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Assay Detail

CHEMBL3411226

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

Binding
Inhibition of PI3Kdelta in human Jeko B cells assessed as inhibition of Akt phosphorylation after 2 hrs
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Péru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N.
J Med Chem (2015) 58 : 943 -962
PubMed 25514658 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.77 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408248 AZD-8186 1.0 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408248 AZD-8186 IC50 = 17.0 nM 7.77