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Assay Detail

CHEMBL3739101

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

Binding
Inhibition of human wild-type plasma kallikrein catalytic domain after 15 mins using H-D-Pro-Phe-Arg-p-nitroanilide as substrate
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Plasma kallikrein (CHEMBL2000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.
Xu P, Xu M, Jiang L, Yang Q, Luo Z, Dauter Z, Huang M, Andreasen PA.
J Med Chem (2015) 58 : 8868 -8876
PubMed 26536069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.02 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735263 1 8.00
CHEMBL3735080 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735263 Ki = 9.93 nM 8.00
CHEMBL3735080 Ki = 907.0 nM 6.04