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Assay Detail

CHEMBL865567

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Toxicity
Inhibition of hERG potassium channel expressed in CHO cells by whole cell patch clamp method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
Richter HG, Adams DR, Benardeau A, Bickerdike MJ, Bentley JM, Blench TJ, Cliffe IA, Dourish C, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Monck NJ, Plancher JM, Roever S, Roffey JR, Taylor S, Vickers SP.
Bioorg Med Chem Lett (2006) 16 : 1207 -1211
PubMed 16361098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.89 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191054 1 5.60
CHEMBL206845 1 4.68
CHEMBL203230 1 4.40
CHEMBL203013 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191054 IC50 = 2500.0 nM 5.60
CHEMBL206845 IC50 = 21000.0 nM 4.68
CHEMBL203230 IC50 = 40000.0 nM 4.40
CHEMBL203013 IC50 > 30000.0 nM -