Assay Detail

CHEMBL4004500

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Binding

Inhibition of Kv1.5 mediated ultra-rapid delayed rectifier current Ikur in human atrial myocytes by voltage-patch clamp electrophysiology method

ChEMBL ↗

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Target

Potassium voltage-gated channel subfamily A member 5 (CHEMBL4306) ↗

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Potassium voltage-gated channel subfamily A member 5 (CHEMBL4306) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Potassium voltage-gated channel subfamily A member 5

CHEMBL4306

Anchored from Assay target.

Protein identity Potassium voltage-gated channel subfamily A member 5

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Potassium voltage-gated channel subfamily A member 5 (CHEMBL4306) ↗

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	7.96	7.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4065169	—	—	1	7.96
CHEMBL4104525	—	—	1	7.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4065169	—	IC50	=	11.0	nM	7.96
CHEMBL4104525	—	IC50	=	11.0	nM	7.96