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Assay Detail

CHEMBL3370358

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

Binding
Inhibition of CDK2/cyclin A (unknown origin) by HTRF kinase assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

CDK2/Cyclin A2 (CHEMBL3038469)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.
Song P, Peng P, Han M, Cao X, Ma X, Liu T, Zhou Y, Hu Y.
Bioorg Med Chem (2014) 22 : 4882 -4892
PubMed 25042558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.10 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3330230 1 6.61
CHEMBL3330236 1 6.59
CHEMBL3330148 1 6.48
CHEMBL3330232 1 6.41
CHEMBL3330132 1 6.07
CHEMBL3330133 1 6.07
CHEMBL3330136 1 5.79
CHEMBL3330229 1 5.50
CHEMBL3330233 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3330230 IC50 = 246.2 nM 6.61
CHEMBL3330236 IC50 = 255.99 nM 6.59
CHEMBL3330148 IC50 = 334.33 nM 6.48
CHEMBL3330232 IC50 = 393.33 nM 6.41
CHEMBL3330132 IC50 = 848.82 nM 6.07
CHEMBL3330133 IC50 = 851.83 nM 6.07
CHEMBL3330136 IC50 = 1630.44 nM 5.79
CHEMBL3330229 IC50 = 3187.14 nM 5.50
CHEMBL3330233 IC50 = 4304.83 nM 5.37