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Assay Detail

CHEMBL2380180

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

Binding
Inhibition of CDK4/Cyclin D1 (unknown origin)-mediated phosphorylation of peptide substrate incubated for 15 mins prior to substrate addition measured after 90 mins by P33-radiolabeled assay
2
Total Activities
2
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

Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.
Schonbrunn E, Betzi S, Alam R, Martin MP, Becker A, Han H, Francis R, Chakrasali R, Jakkaraj S, Kazi A, Sebti SM, Cubitt CL, Gebhard AW, Hazlehurst LA, Tash JS, Georg GI.
J Med Chem (2013) 56 : 3768 -3782
PubMed 23600925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.29 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2377825 1 8.40
CHEMBL388978 STAUROSPORINE 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2377825 IC50 = 4.0 nM 8.40
CHEMBL388978 STAUROSPORINE IC50 = 6.6 nM 8.18