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Assay Detail

CHEMBL4366850

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

Binding
Inhibition of human CDK2/cyclin-A2 using H1 histone as substrate after 2 hrs by [gamma-33P]-ATP assay
6
Total Activities
6
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 of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.
Wang J, Li T, Zhao T, Wu T, Liu C, Ding H, Li Z, Bian J.
Eur J Med Chem (2019) 178 : 782 -801
PubMed 31238183 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.99 6.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4554243 1 6.08
CHEMBL4446230 1 6.04
CHEMBL4467886 1 5.98
CHEMBL16171 WOGONIN 1 5.84
CHEMBL4461927 1 -
CHEMBL4463420 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4554243 IC50 = 830.0 nM 6.08
CHEMBL4446230 IC50 = 913.0 nM 6.04
CHEMBL4467886 IC50 = 1040.0 nM 5.98
CHEMBL16171 WOGONIN IC50 = 1460.0 nM 5.84
CHEMBL4461927 IC50 - -
CHEMBL4463420 IC50 - -