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Assay Detail

CHEMBL2330743

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

Binding
Inhibition of human ERG K+ channel expressed in HEK293 cells after 15 mins by patch clamp assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide.
Carvalho JF, Louvel J, Doornbos ML, Klaasse E, Yu Z, Brussee J, IJzerman AP.
J Med Chem (2013) 56 : 2828 -2840
PubMed 23473309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.56 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2324256 1 6.84
CHEMBL2325199 1 6.71
CHEMBL2325200 1 6.67
CHEMBL2325205 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2324256 IC50 = 146.0 nM 6.84
CHEMBL2325199 IC50 = 194.0 nM 6.71
CHEMBL2325200 IC50 = 214.0 nM 6.67
CHEMBL2325205 IC50 = 962.0 nM 6.02