Duan W.
Eur J Med Chem (2017) 139 : 128 -152
PubMed 28800453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.90 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205489 1 7.52
CHEMBL4203455 1 7.30
CHEMBL4214183 1 6.82
CHEMBL2165615 NERIGLIATIN 2.0 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205489 EC50 = 30.0 nM 7.52
CHEMBL4203455 EC50 = 50.0 nM 7.30
CHEMBL4214183 EC50 = 150.0 nM 6.82
CHEMBL2165615 NERIGLIATIN EC50 = 1090.0 nM 5.96