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Assay Detail

CHEMBL3223676

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

Binding
Inhibition of recombinant human pancreatic glucokinase by G-6-P dehydrogenase assay
17
Total Activities
17
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

Property based optimisation of glucokinase activators discovery of the phase IIb clinical candidate AZD1656
Waring MJ, Clarke DS, Fenwick MD, Godfrey L, Groombridge SD, Johnstone C, McKerrecher D, Pike KG, Rayner JW, Robb GR, Wilson I
Medchemcomm (2012) 3 : 1077 -1081
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.22 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217925 1 7.52
CHEMBL3219105 1 7.51
CHEMBL3219108 1 7.50
CHEMBL3219109 1 7.46
CHEMBL3219121 1 7.44
CHEMBL3219115 1 7.43
CHEMBL3219119 1 7.33
CHEMBL3219107 1 7.28
CHEMBL3219123 1 7.22
CHEMBL3219124 AZD-1656 2.0 1 7.21
CHEMBL3219110 1 7.21
CHEMBL3219117 1 7.16
CHEMBL3219120 1 7.14
CHEMBL3219106 1 7.14
CHEMBL3219116 1 6.96
CHEMBL3219118 1 6.77
CHEMBL3219122 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217925 EC50 = 30.0 nM 7.52
CHEMBL3219105 EC50 = 31.0 nM 7.51
CHEMBL3219108 EC50 = 32.0 nM 7.50
CHEMBL3219109 EC50 = 35.0 nM 7.46
CHEMBL3219121 EC50 = 36.0 nM 7.44
CHEMBL3219115 EC50 = 37.0 nM 7.43
CHEMBL3219119 EC50 = 47.0 nM 7.33
CHEMBL3219107 EC50 = 53.0 nM 7.28
CHEMBL3219123 EC50 = 60.0 nM 7.22
CHEMBL3219124 AZD-1656 EC50 = 61.0 nM 7.21
CHEMBL3219110 EC50 = 61.0 nM 7.21
CHEMBL3219117 EC50 = 70.0 nM 7.16
CHEMBL3219120 EC50 = 73.0 nM 7.14
CHEMBL3219106 EC50 = 73.0 nM 7.14
CHEMBL3219116 EC50 = 110.0 nM 6.96
CHEMBL3219118 EC50 = 170.0 nM 6.77
CHEMBL3219122 EC50 = 370.0 nM 6.43