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Assay Detail

CHEMBL898630

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

Binding
Inhibition of human Chk1
18
Total Activities
18
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

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activities of isogranulatimide analogues.
Hugon B, Anizon F, Bailly C, Golsteyn RM, Pierré A, Léonce S, Hickman J, Pfeiffer B, Prudhomme M.
Bioorg Med Chem (2007) 15 : 5965 -5980
PubMed 17582773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.84 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239698 1 7.80
CHEMBL393545 1 7.62
CHEMBL238625 1 7.18
CHEMBL240747 GRANULATIMIDE 1 7.10
CHEMBL392052 1 7.05
CHEMBL413188 ISOGRANULATIMIDE 1 6.36
CHEMBL427684 1 6.19
CHEMBL392154 1 5.44
CHEMBL239697 1 -
CHEMBL400012 1 -
CHEMBL392153 1 -
CHEMBL392940 1 -
CHEMBL392737 1 -
CHEMBL400203 1 -
CHEMBL391232 1 -
CHEMBL392053 1 -
CHEMBL392700 1 -
CHEMBL239914 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239698 IC50 = 16.0 nM 7.80
CHEMBL393545 IC50 = 24.0 nM 7.62
CHEMBL238625 IC50 = 66.0 nM 7.18
CHEMBL240747 GRANULATIMIDE IC50 = 80.0 nM 7.10
CHEMBL392052 IC50 = 89.0 nM 7.05
CHEMBL413188 ISOGRANULATIMIDE IC50 = 440.0 nM 6.36
CHEMBL427684 IC50 = 640.0 nM 6.19
CHEMBL392154 IC50 = 3600.0 nM 5.44
CHEMBL239697 IC50 - -
CHEMBL400012 IC50 - -
CHEMBL392153 IC50 - -
CHEMBL392940 IC50 - -
CHEMBL392737 IC50 - -
CHEMBL400203 IC50 - -
CHEMBL391232 IC50 - -
CHEMBL392053 IC50 - -
CHEMBL392700 IC50 - -
CHEMBL239914 IC50 - -