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Assay Detail

CHEMBL769617

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

Binding
Displacement of [3H]- PDBu from recombinant PKC alpha expressed in baculovirus
5
Total Activities
5
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

Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.
Kozikowski AP, Wang S, Ma D, Yao J, Ahmad S, Glazer RI, Bogi K, Acs P, Modarres S, Lewin NE, Blumberg PM.
J Med Chem (1997) 40 : 1316 -1326
PubMed 9135029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.78 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL285801 1 9.30
CHEMBL27266 INDOLACTUM 1 7.96
CHEMBL6453 1 7.83
CHEMBL28205 1 7.33
CHEMBL267144 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL285801 Ki = 0.5 nM 9.30
CHEMBL27266 INDOLACTUM Ki = 11.0 nM 7.96
CHEMBL6453 Ki = 14.7 nM 7.83
CHEMBL28205 Ki = 46.6 nM 7.33
CHEMBL267144 Ki = 334.0 nM 6.48