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Assay Detail

CHEMBL3866459

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

Binding
Inhibition of human CDK1/cyclinA expressed in Baculovirus infected Sf9 cells using Biotin-aminohexyl-Ala-Arg-Arg-Pro-Met-Ser-Pro-Lys-LysLys-Ala-CONH2 as substrate measured after 30 to 60 mins in presence of [gamma-32P]ATP by scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

CDK1/Cyclin A (CHEMBL3038467)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-Hydrazinoindolin-2-one derivatives: Chemical classification and investigation of their targets as anticancer agents.
Ibrahim HS, Abou-Seri SM, Abdel-Aziz HA.
Eur J Med Chem (2016) 122 : 366 -381
PubMed 27391135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.49 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410883 1 8.55
CHEMBL269827 GW276655X 1 8.00
CHEMBL409892 GW305178X 1 7.92
CHEMBL411426 1 7.43
CHEMBL271160 1 7.39
CHEMBL407709 1 7.37
CHEMBL272387 1 6.77
CHEMBL272389 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410883 IC50 = 2.8 nM 8.55
CHEMBL269827 GW276655X IC50 = 10.0 nM 8.00
CHEMBL409892 GW305178X IC50 = 12.0 nM 7.92
CHEMBL411426 IC50 = 37.0 nM 7.43
CHEMBL271160 IC50 = 41.0 nM 7.39
CHEMBL407709 IC50 = 43.0 nM 7.37
CHEMBL272387 IC50 = 170.0 nM 6.77
CHEMBL272389 IC50 = 350.0 nM 6.46