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Assay Detail

CHEMBL2060804

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

Binding
Inhibition of human ERG channel expressed in CHO cells by patch clamp assay
13
Total Activities
13
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

Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK.
J Med Chem (2012) 55 : 4244 -4273
PubMed 22524250 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.91 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800137 1 5.25
CHEMBL2058833 GANAPLACIDE 2.0 1 4.87
CHEMBL2058831 1 4.87
CHEMBL2058837 1 4.66
CHEMBL2059066 1 -
CHEMBL2058844 1 -
CHEMBL2058843 1 -
CHEMBL2058842 1 -
CHEMBL2058841 1 -
CHEMBL2058840 1 -
CHEMBL2058838 1 -
CHEMBL2057225 1 -
CHEMBL1800836 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800137 IC50 = 5600.0 nM 5.25
CHEMBL2058833 GANAPLACIDE IC50 = 13400.0 nM 4.87
CHEMBL2058831 IC50 = 13400.0 nM 4.87
CHEMBL2058837 IC50 = 21900.0 nM 4.66
CHEMBL2059066 IC50 - -
CHEMBL2058844 IC50 - -
CHEMBL2058843 IC50 > 30000.0 nM -
CHEMBL2058842 IC50 - -
CHEMBL2058841 IC50 - -
CHEMBL2058840 IC50 - -
CHEMBL2058838 IC50 > 30000.0 nM -
CHEMBL2057225 IC50 > 30000.0 nM -
CHEMBL1800836 IC50 - -