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Assay Detail

CHEMBL4716075

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

Binding
Inhibition of PI3kdelta in anti-IgD-induced human whole blood cells assessed as reduction in CD69 expression measured after 6 hrs by immunostaining based flow cytometric analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Shin Y,Suchomel J,Cardozo M,Duquette J,He X,Henne K,Hu YL,Kelly RC,McCarter J,McGee LR,Medina JC,Metz D,San Miguel T,Mohn D,Tran T,Vissinga C,Wong S,Wannberg S,Whittington DA,Whoriskey J,Yu G,Zalameda L,Zhang X,Cushing TD
J Med Chem (2016) 59 : 431 -447
PubMed 26652588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.52 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790186 1 7.72
CHEMBL4754382 1 7.71
CHEMBL2216895 1 7.66
CHEMBL4784595 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790186 IC50 = 19.0 nM 7.72
CHEMBL4754382 IC50 = 19.5 nM 7.71
CHEMBL2216895 IC50 = 22.0 nM 7.66
CHEMBL4784595 IC50 = 107.0 nM 6.97