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Assay Detail

CHEMBL2148241

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

Binding
Inhibition of [3H]PDBu binding to PKCepsilon C1B domain
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Protein kinase C epsilon type (CHEMBL3582)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.
Kikumori M, Yanagita RC, Tokuda H, Suzuki N, Nagai H, Suenaga K, Irie K.
J Med Chem (2012) 55 : 5614 -5626
PubMed 22625994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.32 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2148106 DEBROMOAPLYSIATOXIN 1 9.20
CHEMBL2148108 1 8.70
CHEMBL2148107 1 7.77
CHEMBL1258348 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2148106 DEBROMOAPLYSIATOXIN Ki = 0.63 nM 9.20
CHEMBL2148108 Ki = 2.0 nM 8.70
CHEMBL2148107 Ki = 17.0 nM 7.77
CHEMBL1258348 Ki = 25.0 nM 7.60