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Assay Detail

CHEMBL3364869

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

Binding
Inhibition of human Kv1.5 expressed in mouse L929 cells assessed as inhibition of current
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type L929
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

Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.
Johnson JA, Xu N, Jeon Y, Finlay HJ, Kover A, Conder ML, Sun H, Li D, Levesque P, Hsueh MM, Harper TW, Wexler RR, Lloyd J.
Bioorg Med Chem Lett (2014) 24 : 3018 -3022
PubMed 24881565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.99 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298226 1 7.66
CHEMBL3298228 1 7.64
CHEMBL3356073 1 7.60
CHEMBL3298140 1 7.37
CHEMBL3298227 1 7.14
CHEMBL3356074 1 7.08
CHEMBL3298231 1 7.06
CHEMBL3298225 1 6.93
CHEMBL3298232 1 6.86
CHEMBL3298147 1 6.73
CHEMBL3298229 1 6.71
CHEMBL3356070 1 6.70
CHEMBL3298145 1 6.66
CHEMBL3298146 1 6.58
CHEMBL3298141 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298226 IC50 = 22.0 nM 7.66
CHEMBL3298228 IC50 = 23.0 nM 7.64
CHEMBL3356073 IC50 = 25.0 nM 7.60
CHEMBL3298140 IC50 = 43.0 nM 7.37
CHEMBL3298227 IC50 = 73.0 nM 7.14
CHEMBL3356074 IC50 = 84.0 nM 7.08
CHEMBL3298231 IC50 = 88.0 nM 7.06
CHEMBL3298225 IC50 = 118.0 nM 6.93
CHEMBL3298232 IC50 = 138.0 nM 6.86
CHEMBL3298147 IC50 = 187.0 nM 6.73
CHEMBL3298229 IC50 = 197.0 nM 6.71
CHEMBL3356070 IC50 = 198.0 nM 6.70
CHEMBL3298145 IC50 = 219.0 nM 6.66
CHEMBL3298146 IC50 = 262.0 nM 6.58
CHEMBL3298141 IC50 = 784.0 nM 6.11