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Assay Detail

CHEMBL767029

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Binding
Inhibition of Protein kinase C alpha
8
Total Activities
8
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

Protein kinase C- inhibitors; structure-activity relationships in bis-indole series
Xie G, Zimmermann J, Meyer T, William Lown J
Bioorg Med Chem Lett (1995) 5 : 497 -500
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.82 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.40
CHEMBL7463 GF-109203 1 8.00
CHEMBL149237 1 6.77
CHEMBL269437 1 6.55
CHEMBL268744 1 6.34
CHEMBL9680 1 6.30
CHEMBL429569 1 6.20
CHEMBL9333 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 4.0 nM 8.40
CHEMBL7463 GF-109203 IC50 = 10.0 nM 8.00
CHEMBL149237 IC50 = 170.0 nM 6.77
CHEMBL269437 IC50 = 280.0 nM 6.55
CHEMBL268744 IC50 = 460.0 nM 6.34
CHEMBL9680 IC50 = 500.0 nM 6.30
CHEMBL429569 IC50 = 630.0 nM 6.20
CHEMBL9333 IC50 = 1000.0 nM 6.00