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Assay Detail

CHEMBL5043593

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

Binding
Inhibition of mouse uPA using Z-Gly-Gly-Arg-AMC as substrate measured for 15 mins by fluorometric assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Urokinase-type plasminogen activator (CHEMBL1075311)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA).
S El Salamouni N, Buckley BJ, Jiang L, Huang M, Ranson M, Kelso MJ, Yu H.
J Med Chem (2022) 65 : 1933 -1945
PubMed 34898192 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.69 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4513418 1 6.02
CHEMBL4211423 1 5.56
CHEMBL4206764 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4513418 Ki = 956.0 nM 6.02
CHEMBL4211423 Ki = 2768.0 nM 5.56
CHEMBL4206764 Ki = 3293.0 nM 5.48