Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1805470

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

Binding
Inhibition of CDK4/cyclinD1 assessed as amount of ATP released by luciferase activity based PKLight assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.
Heathcote DA, Patel H, Kroll SH, Hazel P, Periyasamy M, Alikian M, Kanneganti SK, Jogalekar AS, Scheiper B, Barbazanges M, Blum A, Brackow J, Siwicka A, Pace RD, Fuchter MJ, Snyder JP, Liotta DC, Freemont PS, Aboagye EO, Coombes RC, Barrett AG, Ali S.
J Med Chem (2010) 53 : 8508 -8522
PubMed 21080703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.79 4.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14762 SELICICLIB 2.0 1 4.87
CHEMBL1234833 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14762 SELICICLIB IC50 = 13500.0 nM 4.87
CHEMBL1234833 IC50 = 20000.0 nM 4.70