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Assay Detail

CHEMBL939830

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

Binding
Inhibition of human ERG expressed in HEK cells by competitive radioligand binding assay
6
Total Activities
6
Compounds Tested
1
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

Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
Li Y, Liang J, Siu T, Hu E, Rossi MA, Barnett SF, Defeo-Jones D, Jones RE, Robinson RG, Leander K, Huber HE, Mittal S, Cosford N, Prasit P.
Bioorg Med Chem Lett (2009) 19 : 834 -836
PubMed 19097777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.41 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508861 1 5.70
CHEMBL445464 1 5.56
CHEMBL506077 1 5.28
CHEMBL499555 1 5.27
CHEMBL507130 1 5.25
CHEMBL447328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508861 IC50 = 2018.0 nM 5.70
CHEMBL445464 IC50 = 2778.0 nM 5.56
CHEMBL506077 IC50 = 5312.0 nM 5.28
CHEMBL499555 IC50 = 5319.0 nM 5.27
CHEMBL507130 IC50 = 5610.0 nM 5.25
CHEMBL447328 IC50 > 10000.0 nM -