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Assay Detail

CHEMBL828086

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

Binding
Concentration required for 50% inhibition of cyclin dependant kinase 2-cyclin E was measured by scintillation proximity assay
6
Total Activities
6
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 2/cyclin E1 (CHEMBL1907605)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.
Helal CJ, Sanner MA, Cooper CB, Gant T, Adam M, Lucas JC, Kang Z, Kupchinsky S, Ahlijanian MK, Tate B, Menniti FS, Kelly K, Peterson M.
Bioorg Med Chem Lett (2004) 14 : 5521 -5525
PubMed 15482916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.16 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426972 1 7.01
CHEMBL186510 1 6.58
CHEMBL185498 1 6.38
CHEMBL186120 1 6.01
CHEMBL188172 1 5.99
CHEMBL434917 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426972 IC50 = 98.0 nM 7.01
CHEMBL186510 IC50 = 265.0 nM 6.58
CHEMBL185498 IC50 = 412.0 nM 6.38
CHEMBL186120 IC50 = 980.0 nM 6.01
CHEMBL188172 IC50 = 1020.0 nM 5.99
CHEMBL434917 IC50 = 9770.0 nM 5.01