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Assay Detail

CHEMBL4199837

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Binding
Inhibition of recombinant human full-length His-tagged p110gamma expressed in baculovirus expression system using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polarization assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 5 6.61 6.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4206442 1 6.79
CHEMBL4211915 1 6.69
CHEMBL4215969 1 6.54
CHEMBL2017974 BUPARLISIB 3.0 1 6.43
CHEMBL4210320 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4206442 IC50 = 164.0 nM 6.79
CHEMBL4211915 IC50 = 204.0 nM 6.69
CHEMBL4215969 IC50 = 288.0 nM 6.54
CHEMBL2017974 BUPARLISIB IC50 = 372.0 nM 6.43
CHEMBL4210320 IC50 - -