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Assay Detail

CHEMBL5167636

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

Binding
Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
4
Total Activities
4
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

Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
Zhang J, Jiang H, Lin S, Wu D, Tian H, Jiang L, Cui Y, Jin J, Chen X, Xu H.
J Med Chem (2022) 65 : 8011 -8028
PubMed 35609190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.71 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3643413 LENIOLISIB 4.0 1 6.04
CHEMBL5192588 1 5.70
CHEMBL5204818 1 5.57
CHEMBL5203775 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3643413 LENIOLISIB IC50 = 902.0 nM 6.04
CHEMBL5192588 IC50 = 1989.0 nM 5.70
CHEMBL5204818 IC50 = 2678.0 nM 5.57
CHEMBL5203775 IC50 = 2855.5 nM 5.54