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Assay Detail

CHEMBL759068

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

Binding
Inhibition of serine/threonine kinase(PKC-alpha)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Phenylamino-pyrimidine (PAP) derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors
Zimmermann J, Buchdunger E, Mett H, Meyer T, Lydon NB, Traxler P
Bioorg Med Chem Lett (1996) 6 : 1221 -1226
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.66 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277931 1 5.92
CHEMBL21086 1 5.00
CHEMBL21215 1 4.15
CHEMBL20926 1 4.14
CHEMBL278287 1 4.07
CHEMBL21162 1 -
CHEMBL20426 1 -
CHEMBL418010 1 -
CHEMBL21079 1 -
CHEMBL278103 1 -
CHEMBL277430 1 -
CHEMBL20867 1 -
CHEMBL20252 1 -
CHEMBL21078 1 -
CHEMBL423288 1 -
CHEMBL278630 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277931 IC50 = 1200.0 nM 5.92
CHEMBL21086 IC50 = 10000.0 nM 5.00
CHEMBL21215 IC50 = 71000.0 nM 4.15
CHEMBL20926 IC50 = 72000.0 nM 4.14
CHEMBL278287 IC50 = 85000.0 nM 4.07
CHEMBL21162 IC50 > 100000.0 nM -
CHEMBL20426 IC50 > 500000.0 nM -
CHEMBL418010 IC50 > 100000.0 nM -
CHEMBL21079 IC50 > 100000.0 nM -
CHEMBL278103 IC50 > 100000.0 nM -
CHEMBL277430 IC50 > 100000.0 nM -
CHEMBL20867 IC50 > 100000.0 nM -
CHEMBL20252 IC50 > 100000.0 nM -
CHEMBL21078 IC50 > 100000.0 nM -
CHEMBL423288 IC50 > 100000.0 nM -
CHEMBL278630 IC50 > 100000.0 nM -