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Assay Detail

CHEMBL4253404

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

Binding
Inhibition of CDK2/Cyclin-E1 (unknown origin) using histone-H1 as substrate after 90 mins by ADP-Glo assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Yin L, Li H, Liu W, Yao Z, Cheng Z, Zhang H, Zou H.
Eur J Med Chem (2018) 144 : 1 -28
PubMed 29247857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.63 5.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4277900 CROZBACICLIB 2.0 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4277900 CROZBACICLIB IC50 = 2321.0 nM 5.63