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Assay Detail

CHEMBL1947992

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

Binding
Inhibition of guinea pig ENaCbeta1/gamma1 expressed in FRT cells by short-circuit current technique
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Cell Type FRT
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a novel chemotype of potent human ENaC blockers using a bioisostere approach. Part 1: quaternary amines.
Hunt T, Atherton-Watson HC, Axford J, Collingwood SP, Coote KJ, Cox B, Czarnecki S, Danahay H, Devereux N, Howsham C, Hunt P, Paddock V, Paisley D, Young A.
Bioorg Med Chem Lett (2012) 22 : 929 -932
PubMed 22197144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.51 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1944743 1 6.75
CHEMBL945 AMILORIDE 4.0 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1944743 IC50 = 180.0 nM 6.75
CHEMBL945 AMILORIDE IC50 = 540.0 nM 6.27