Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3768919

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

Binding
Activation of recombinant human glucokinase assessed as NADPH formation using glucose as substrate incubated for 30 mins in presence of NADP+ and glucose 6-phosphate dehydrogenase
ChEMBL ↗
43
Total Activities
37
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

Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
Paczal A, Bálint B, Wéber C, Szabó ZB, Ondi L, Theret I, De Ceuninck F, Bernard C, Ktorza A, Perron-Sierra F, Kotschy A.
J Med Chem (2016) 59 : 687 -706
PubMed 26685731 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 6.09 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764079 — — 1 7.91
CHEMBL3764668 — — 1 6.94
CHEMBL3764630 — — 1 6.83
CHEMBL3764824 — — 1 6.76
CHEMBL3765780 — — 1 6.71
CHEMBL3765816 — — 3 6.59
CHEMBL3765270 — — 1 6.58
CHEMBL3764930 — — 1 6.47
CHEMBL3763295 — — 1 6.27
CHEMBL3763349 — — 1 6.22
CHEMBL3764328 — — 1 6.20
CHEMBL3764711 — — 1 6.16
CHEMBL3763700 — — 1 6.16
CHEMBL3765308 — — 1 6.12
CHEMBL3764342 — — 1 6.11
CHEMBL3763854 — — 1 6.09
CHEMBL3763162 — — 5 5.96
CHEMBL3764856 — — 1 5.96
CHEMBL3763635 — — 1 5.91
CHEMBL3763337 — — 1 5.90
CHEMBL3765330 — — 1 5.89
CHEMBL3763616 — — 1 5.85
CHEMBL3765466 — — 1 5.73
CHEMBL3763775 — — 1 5.69
CHEMBL3763283 — — 1 5.53
CHEMBL3763855 — — 1 5.48
CHEMBL1783734 PIRAGLIATIN 2.0 1 5.20
CHEMBL3765684 — — 1 5.18
CHEMBL3765430 — — 1 4.42
CHEMBL3763788 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764079 — EC50 = 12.4 nM 7.91
CHEMBL3764668 — EC50 = 115.0 nM 6.94
CHEMBL3764630 — EC50 = 148.0 nM 6.83
CHEMBL3764824 — EC50 = 173.0 nM 6.76
CHEMBL3765780 — EC50 = 194.0 nM 6.71
CHEMBL3765816 — EC50 = 255.0 nM 6.59
CHEMBL3765270 — EC50 = 263.0 nM 6.58
CHEMBL3764930 — EC50 = 342.0 nM 6.47
CHEMBL3763295 — EC50 = 535.0 nM 6.27
CHEMBL3765816 — EC50 = 549.0 nM 6.26
CHEMBL3763349 — EC50 = 608.0 nM 6.22
CHEMBL3764328 — EC50 = 638.0 nM 6.20
CHEMBL3763700 — EC50 = 695.0 nM 6.16
CHEMBL3764711 — EC50 = 688.0 nM 6.16
CHEMBL3765308 — EC50 = 756.0 nM 6.12
CHEMBL3764342 — EC50 = 783.0 nM 6.11
CHEMBL3763854 — EC50 = 810.0 nM 6.09
CHEMBL3765816 — EC50 = 1010.0 nM 6.00
CHEMBL3764856 — EC50 = 1100.0 nM 5.96
CHEMBL3763162 — EC50 = 1100.0 nM 5.96
CHEMBL3763162 — EC50 = 1150.0 nM 5.94
CHEMBL3763635 — EC50 = 1240.0 nM 5.91
CHEMBL3763337 — EC50 = 1260.0 nM 5.90
CHEMBL3765330 — EC50 = 1300.0 nM 5.89
CHEMBL3763616 — EC50 = 1410.0 nM 5.85
CHEMBL3763162 — EC50 = 1500.0 nM 5.82
CHEMBL3765466 — EC50 = 1870.0 nM 5.73
CHEMBL3763775 — EC50 = 2050.0 nM 5.69
CHEMBL3763283 — EC50 = 2930.0 nM 5.53
CHEMBL3763855 — EC50 = 3290.0 nM 5.48
CHEMBL1783734 PIRAGLIATIN EC50 = 6320.0 nM 5.20
CHEMBL3765684 — EC50 = 6630.0 nM 5.18
CHEMBL3765430 — EC50 = 38300.0 nM 4.42
CHEMBL3763788 — EC50 - — -
CHEMBL3764631 — EC50 - — -
CHEMBL3763940 — EC50 - — -
CHEMBL3765196 — EC50 - — -
CHEMBL3763162 — EC50 - — -
CHEMBL3763162 — EC50 - — -
CHEMBL3764855 — EC50 - — -
CHEMBL3764854 — EC50 - — -
CHEMBL3765579 — EC50 - — -
CHEMBL3765635 — EC50 - — -