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Assay Detail

CHEMBL2168044

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Binding
Inhibition of human recombinant hERG expressed in CHO cells by automated patch clamp assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Danthi S, Langille J, Harwig C, Veale D, Carpenter B, Ba T, Bey M, Baird I, Wilson T, Metz M, MacFarland R, Mosi R, Bodart V, Wong R, Fricker S, Huskens D, Schols D.
ACS Med Chem Lett (2012) 3 : 216 -221
PubMed 24900457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.27 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164207 1 6.52
CHEMBL2164203 1 5.80
CHEMBL2164206 1 5.26
CHEMBL2164219 1 5.08
CHEMBL2164210 1 4.97
CHEMBL2164220 1 4.80
CHEMBL2164208 1 4.48
CHEMBL2164212 1 -
CHEMBL2164211 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164207 IC50 = 300.0 nM 6.52
CHEMBL2164203 IC50 = 1600.0 nM 5.80
CHEMBL2164206 IC50 = 5500.0 nM 5.26
CHEMBL2164219 IC50 = 8400.0 nM 5.08
CHEMBL2164210 IC50 = 10800.0 nM 4.97
CHEMBL2164220 IC50 = 16000.0 nM 4.80
CHEMBL2164208 IC50 = 33000.0 nM 4.48
CHEMBL2164212 IC50 > 50000.0 nM -
CHEMBL2164211 IC50 > 40000.0 nM -