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Assay Detail

CHEMBL4385720

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

Binding
Inhibition of His-tagged recombinant human full length PI3K p110alpha/p85alpha expressed in baculovirus expression system using lipid substrate incubated for 60 mins by kinase-Glo reagent based luminescence assay
5
Total Activities
5
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

Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.
Ma X, Wei J, Wang C, Gu D, Hu Y, Sheng R.
Eur J Med Chem (2019) 170 : 112 -125
PubMed 30878826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.70 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453364 1 6.00
CHEMBL2216870 IDELALISIB 4.0 1 5.67
CHEMBL4468379 1 5.44
CHEMBL4520088 1 -
CHEMBL4471020 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453364 IC50 = 996.0 nM 6.00
CHEMBL2216870 IDELALISIB IC50 = 2164.0 nM 5.67
CHEMBL4468379 IC50 = 3637.0 nM 5.44
CHEMBL4520088 IC50 > 5000.0 nM -
CHEMBL4471020 IC50 > 5000.0 nM -