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Assay Detail

CHEMBL1827362

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

Binding
Displacement of [3H]dofetilide from human recombinant ERG by Competitive binding assay
ChEMBL ↗
234
Total Activities
234
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity.
Levoin N, Labeeuw O, Calmels T, Poupardin-Olivier O, Berrebi-Bertrand I, Lecomte JM, Schwartz JC, Capet M.
Bioorg Med Chem Lett (2011) 21 : 5378 -5383
PubMed 21802950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 217 5.37 8.36
Ki 17 6.47 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL560923 — — 1 8.36
CHEMBL557853 — — 1 8.30
CHEMBL1822858 — — 1 8.30
CHEMBL1822861 — — 1 8.10
CHEMBL549433 — — 1 7.96
CHEMBL564514 — — 1 7.92
CHEMBL1822854 — — 1 7.89
CHEMBL1822688 — — 1 7.85
CHEMBL550393 — — 1 7.60
CHEMBL1822859 — — 1 7.12
CHEMBL1822689 — — 1 7.05
CHEMBL573485 — — 1 7.00
CHEMBL584766 — — 1 7.00
CHEMBL1082488 — — 1 6.92
CHEMBL487059 — — 1 6.77
CHEMBL1094028 — — 1 6.75
CHEMBL1094029 — — 1 6.73
CHEMBL1822850 — — 1 6.72
CHEMBL1094030 — — 1 6.70
CHEMBL573034 — — 1 6.69
CHEMBL583582 — — 1 6.69
CHEMBL1822853 — — 1 6.64
CHEMBL552279 — — 1 6.53
CHEMBL574837 — — 1 6.51
CHEMBL453894 — — 1 6.46
CHEMBL476322 — — 1 6.46
CHEMBL1091836 — — 1 6.42
CHEMBL1823340 — — 1 6.38
CHEMBL1823180 — — 1 6.36
CHEMBL487060 — — 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL560923 — IC50 = 4.4 nM 8.36
CHEMBL557853 — IC50 = 5.0 nM 8.30
CHEMBL1822858 — Ki = 5.0 nM 8.30
CHEMBL1822861 — Ki = 8.0 nM 8.10
CHEMBL549433 — IC50 = 11.0 nM 7.96
CHEMBL564514 — IC50 = 12.0 nM 7.92
CHEMBL1822854 — Ki = 13.0 nM 7.89
CHEMBL1822688 — Ki = 14.0 nM 7.85
CHEMBL550393 — IC50 = 25.0 nM 7.60
CHEMBL1822859 — Ki = 76.0 nM 7.12
CHEMBL1822689 — Ki = 90.0 nM 7.05
CHEMBL584766 — IC50 = 101.01 nM 7.00
CHEMBL573485 — IC50 = 101.01 nM 7.00
CHEMBL1082488 — IC50 = 120.0 nM 6.92
CHEMBL487059 — IC50 = 170.0 nM 6.77
CHEMBL1094028 — IC50 = 178.0 nM 6.75
CHEMBL1094029 — IC50 = 188.0 nM 6.73
CHEMBL1822850 — Ki = 190.0 nM 6.72
CHEMBL1094030 — IC50 = 202.0 nM 6.70
CHEMBL583582 — IC50 = 204.08 nM 6.69
CHEMBL573034 — IC50 = 204.08 nM 6.69
CHEMBL1822853 — Ki = 230.0 nM 6.64
CHEMBL552279 — IC50 = 296.7 nM 6.53
CHEMBL574837 — IC50 = 309.28 nM 6.51
CHEMBL476322 — IC50 = 350.0 nM 6.46
CHEMBL453894 — IC50 = 350.0 nM 6.46
CHEMBL1091836 — IC50 = 384.0 nM 6.42
CHEMBL1823340 — IC50 = 420.0 nM 6.38
CHEMBL1823180 — IC50 = 440.0 nM 6.36
CHEMBL487060 — IC50 = 460.0 nM 6.34
CHEMBL556100 — IC50 = 470.0 nM 6.33
CHEMBL558456 — IC50 = 571.43 nM 6.24
CHEMBL1083463 — IC50 = 600.0 nM 6.22
CHEMBL518431 — IC50 = 710.0 nM 6.15
CHEMBL563118 — IC50 = 750.0 nM 6.12
CHEMBL1822860 — Ki = 818.0 nM 6.09
CHEMBL1822855 — Ki = 841.0 nM 6.08
CHEMBL1086520 — IC50 = 880.0 nM 6.06
CHEMBL575022 — IC50 = 989.01 nM 6.00
CHEMBL565007 — IC50 = 1000.0 nM 6.00
CHEMBL453893 — IC50 = 1100.0 nM 5.96
CHEMBL562629 — IC50 = 1109.59 nM 5.96
CHEMBL479241 — IC50 = 1100.0 nM 5.96
CHEMBL1822856 — Ki = 1125.0 nM 5.95
CHEMBL572558 — IC50 = 1111.11 nM 5.95
CHEMBL575483 — IC50 = 1111.11 nM 5.95
CHEMBL561279 — IC50 = 1166.67 nM 5.93
CHEMBL1822851 — Ki = 1194.0 nM 5.92
CHEMBL578862 — IC50 = 1235.96 nM 5.91
CHEMBL582876 — IC50 = 1363.64 nM 5.87