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Assay Detail

CHEMBL3407223

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

Binding
Inhibition of human ERG expressed in HEK293 cells assessed as reduction in tail current at membrane potential of +20 mV
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.
Seebacher W, Wolkinger V, Faist J, Kaiser M, Brun R, Saf R, Bucar F, Gröblacher B, Brantner A, Merino V, Kalia Y, Scapozza L, Perozzo R, Weis R.
Bioorg Med Chem Lett (2015) 25 : 1390 -1393
PubMed 25746816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.59 5.60
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 5.60
CHEMBL3401424 2 5.58
CHEMBL172 (S,R)-MEFLOQUINE 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 2500.0 nM 5.60
CHEMBL3401424 IC50 = 2630.0 nM 5.58
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 2600.0 nM 5.58
CHEMBL3401424 Inhibition - % -