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Assay Detail

CHEMBL769625

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

Binding
Displacement of PDBU from recombinant Protein kinase C alpha with phosphatidylserine
11
Total Activities
11
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

New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.
Kozikowski AP, Nowak I, Petukhov PA, Etcheberrigaray R, Mohamed A, Tan M, Lewin N, Hennings H, Pearce LL, Blumberg PM.
J Med Chem (2003) 46 : 364 -373
PubMed 12540236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.60 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330952 1 8.25
CHEMBL333323 1 8.11
CHEMBL123244 1 8.04
CHEMBL123355 1 7.95
CHEMBL331344 1 7.92
CHEMBL123159 1 7.90
CHEMBL6453 1 7.83
CHEMBL333240 1 7.80
CHEMBL333801 1 7.47
CHEMBL334195 1 6.65
CHEMBL420170 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330952 Ki = 5.6 nM 8.25
CHEMBL333323 Ki = 7.8 nM 8.11
CHEMBL123244 Ki = 9.2 nM 8.04
CHEMBL123355 Ki = 11.2 nM 7.95
CHEMBL331344 Ki = 11.9 nM 7.92
CHEMBL123159 Ki = 12.5 nM 7.90
CHEMBL6453 Ki = 14.7 nM 7.83
CHEMBL333240 Ki = 15.8 nM 7.80
CHEMBL333801 Ki = 34.2 nM 7.47
CHEMBL334195 Ki = 225.0 nM 6.65
CHEMBL420170 Ki = 1970.0 nM 5.71