Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1027667

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

Binding
Inhibition of human ERG channel
ChEMBL ↗
140
Total Activities
113
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

Side chain flexibilities in the human ether-a-go-go related gene potassium channel (hERG) together with matched-pair binding studies suggest a new binding mode for channel blockers.
Zachariae U, Giordanetto F, Leach AG.
J Med Chem (2009) 52 : 4266 -4276
PubMed 19534531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 98 6.03 8.17
Ki 42 5.96 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1729 CISAPRIDE 4.0 2 8.17
CHEMBL12713 SERTINDOLE 4.0 2 7.83
CHEMBL501295 — — 1 7.75
CHEMBL536480 — — 2 7.74
CHEMBL146233 — — 1 7.70
CHEMBL329067 — — 1 7.62
CHEMBL54 HALOPERIDOL 4.0 2 7.57
CHEMBL479 THIORIDAZINE 4.0 2 7.48
CHEMBL1423 PIMOZIDE 4.0 2 7.26
CHEMBL150210 — — 1 7.16
CHEMBL526466 — — 2 7.10
CHEMBL40584 — — 1 7.10
CHEMBL525413 — — 2 7.09
CHEMBL98553 — — 1 6.96
CHEMBL496687 — — 1 6.96
CHEMBL147431 — — 1 6.96
CHEMBL708 ZIPRASIDONE 4.0 2 6.90
CHEMBL85 RISPERIDONE 4.0 2 6.83
CHEMBL516874 — — 2 6.82
CHEMBL149429 — — 1 6.82
CHEMBL498100 — — 1 6.75
CHEMBL100415 — — 1 6.72
CHEMBL526277 — — 1 6.72
CHEMBL83894 FANANSERIN 2.0 1 6.70
CHEMBL498260 — — 1 6.68
CHEMBL17157 TERFENADINE 4.0 2 6.67
CHEMBL524352 — — 1 6.66
CHEMBL715 OLANZAPINE 4.0 2 6.64
CHEMBL46523 — — 1 6.54
CHEMBL210537 — — 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1729 CISAPRIDE IC50 = 6.7 nM 8.17
CHEMBL1729 CISAPRIDE IC50 = 6.7 nM 8.17
CHEMBL12713 SERTINDOLE IC50 = 14.7 nM 7.83
CHEMBL12713 SERTINDOLE IC50 = 14.7 nM 7.83
CHEMBL501295 — Ki = 18.0 nM 7.75
CHEMBL536480 — IC50 = 18.1 nM 7.74
CHEMBL536480 — IC50 = 18.1 nM 7.74
CHEMBL146233 — Ki = 20.0 nM 7.70
CHEMBL329067 — IC50 = 24.0 nM 7.62
CHEMBL54 HALOPERIDOL IC50 = 26.8 nM 7.57
CHEMBL54 HALOPERIDOL IC50 = 26.8 nM 7.57
CHEMBL479 THIORIDAZINE IC50 = 33.2 nM 7.48
CHEMBL479 THIORIDAZINE IC50 = 33.2 nM 7.48
CHEMBL1423 PIMOZIDE IC50 = 54.6 nM 7.26
CHEMBL1423 PIMOZIDE IC50 = 54.6 nM 7.26
CHEMBL150210 — Ki = 69.0 nM 7.16
CHEMBL40584 — Ki = 80.0 nM 7.10
CHEMBL526466 — IC50 = 80.0 nM 7.10
CHEMBL526466 — IC50 = 80.0 nM 7.10
CHEMBL525413 — IC50 = 82.0 nM 7.09
CHEMBL98553 — IC50 = 110.0 nM 6.96
CHEMBL496687 — Ki = 110.0 nM 6.96
CHEMBL147431 — Ki = 110.0 nM 6.96
CHEMBL708 ZIPRASIDONE IC50 = 125.0 nM 6.90
CHEMBL708 ZIPRASIDONE IC50 = 125.0 nM 6.90
CHEMBL85 RISPERIDONE IC50 = 148.0 nM 6.83
CHEMBL85 RISPERIDONE IC50 = 148.0 nM 6.83
CHEMBL516874 — IC50 = 150.0 nM 6.82
CHEMBL149429 — Ki = 150.0 nM 6.82
CHEMBL516874 — IC50 = 150.0 nM 6.82
CHEMBL498100 — IC50 = 180.0 nM 6.75
CHEMBL100415 — IC50 = 190.0 nM 6.72
CHEMBL526277 — IC50 = 190.0 nM 6.72
CHEMBL83894 FANANSERIN Ki = 200.0 nM 6.70
CHEMBL498260 — IC50 = 210.0 nM 6.68
CHEMBL17157 TERFENADINE IC50 = 213.0 nM 6.67
CHEMBL17157 TERFENADINE IC50 = 213.0 nM 6.67
CHEMBL524352 — IC50 = 220.0 nM 6.66
CHEMBL715 OLANZAPINE IC50 = 231.3 nM 6.64
CHEMBL715 OLANZAPINE IC50 = 231.3 nM 6.64
CHEMBL46523 — Ki = 290.0 nM 6.54
CHEMBL210537 — IC50 = 300.0 nM 6.52
CHEMBL1088 MESORIDAZINE IC50 = 320.0 nM 6.50
CHEMBL42 CLOZAPINE IC50 = 320.0 nM 6.50
CHEMBL42 CLOZAPINE IC50 = 320.0 nM 6.50
CHEMBL1088 MESORIDAZINE IC50 = 320.0 nM 6.50
CHEMBL501480 — IC50 = 320.0 nM 6.50
CHEMBL312137 — IC50 = 440.0 nM 6.36
CHEMBL322007 — IC50 = 480.0 nM 6.32
CHEMBL496860 — Ki = 500.0 nM 6.30