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Assay Detail

CHEMBL4392953

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

Binding
Inhibition of Kv1.5 in human atrial myocytes assessed as blockade of Ikur current
9
Total Activities
9
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

Potassium voltage-gated channel subfamily A member 5 (CHEMBL4306)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents.
Kajanus J, Antonsson T, Carlsson L, Jurva U, Pettersen A, Sundell J, Inghardt T.
Bioorg Med Chem Lett (2019) 29 : 1241 -1245
PubMed 30879840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.74 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4475999 1 7.22
CHEMBL4451245 1 6.58
CHEMBL4527638 1 6.41
CHEMBL4437013 1 -
CHEMBL4453132 1 -
CHEMBL4466634 1 -
CHEMBL4539540 1 -
CHEMBL4517112 1 -
CHEMBL4474540 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4475999 IC50 = 60.0 nM 7.22
CHEMBL4451245 IC50 = 260.0 nM 6.58
CHEMBL4527638 IC50 = 390.0 nM 6.41
CHEMBL4437013 IC50 - -
CHEMBL4453132 IC50 - -
CHEMBL4466634 IC50 - -
CHEMBL4539540 IC50 - -
CHEMBL4517112 IC50 - -
CHEMBL4474540 IC50 - -