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Assay Detail

CHEMBL4200632

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 after 15 mins by fluorescence assay
4
Total Activities
4
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

6-Substituted Hexamethylene Amiloride (HMA) Derivatives as Potent and Selective Inhibitors of the Human Urokinase Plasminogen Activator for Use in Cancer.
Buckley BJ, Aboelela A, Minaei E, Jiang LX, Xu Z, Ali U, Fildes K, Cheung CY, Cook SM, Johnson DC, Bachovchin DA, Cook GM, Apte M, Huang M, Ranson M, Kelso MJ.
J Med Chem (2018) 61 : 8299 -8320
PubMed 30130401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.55 5.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217043 1 5.79
CHEMBL4213248 1 5.74
CHEMBL945 AMILORIDE 4.0 1 5.64
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217043 Ki = 1611.0 nM 5.79
CHEMBL4213248 Ki = 1802.0 nM 5.74
CHEMBL945 AMILORIDE Ki = 2313.0 nM 5.64
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE Ki = 9308.0 nM 5.03