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Assay Detail

CHEMBL862313

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

Binding
Inhibition of chk2 kinase
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase Chk2 (CHEMBL2527)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel non-benzimidazole chk2 kinase inhibitors.
McClure KJ, Huang L, Arienti KL, Axe FU, Brunmark A, Blevitt J, Breitenbucher JG.
Bioorg Med Chem Lett (2006) 16 : 1924 -1928
PubMed 16442290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.50 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179583 1 7.80
CHEMBL178971 1 7.26
CHEMBL206609 1 7.11
CHEMBL208463 1 6.88
CHEMBL367390 1 6.19
CHEMBL205906 1 5.81
CHEMBL377597 1 5.70
CHEMBL204930 1 5.24
CHEMBL205905 1 -
CHEMBL382588 1 -
CHEMBL204929 1 -
CHEMBL202669 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179583 IC50 = 16.0 nM 7.80
CHEMBL178971 IC50 = 55.0 nM 7.26
CHEMBL206609 IC50 = 77.0 nM 7.11
CHEMBL208463 IC50 = 133.0 nM 6.88
CHEMBL367390 IC50 = 640.0 nM 6.19
CHEMBL205906 IC50 = 1540.0 nM 5.81
CHEMBL377597 IC50 = 2000.0 nM 5.70
CHEMBL204930 IC50 = 5800.0 nM 5.24
CHEMBL205905 IC50 > 10000.0 nM -
CHEMBL382588 IC50 > 10000.0 nM -
CHEMBL204929 IC50 > 10000.0 nM -
CHEMBL202669 IC50 > 10000.0 nM -