Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4038129

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

Binding
Inhibition of rabbit plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide as substrate preincubated for 15 mins followed by substrate addition measured by fluorescence-based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
Ki 5 6.39 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093698 1 8.00
CHEMBL4079260 1 7.08
CHEMBL4059991 1 5.84
CHEMBL4070056 1 5.58
CHEMBL4094403 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093698 Ki = 10.0 nM 8.00
CHEMBL4079260 Ki = 84.0 nM 7.08
CHEMBL4059991 Ki = 1450.0 nM 5.84
CHEMBL4070056 Ki = 2650.0 nM 5.58
CHEMBL4094403 Ki = 3400.0 nM 5.47