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Assay Detail

CHEMBL861277

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Functional
Effect on blockade of Kv1.4 channel
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Potassium voltage-gated channel subfamily A member 4 (CHEMBL4205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.
Harvey AJ, Baell JB, Toovey N, Homerick D, Wulff H.
J Med Chem (2006) 49 : 1433 -1441
PubMed 16480279 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.35 5.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426482 1 5.37
CHEMBL382154 1 5.32
CHEMBL203909 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426482 EC50 = 4300.0 nM 5.37
CHEMBL382154 EC50 = 4800.0 nM 5.32
CHEMBL203909 EC50 > 20000.0 nM -