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Assay Detail

CHEMBL4038158

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

Binding
Inhibition of human plasma kallikrein spiked in pig vitreous using HMWK as substrate assessed as suppression of bradykinin release preincubated for 15 mins followed by substrate addition measured after 15 mins by ELISA
2
Total Activities
2
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

Plasma kallikrein (CHEMBL2000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stable and Long-Lasting, Novel Bicyclic Peptide Plasma Kallikrein Inhibitors for the Treatment of Diabetic Macular Edema.
Teufel DP, Bennett G, Harrison H, van Rietschoten K, Pavan S, Stace C, Le Floch F, Van Bergen T, Vermassen E, Barbeaux P, Hu TT, Feyen JHM, Vanhove M.
J Med Chem (2018) 61 : 2823 -2836
PubMed 29517911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.90 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4094403 1 8.22
CHEMBL4059991 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4094403 IC50 = 6.0 nM 8.22
CHEMBL4059991 IC50 = 27.0 nM 7.57