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Assay Detail

CHEMBL4004499

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

Binding
Inhibition of Kv1.5 (unknown origin)
36
Total Activities
36
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

Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Wolkenberg SE, Nolt MB, Bilodeau MT, Trotter BW, Manley PJ, Kett NR, Nanda KK, Wu Z, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Dinsmore CJ, Lindsley CW, Hartman GD.
Bioorg Med Chem Lett (2017) 27 : 1062 -1069
PubMed 28131713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.87 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065169 1 8.05
CHEMBL4085436 1 7.64
CHEMBL4105245 1 7.58
CHEMBL4104525 1 7.54
CHEMBL4062996 1 7.52
CHEMBL4075394 1 7.48
CHEMBL4095750 1 7.39
CHEMBL4088894 1 7.25
CHEMBL4067665 1 7.21
CHEMBL4100226 1 7.19
CHEMBL4097667 1 7.19
CHEMBL4100098 1 7.08
CHEMBL4094177 1 7.08
CHEMBL4080304 1 7.05
CHEMBL4097545 1 6.96
CHEMBL4094185 1 6.94
CHEMBL4079636 1 6.88
CHEMBL4068841 1 6.87
CHEMBL4072707 1 6.86
CHEMBL4081003 1 6.83
CHEMBL4102309 1 6.82
CHEMBL4080956 1 6.79
CHEMBL4061731 1 6.77
CHEMBL4084347 1 6.71
CHEMBL4074029 1 6.63
CHEMBL4094570 1 6.56
CHEMBL4089812 1 6.55
CHEMBL4076764 1 6.54
CHEMBL4087512 1 6.35
CHEMBL4105373 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065169 IC50 = 9.0 nM 8.05
CHEMBL4085436 IC50 = 23.0 nM 7.64
CHEMBL4105245 IC50 = 26.0 nM 7.58
CHEMBL4104525 IC50 = 29.0 nM 7.54
CHEMBL4062996 IC50 = 30.0 nM 7.52
CHEMBL4075394 IC50 = 33.0 nM 7.48
CHEMBL4095750 IC50 = 41.0 nM 7.39
CHEMBL4088894 IC50 = 56.0 nM 7.25
CHEMBL4067665 IC50 = 62.0 nM 7.21
CHEMBL4097667 IC50 = 64.0 nM 7.19
CHEMBL4100226 IC50 = 64.0 nM 7.19
CHEMBL4100098 IC50 = 84.0 nM 7.08
CHEMBL4094177 IC50 = 84.0 nM 7.08
CHEMBL4080304 IC50 = 90.0 nM 7.05
CHEMBL4097545 IC50 = 110.0 nM 6.96
CHEMBL4094185 IC50 = 116.0 nM 6.94
CHEMBL4079636 IC50 = 133.0 nM 6.88
CHEMBL4068841 IC50 = 136.0 nM 6.87
CHEMBL4072707 IC50 = 137.0 nM 6.86
CHEMBL4081003 IC50 = 148.0 nM 6.83
CHEMBL4102309 IC50 = 153.0 nM 6.82
CHEMBL4080956 IC50 = 161.0 nM 6.79
CHEMBL4061731 IC50 = 171.0 nM 6.77
CHEMBL4084347 IC50 = 195.0 nM 6.71
CHEMBL4074029 IC50 = 233.0 nM 6.63
CHEMBL4094570 IC50 = 276.0 nM 6.56
CHEMBL4089812 IC50 = 283.0 nM 6.55
CHEMBL4076764 IC50 = 290.0 nM 6.54
CHEMBL4087512 IC50 = 444.0 nM 6.35
CHEMBL4105373 IC50 = 579.0 nM 6.24
CHEMBL4074093 IC50 = 1276.0 nM 5.89
CHEMBL4089937 IC50 = 1386.0 nM 5.86
CHEMBL4060189 IC50 = 1592.0 nM 5.80
CHEMBL4098469 IC50 = 2865.0 nM 5.54
CHEMBL4096382 IC50 > 10000.0 nM -
CHEMBL4075240 IC50 > 10000.0 nM -