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Assay Detail

CHEMBL5338527

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Toxicity
Inhibition of human ERG expressed in CHO K1 cells measured after 4 min by QPatch assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

hERG, <i>Plasmodium</i> Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole.
Mambwe D, Coertzen D, Leshabane M, Mulubwa M, Njoroge M, Gibhard L, Girling G, Wicht KJ, Lee MCS, Wittlin S, Moreira DRM, Birkholtz LM, Chibale K.
ACS Med Chem Lett (2024) 15 : 463 -469
PubMed 38628794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.22 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296419 ASTEMIZOLE 4.0 1 8.40
CHEMBL5434251 1 6.38
CHEMBL6966 VERAPAMIL 4.0 1 6.25
CHEMBL5273140 1 6.20
CHEMBL5410878 1 6.08
CHEMBL5429029 1 6.01
CHEMBL5436114 1 5.78
CHEMBL5403581 1 5.57
CHEMBL5434807 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296419 ASTEMIZOLE IC50 = 4.0 nM 8.40
CHEMBL5434251 IC50 = 420.0 nM 6.38
CHEMBL6966 VERAPAMIL IC50 = 560.0 nM 6.25
CHEMBL5273140 IC50 = 630.0 nM 6.20
CHEMBL5410878 IC50 = 830.0 nM 6.08
CHEMBL5429029 IC50 = 980.0 nM 6.01
CHEMBL5436114 IC50 = 1650.0 nM 5.78
CHEMBL5403581 IC50 = 2720.0 nM 5.57
CHEMBL5434807 IC50 = 5070.0 nM 5.29