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Assay Detail

CHEMBL3582655

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

Binding
Inhibition of [20-3H]phorbol 12,13-dibutyrate binding to human PKCalpha by scintillation counting based poly(ethylene) glycol precipitation assay
3
Total Activities
3
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

Neristatin 1 provides critical insight into bryostatin 1 structure-function relationships.
Kedei N, Kraft MB, Keck GE, Herald CL, Melody N, Pettit GR, Blumberg PM.
J Nat Prod (2015) 78 : 896 -900
PubMed 25808573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.28 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449158 BRYOSTATIN 1 2.0 1 9.32
CHEMBL3581528 1 7.86
CHEMBL3581527 1 7.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449158 BRYOSTATIN 1 Ki = 0.48 nM 9.32
CHEMBL3581528 Ki = 13.8 nM 7.86
CHEMBL3581527 Ki = 21.2 nM 7.67