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Assay Detail

CHEMBL5720136

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

Binding
Inhibition of recombinant human full-length N-terminal His6-tagged p110delta/recombinant human full length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using phosphatidylinositol-(3,4,5)-trisphosphate as substrate by HTRF assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

PI3-kinase p110-delta/p85-alpha (CHEMBL2111432)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J, Hao Y, Xu X, Deng SX, Realubit RB, Tatonetti NP, Karan C, Lentzsch S, Fruman DA, Honig B, Landry DW, O'Connor OA.
Blood (2017) 129 : 88 -99
PubMed 27784673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.65 7.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3948730 UMBRALISIB 4.0 1 7.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3948730 UMBRALISIB EC50 = 22.2 nM 7.65