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Assay Detail

CHEMBL1803471

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

Binding
Inhibition of human ERG expressed in CHO cells by Q-patch 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: hit to lead optimization of new antimalarial agents.
Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana SB, Wu J, Ang HQ, Zeng P, Kang ML, Tan W, Tan M, Ye N, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Hollenbeck T, Tuntland T, Isbell J, Fischli C, Brun R, Rottmann M, Dartois V, Keller T, Diagana T, Winzeler E, Glynne R, Tully DC, Chatterjee AK.
J Med Chem (2011) 54 : 5116 -5130
PubMed 21644570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.21 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800770 1 5.82
CHEMBL1800772 1 5.64
CHEMBL1800774 1 5.32
CHEMBL1800137 1 5.25
CHEMBL1800776 1 5.25
CHEMBL1800768 1 5.24
CHEMBL1800769 1 4.96
CHEMBL601821 1 4.72
CHEMBL1800775 1 4.68
CHEMBL1800836 1 -
CHEMBL1800831 1 -
CHEMBL1800771 1 -
CHEMBL1800773 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800770 IC50 = 1500.0 nM 5.82
CHEMBL1800772 IC50 = 2300.0 nM 5.64
CHEMBL1800774 IC50 = 4800.0 nM 5.32
CHEMBL1800137 IC50 = 5600.0 nM 5.25
CHEMBL1800776 IC50 = 5600.0 nM 5.25
CHEMBL1800768 IC50 = 5700.0 nM 5.24
CHEMBL1800769 IC50 = 11100.0 nM 4.96
CHEMBL601821 IC50 = 19000.0 nM 4.72
CHEMBL1800775 IC50 = 21000.0 nM 4.68
CHEMBL1800836 IC50 - -
CHEMBL1800831 IC50 > 30000.0 nM -
CHEMBL1800771 IC50 - -
CHEMBL1800773 IC50 - -