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Assay Detail

CHEMBL4352651

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

Binding
Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgM-stimulated CD69 expression on B-cells preincubated for 60 mins followed by anti-IgM stimulation and measured after overnight incubation by flow cytometry
2
Total Activities
2
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 Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.
Jia H, Dai G, Su W, Xiao K, Weng J, Zhang Z, Wang Q, Yuan T, Shi F, Zhang Z, Chen W, Sai Y, Wang J, Li X, Cai Y, Yu J, Ren P, Venable J, Rao T, Edwards JP, Bembenek SD.
J Med Chem (2019) 62 : 4936 -4948
PubMed 31033293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.53 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3039502 DUVELISIB 4.0 1 7.85
CHEMBL4513442 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3039502 DUVELISIB IC50 = 14.0 nM 7.85
CHEMBL4513442 IC50 = 63.0 nM 7.20