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Assay Detail

CHEMBL999748

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

Binding
Displacement of [3H]PDBu from human recombinant PKCalpha expressed in Sf9 cells by liquid scintillation counting
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.
Boije af Gennäs G, Talman V, Aitio O, Ekokoski E, Finel M, Tuominen RK, Yli-Kauhaluoma J.
J Med Chem (2009) 52 : 3969 -3981
PubMed 19438240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 17 - -
Ki 5 6.69 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55267 1 7.40
CHEMBL466211 1 6.69
CHEMBL494361 1 6.50
CHEMBL523053 1 6.18
CHEMBL494179 1 -
CHEMBL493164 1 -
CHEMBL493005 1 -
CHEMBL493004 1 -
CHEMBL523703 1 -
CHEMBL494362 1 -
CHEMBL468924 1 -
CHEMBL468923 1 -
CHEMBL513861 1 -
CHEMBL466212 1 -
CHEMBL444698 1 -
CHEMBL468717 1 -
CHEMBL1162992 1 -
CHEMBL468716 1 -
CHEMBL513125 1 -
CHEMBL493003 1 -
CHEMBL450870 1 -
CHEMBL449158 BRYOSTATIN 1 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55267 Ki = 40.1 nM 7.40
CHEMBL466211 Ki = 205.0 nM 6.69
CHEMBL494361 Ki = 319.0 nM 6.50
CHEMBL523053 Ki = 661.0 nM 6.18
CHEMBL494179 Activity - -
CHEMBL493164 Activity - -
CHEMBL493005 Activity - -
CHEMBL493004 Activity - -
CHEMBL523703 Activity - -
CHEMBL494362 Activity - -
CHEMBL468924 Activity - -
CHEMBL468923 Activity - -
CHEMBL513861 Activity - -
CHEMBL466212 Activity - -
CHEMBL444698 Activity - -
CHEMBL468717 Activity - -
CHEMBL1162992 Activity - -
CHEMBL468716 Activity - -
CHEMBL513125 Activity - -
CHEMBL493003 Activity - -
CHEMBL450870 Activity - -
CHEMBL449158 BRYOSTATIN 1 Ki - -