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Assay Detail

CHEMBL907685

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Functional
Inhibition of Kv1.5 expressed in LTK- cells by whole cell patch clamp assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery and synthesis of tetrahydroindolone-derived carbamates as Kv1.5 blockers.
Fluxe A, Wu S, Sheffer JB, Janusz JM, Murawsky M, Fadayel GM, Fang B, Hare M, Djandjighian L.
Bioorg Med Chem Lett (2006) 16 : 5855 -5858
PubMed 16942878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.76 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216281 1 7.68
CHEMBL217347 1 7.17
CHEMBL217333 1 6.56
CHEMBL217348 1 6.46
CHEMBL385237 1 6.43
CHEMBL217672 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216281 IC50 = 21.0 nM 7.68
CHEMBL217347 IC50 = 67.0 nM 7.17
CHEMBL217333 IC50 = 275.0 nM 6.56
CHEMBL217348 IC50 = 350.0 nM 6.46
CHEMBL385237 IC50 = 368.0 nM 6.43
CHEMBL217672 IC50 = 547.0 nM 6.26