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Assay Detail

CHEMBL4331742

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

Binding
Inhibition of human N-terminal His-tagged PI3Kalpha/p85alpha expressed in Spodoptera frugiperda using phosphatidylinositol as substrate
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

PI3-kinase p110-alpha/p85-alpha (CHEMBL2111367)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Targeting the immunity protein kinases for immuno-oncology.
Yuan X, Wu H, Bu H, Zhou J, Zhang H.
Eur J Med Chem (2019) 163 : 413 -427
PubMed 30530193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.87 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2216870 IDELALISIB 4.0 1 6.10
CHEMBL4450504 1 5.64
CHEMBL2216863 DEZAPELISIB 2.0 1 -
CHEMBL3948730 UMBRALISIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2216870 IDELALISIB IC50 = 800.0 nM 6.10
CHEMBL4450504 IC50 = 2299.0 nM 5.64
CHEMBL2216863 DEZAPELISIB IC50 > 10000.0 nM -
CHEMBL3948730 UMBRALISIB IC50 > 10000.0 nM -