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Assay Detail

CHEMBL911174

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

Binding
Inhibition of CDK2/Cyclin E in presence of 15 uM ATP
14
Total Activities
14
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 2/cyclin E (CHEMBL2094126)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Krystof V, Cankar P, Frysová I, Slouka J, Kontopidis G, Dzubák P, Hajdúch M, Srovnal J, de Azevedo WF, Orság M, Paprskárová M, Rolcík J, Látr A, Fischer PM, Strnad M.
J Med Chem (2006) 49 : 6500 -6509
PubMed 17064068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.90 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386422 1 5.60
CHEMBL215205 1 5.46
CHEMBL280074 OLOMOUCINE 1 5.30
CHEMBL214475 1 5.22
CHEMBL387068 1 5.21
CHEMBL425089 1 5.00
CHEMBL215072 1 4.82
CHEMBL428639 1 4.77
CHEMBL384625 1 4.66
CHEMBL217734 1 4.64
CHEMBL425975 1 4.55
CHEMBL217836 1 4.40
CHEMBL216673 1 4.04
CHEMBL383939 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386422 IC50 = 2500.0 nM 5.60
CHEMBL215205 IC50 = 3500.0 nM 5.46
CHEMBL280074 OLOMOUCINE IC50 = 5000.0 nM 5.30
CHEMBL214475 IC50 = 6000.0 nM 5.22
CHEMBL387068 IC50 = 6100.0 nM 5.21
CHEMBL425089 IC50 = 10000.0 nM 5.00
CHEMBL215072 IC50 = 15000.0 nM 4.82
CHEMBL428639 IC50 = 17000.0 nM 4.77
CHEMBL384625 IC50 = 22000.0 nM 4.66
CHEMBL217734 IC50 = 23000.0 nM 4.64
CHEMBL425975 IC50 = 28000.0 nM 4.55
CHEMBL217836 IC50 = 40000.0 nM 4.40
CHEMBL216673 IC50 = 92000.0 nM 4.04
CHEMBL383939 IC50 > 100000.0 nM -