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Assay Detail

CHEMBL4004501

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ADMET
Inhibition of human KCNQ1/KCNE1 expressed in HEK293 cells assessed as reduction in slowly activating delayed rectifier cardiac potassium current by patch clamp electrophysiology method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Wolkenberg SE, Nolt MB, Bilodeau MT, Trotter BW, Manley PJ, Kett NR, Nanda KK, Wu Z, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Dinsmore CJ, Lindsley CW, Hartman GD.
Bioorg Med Chem Lett (2017) 27 : 1062 -1069
PubMed 28131713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.10 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065169 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065169 IC50 = 790.0 nM 6.10