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Assay Detail

CHEMBL2384826

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Binding
Inhibition of [3H]PDBu binding to PKCdelta-C1A domain peptide (unknown origin)
11
Total Activities
11
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 delta type (CHEMBL2996)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.
Kamachi H, Tanaka K, Yanagita RC, Murakami A, Murakami K, Tokuda H, Suzuki N, Nakagawa Y, Irie K.
Bioorg Med Chem (2013) 21 : 2695 -2702
PubMed 23582444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.91 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2148106 DEBROMOAPLYSIATOXIN 1 8.01
CHEMBL2148108 1 7.66
CHEMBL2381162 1 7.18
CHEMBL2381164 1 7.10
CHEMBL2381165 1 7.09
CHEMBL2381163 1 7.03
CHEMBL2381166 1 6.96
CHEMBL1258348 1 6.85
CHEMBL2381161 1 6.54
CHEMBL2381167 1 6.48
CHEMBL2381160 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2148106 DEBROMOAPLYSIATOXIN Ki = 9.7 nM 8.01
CHEMBL2148108 Ki = 22.0 nM 7.66
CHEMBL2381162 Ki = 66.0 nM 7.18
CHEMBL2381164 Ki = 79.0 nM 7.10
CHEMBL2381165 Ki = 82.0 nM 7.09
CHEMBL2381163 Ki = 93.0 nM 7.03
CHEMBL2381166 Ki = 110.0 nM 6.96
CHEMBL1258348 Ki = 140.0 nM 6.85
CHEMBL2381161 Ki = 290.0 nM 6.54
CHEMBL2381167 Ki = 330.0 nM 6.48
CHEMBL2381160 Ki = 8700.0 nM 5.06