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Assay Detail

CHEMBL4200611

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

Binding
Inhibition of human kidney uPA using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay
4
Total Activities
4
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

Urokinase-type plasminogen activator (CHEMBL3286)
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 4 6.42 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217043 1 7.41
CHEMBL4207715 1 6.37
CHEMBL4213248 1 6.28
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217043 IC50 = 39.0 nM 7.41
CHEMBL4207715 IC50 = 430.0 nM 6.37
CHEMBL4213248 IC50 = 530.0 nM 6.28
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE IC50 = 2400.0 nM 5.62