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Assay Detail

CHEMBL856062

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Binding
Inhibition of human recombinant PKCalpha
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Inhibition of protein kinase C(alpha) by dequalinium analogues: dependence on linker length and geometry.
Qin D, Sullivan R, Berkowitz WF, Bittman R, Rotenberg SA.
J Med Chem (2000) 43 : 1413 -1417
PubMed 10753478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.93 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1315457 1 5.58
CHEMBL2113330 1 5.55
CHEMBL2113338 1 5.30
CHEMBL1256847 1 4.96
CHEMBL2113331 1 4.92
CHEMBL2113341 1 4.60
CHEMBL2112065 1 4.28
CHEMBL2113332 1 4.27
CHEMBL2113335 1 -
CHEMBL2113334 1 -
CHEMBL2113333 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1315457 IC50 = 2600.0 nM 5.58
CHEMBL2113330 IC50 = 2800.0 nM 5.55
CHEMBL2113338 IC50 = 5000.0 nM 5.30
CHEMBL1256847 IC50 = 11000.0 nM 4.96
CHEMBL2113331 IC50 = 12000.0 nM 4.92
CHEMBL2113341 IC50 = 25000.0 nM 4.60
CHEMBL2112065 IC50 = 52000.0 nM 4.28
CHEMBL2113332 IC50 = 54000.0 nM 4.27
CHEMBL2113335 IC50 = 3590000.0 nM -
CHEMBL2113334 IC50 = 117000.0 nM -
CHEMBL2113333 IC50 = 137000.0 nM -