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Assay Detail

CHEMBL3611619

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

Binding
Antagonist activity at human Kv1.1 expressed in HEK293 cells assessed as inhibition of potassium currents by automated patchXpress planar patch clamp electrophysiology assay
3
Total Activities
3
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

Target

Potassium voltage-gated channel subfamily A member 1 (CHEMBL2309)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3.
Murray JK, Qian YX, Liu B, Elliott R, Aral J, Park C, Zhang X, Stenkilsson M, Salyers K, Rose M, Li H, Yu S, Andrews KL, Colombero A, Werner J, Gaida K, Sickmier EA, Miu P, Itano A, McGivern J, Gegg CV, Sullivan JK, Miranda LP.
J Med Chem (2015) 58 : 6784 -6802
PubMed 26288216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.39 10.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609093 1 10.06
CHEMBL3609095 1 9.67
CHEMBL3609073 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609093 IC50 = 0.087 nM 10.06
CHEMBL3609095 IC50 = 0.214 nM 9.67
CHEMBL3609073 IC50 = 3.677 nM 8.44