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Assay Detail

CHEMBL767023

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Binding
Inhibition of Protein kinase C alpha
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Protein kinase C alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.
Imbach P, Capraro HG, Furet P, Mett H, Meyer T, Zimmermann J.
Bioorg Med Chem Lett (1999) 9 : 91 -96
PubMed 9990463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.55 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368278 1 5.22
CHEMBL367625 2 4.87
CHEMBL173647 1 4.50
CHEMBL173459 1 4.42
CHEMBL366734 1 4.42
CHEMBL534909 1 4.30
CHEMBL557975 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368278 IC50 = 6000.0 nM 5.22
CHEMBL367625 IC50 = 13500.0 nM 4.87
CHEMBL367625 IC50 = 30000.0 nM 4.52
CHEMBL173647 IC50 = 31500.0 nM 4.50
CHEMBL173459 IC50 = 38500.0 nM 4.42
CHEMBL366734 IC50 = 38500.0 nM 4.42
CHEMBL534909 IC50 = 50000.0 nM 4.30
CHEMBL557975 IC50 = 78000.0 nM 4.11