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Assay Detail

CHEMBL4385717

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

Binding
Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

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 6.47 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453364 1 7.26
CHEMBL2216870 IDELALISIB 4.0 1 6.81
CHEMBL4471020 1 6.77
CHEMBL4468379 1 6.12
CHEMBL4520088 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453364 IC50 = 55.0 nM 7.26
CHEMBL2216870 IDELALISIB IC50 = 154.0 nM 6.81
CHEMBL4471020 IC50 = 169.0 nM 6.77
CHEMBL4468379 IC50 = 766.0 nM 6.12
CHEMBL4520088 IC50 = 3990.0 nM 5.40