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Assay Detail

CHEMBL4200628

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

ADMET
Cytotoxicity against HEK293 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 ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 1 — Organism
Curated By Intermediate

Target

HEK293 (CHEMBL614818)
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 5.03 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE 1 5.55
CHEMBL4213248 1 5.51
CHEMBL4207715 1 4.92
CHEMBL4217043 1 4.13
CHEMBL4212068 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL501701 N,N-HEXAMETHYLENEAMILORIDE IC50 = 2800.0 nM 5.55
CHEMBL4213248 IC50 = 3100.0 nM 5.51
CHEMBL4207715 IC50 = 12000.0 nM 4.92
CHEMBL4217043 IC50 = 74900.0 nM 4.13
CHEMBL4212068 IC50 > 100000.0 nM -