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Assay Detail

CHEMBL4200629

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

Functional
Cytotoxicity against human HT1080 cells assessed as reduction in cell viability after 48 hrs by CellTiter 96 Aqueous One solution cell proliferation assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-1080
Confidence 1 — Organism
Curated By Intermediate

Target

HT-1080 (CHEMBL614580)
Type CELL-LINE
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 5 5.00 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4207715 1 5.68
CHEMBL4213248 1 5.34
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE 1 5.18
CHEMBL4212068 1 4.43
CHEMBL4217043 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4207715 IC50 = 2100.0 nM 5.68
CHEMBL4213248 IC50 = 4600.0 nM 5.34
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE IC50 = 6600.0 nM 5.18
CHEMBL4212068 IC50 = 37100.0 nM 4.43
CHEMBL4217043 IC50 = 44800.0 nM 4.35