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Assay Detail

CHEMBL4354193

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

Binding
Inhibition of CDK2/cyclin A2 (unknown origin) using histone H1 and ATP as substrate incubated for 40 mins by kinase-glo luminescence assay
14
Total Activities
14
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

Discovery of novel pyrimidine-based benzothiazole derivatives as potent cyclin-dependent kinase 2 inhibitors with anticancer activity.
Diao PC, Lin WY, Jian XE, Li YH, You WW, Zhao PL.
Eur J Med Chem (2019) 179 : 196 -207
PubMed 31254921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.66 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4526687 1 7.90
CHEMBL4454288 1 7.81
CHEMBL4435968 1 7.78
CHEMBL4528300 1 7.67
CHEMBL4475342 1 7.66
CHEMBL4543030 1 7.42
CHEMBL488436 AZD-5438 1.0 1 7.35
CHEMBL4539730 1 -
CHEMBL4470088 1 -
CHEMBL4527631 1 -
CHEMBL4543207 1 -
CHEMBL4552048 1 -
CHEMBL4459752 1 -
CHEMBL4468668 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4526687 IC50 = 12.7 nM 7.90
CHEMBL4454288 IC50 = 15.4 nM 7.81
CHEMBL4435968 IC50 = 16.5 nM 7.78
CHEMBL4528300 IC50 = 21.4 nM 7.67
CHEMBL4475342 IC50 = 21.7 nM 7.66
CHEMBL4543030 IC50 = 37.8 nM 7.42
CHEMBL488436 AZD-5438 IC50 = 45.0 nM 7.35
CHEMBL4539730 IC50 - -
CHEMBL4470088 IC50 - -
CHEMBL4527631 IC50 - -
CHEMBL4543207 IC50 - -
CHEMBL4552048 IC50 - -
CHEMBL4459752 IC50 - -
CHEMBL4468668 IC50 - -