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Assay Detail

CHEMBL1167927

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

Binding
Activation of human glucokinase expressed in Escherichia coli BL21(DE3) coexpressing G6PDH by spectrometry
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators.
Li F, Zhu Q, Zhang Y, Feng Y, Leng Y, Zhang A.
Bioorg Med Chem (2010) 18 : 3875 -3884
PubMed 20472448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 6.42 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1165653 1 7.58
CHEMBL205627 1 7.52
CHEMBL499520 1 7.21
CHEMBL1165284 1 7.21
CHEMBL1164790 1 7.10
CHEMBL1164184 1 7.05
CHEMBL1165817 1 6.92
CHEMBL1164578 1 6.80
CHEMBL1165587 1 6.80
CHEMBL1165042 1 6.51
CHEMBL1164519 1 6.50
CHEMBL1164577 1 6.48
CHEMBL1164315 1 6.45
CHEMBL517534 1 6.24
CHEMBL1164323 1 6.14
CHEMBL1164268 1 6.00
CHEMBL1165056 1 5.98
CHEMBL1164508 1 5.93
CHEMBL1164970 1 5.87
CHEMBL519934 1 5.77
CHEMBL1165213 1 5.54
CHEMBL1164579 1 5.54
CHEMBL1165692 1 5.53
CHEMBL1165294 1 5.33
CHEMBL1164726 1 -
CHEMBL1165479 1 -
CHEMBL1164587 1 -
CHEMBL1164586 1 -
CHEMBL1164848 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1165653 EC50 = 26.0 nM 7.58
CHEMBL205627 EC50 = 30.0 nM 7.52
CHEMBL499520 EC50 = 62.0 nM 7.21
CHEMBL1165284 EC50 = 61.0 nM 7.21
CHEMBL1164790 EC50 = 79.0 nM 7.10
CHEMBL1164184 EC50 = 89.0 nM 7.05
CHEMBL1165817 EC50 = 120.0 nM 6.92
CHEMBL1164578 EC50 = 157.0 nM 6.80
CHEMBL1165587 EC50 = 158.0 nM 6.80
CHEMBL1165042 EC50 = 310.0 nM 6.51
CHEMBL1164519 EC50 = 320.0 nM 6.50
CHEMBL1164577 EC50 = 330.0 nM 6.48
CHEMBL1164315 EC50 = 355.0 nM 6.45
CHEMBL517534 EC50 = 570.0 nM 6.24
CHEMBL1164323 EC50 = 724.0 nM 6.14
CHEMBL1164268 EC50 = 1000.0 nM 6.00
CHEMBL1165056 EC50 = 1040.0 nM 5.98
CHEMBL1164508 EC50 = 1180.0 nM 5.93
CHEMBL1164970 EC50 = 1350.0 nM 5.87
CHEMBL519934 EC50 = 1690.0 nM 5.77
CHEMBL1165213 EC50 = 2860.0 nM 5.54
CHEMBL1164579 EC50 = 2860.0 nM 5.54
CHEMBL1165692 EC50 = 2930.0 nM 5.53
CHEMBL1165294 EC50 = 4680.0 nM 5.33
CHEMBL1164726 EC50 - -
CHEMBL1165479 EC50 - -
CHEMBL1164587 EC50 - -
CHEMBL1164586 EC50 - -
CHEMBL1164848 EC50 - -