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Assay Detail

CHEMBL5031250

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

Binding
Displacement of [3H]-PDBu from recombinant human PKCalpha by scintillation counter method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 Characterization of Novel <i>sn</i>-1 Heterocyclic DAG-Lactones as PKC Activators.
Elhalem E, Bellomo A, Cooke M, Scravaglieri A, Pearce LV, Peach ML, Gandolfi Donadío L, Kazanietz MG, Comin MJ.
J Med Chem (2021) 64 : 11418 -11431
PubMed 34279947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.37 7.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL137386 1 7.63
CHEMBL5077090 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL137386 Ki = 23.6 nM 7.63
CHEMBL5077090 Ki = 79.3 nM 7.10