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Assay Detail

CHEMBL3117751

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

Binding
Inhibition of human PC7 expressed in drosophila schneider 2 cells using pyroGlu-Arg-Thr-Lys-Arg-AMC as substrate after 1 hr
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Schneider 2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Proprotein convertase subtilisin/kexin type 7 (CHEMBL2232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship studies of a potent PACE4 inhibitor.
Kwiatkowska A, Couture F, Levesque C, Ly K, Desjardins R, Beauchemin S, Prahl A, Lammek B, Neugebauer W, Dory YL, Day R.
J Med Chem (2014) 57 : 98 -109
PubMed 24350995 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.50 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3115771 1 7.86
CHEMBL3115770 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3115771 Ki = 13.8 nM 7.86
CHEMBL3115770 Ki = 72.0 nM 7.14