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Assay Detail

CHEMBL3606997

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

Binding
Inhibition of CDK4 (unknown origin) using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 4 (CHEMBL331)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.
Sánchez-Martínez C, Gelbert LM, Lallena MJ, de Dios A.
Bioorg Med Chem Lett (2015) 25 : 3420 -3435
PubMed 26115571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.98 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190281 1 8.70
CHEMBL365847 1 8.70
CHEMBL189937 1 8.30
CHEMBL142648 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190281 IC50 = 2.0 nM 8.70
CHEMBL365847 IC50 = 2.0 nM 8.70
CHEMBL189937 IC50 = 5.0 nM 8.30
CHEMBL142648 IC50 = 620.0 nM 6.21