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Assay Detail

CHEMBL3375306

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

Binding
Binding affinity to human CDK4/cyclinD1 using GST-pRB152 as substrate by chemiluminescence assay
4
Total Activities
4
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

Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Biphenyl-4-carboxylic acid [2-(1H-indol-3-yl)-ethyl]-methylamide (CA224), a nonplanar analogue of fascaplysin, inhibits Cdk4 and tubulin polymerization: evaluation of in vitro and in vivo anticancer activity.
Mahale S, Bharate SB, Manda S, Joshi P, Bharate SS, Jenkins PR, Vishwakarma RA, Chaudhuri B.
J Med Chem (2014) 57 : 9658 -9672
PubMed 25368960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.08 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258765 FASCAPLYSIN CHLORIDE 1 6.39
CHEMBL213805 1 5.21
CHEMBL213302 1 4.42
CHEMBL209467 1 4.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258765 FASCAPLYSIN CHLORIDE IC50 = 410.0 nM 6.39
CHEMBL213805 IC50 = 6200.0 nM 5.21
CHEMBL213302 IC50 = 38000.0 nM 4.42
CHEMBL209467 IC50 = 49000.0 nM 4.31