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Assay Detail

CHEMBL3225185

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

Binding
Activation of recombinant human His6-tagged glucokinase by G6PDH-coupled spectrophotometry
23
Total Activities
23
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

N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators
Liu Z, Zhu Q, Li F, Zhang L, Leng Y, Zhang A
Medchemcomm (2011) 2 : 531 -535
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.35 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL499520 1 7.21
CHEMBL1164184 1 7.05
CHEMBL1164578 1 6.80
CHEMBL3218723 1 6.77
CHEMBL3218731 1 6.75
CHEMBL3218727 1 6.68
CHEMBL3218732 1 6.66
CHEMBL3218730 1 6.54
CHEMBL3218726 1 6.52
CHEMBL3218722 1 6.48
CHEMBL3218720 1 6.46
CHEMBL3218719 1 6.35
CHEMBL3218714 1 6.28
CHEMBL3218729 1 6.19
CHEMBL3218728 1 6.10
CHEMBL3218721 1 5.87
CHEMBL3218716 1 5.84
CHEMBL3217766 1 5.82
CHEMBL3218715 1 5.75
CHEMBL3218717 1 4.95
CHEMBL3218718 1 -
CHEMBL3218724 1 -
CHEMBL3218725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL499520 EC50 = 62.0 nM 7.21
CHEMBL1164184 EC50 = 89.0 nM 7.05
CHEMBL1164578 EC50 = 157.0 nM 6.80
CHEMBL3218723 EC50 = 170.0 nM 6.77
CHEMBL3218731 EC50 = 180.0 nM 6.75
CHEMBL3218727 EC50 = 210.0 nM 6.68
CHEMBL3218732 EC50 = 220.0 nM 6.66
CHEMBL3218730 EC50 = 290.0 nM 6.54
CHEMBL3218726 EC50 = 300.0 nM 6.52
CHEMBL3218722 EC50 = 330.0 nM 6.48
CHEMBL3218720 EC50 = 350.0 nM 6.46
CHEMBL3218719 EC50 = 450.0 nM 6.35
CHEMBL3218714 EC50 = 520.0 nM 6.28
CHEMBL3218729 EC50 = 640.0 nM 6.19
CHEMBL3218728 EC50 = 790.0 nM 6.10
CHEMBL3218721 EC50 = 1350.0 nM 5.87
CHEMBL3218716 EC50 = 1440.0 nM 5.84
CHEMBL3217766 EC50 = 1520.0 nM 5.82
CHEMBL3218715 EC50 = 1800.0 nM 5.75
CHEMBL3218717 EC50 = 11350.0 nM 4.95
CHEMBL3218718 EC50 > 20000.0 nM -
CHEMBL3218724 EC50 > 20000.0 nM -
CHEMBL3218725 EC50 > 20000.0 nM -