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Assay Detail

CHEMBL1954560

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Binding
Inhibition of human ERG by electrophysiological assay
2
Total Activities
2
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

Publication

Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.
Cumming JG, Tucker H, Oldfield J, Fielding C, Highton A, Faull A, Wild M, Brown D, Wells S, Shaw J.
Bioorg Med Chem Lett (2012) 22 : 1655 -1659
PubMed 22266038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.34 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212689 1 5.72
CHEMBL1951914 AZD5672 2.0 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212689 IC50 = 1900.0 nM 5.72
CHEMBL1951914 AZD5672 IC50 = 11000.0 nM 4.96