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Assay Detail

CHEMBL4199847

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

Binding
Inhibition of recombinant human His-tagged p85alpha/p110alpha E542K mutant expressed in insect cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.
Shen S, He X, Yang Z, Zhang L, Liu Y, Zhang Z, Wang W, Liu W, Li Y, Huang D, Sun K, Ni X, Yang X, Chu X, Cui Y, Lv Q, Lan J, Zhou F.
ACS Med Chem Lett (2018) 9 : 719 -724
PubMed 30034607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.75 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211915 1 7.96
CHEMBL2017974 BUPARLISIB 3.0 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211915 IC50 = 11.0 nM 7.96
CHEMBL2017974 BUPARLISIB IC50 = 29.0 nM 7.54