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Assay Detail

CHEMBL957971

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

Binding
Inhibition of human recombinant CDK4/cyclin D1
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

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

Publication

Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Peifer C, Selig R, Kinkel K, Ott D, Totzke F, Schächtele C, Heidenreich R, Röcken M, Schollmeyer D, Laufer S.
J Med Chem (2008) 51 : 3814 -3824
PubMed 18529047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.53 4.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201511 MALEIMIDE 1 4.85
CHEMBL488646 1 4.57
CHEMBL521201 1 4.52
CHEMBL452812 1 4.46
CHEMBL509435 1 4.40
CHEMBL488811 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201511 MALEIMIDE IC50 = 14000.0 nM 4.85
CHEMBL488646 IC50 = 27000.0 nM 4.57
CHEMBL521201 IC50 = 30000.0 nM 4.52
CHEMBL452812 IC50 = 35000.0 nM 4.46
CHEMBL509435 IC50 = 40000.0 nM 4.40
CHEMBL488811 IC50 = 44000.0 nM 4.36