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Assay Detail

CHEMBL4004506

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Binding
Inhibition of Kv4.3 (unknown origin) assessed as reduction in transient outward potassium current by high throughput clamp method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

A-type voltage-gated potassium channel KCND3 (CHEMBL1964)
Type SINGLE PROTEIN
Organism Homo sapiens

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 2 5.36 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065169 1 5.64
CHEMBL4104525 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065169 IC50 = 2300.0 nM 5.64
CHEMBL4104525 IC50 = 8300.0 nM 5.08