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Assay Detail

CHEMBL5519908

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

Binding
Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured for 1 hr in presence of ATP by ADP-Glo assay
6
Total Activities
6
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

Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Hu J, Fu S, Zhan Z, Zhang J.
Eur J Med Chem (2024) 265 : 116109 -116109
PubMed 38183777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.92 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3218576 COPANLISIB 4.0 1 8.76
CHEMBL5170300 1 8.35
CHEMBL1879463 DACTOLISIB 3.0 1 8.15
CHEMBL4749655 1 7.43
CHEMBL4297181 SAMOTOLISIB 2.0 1 7.42
CHEMBL3393066 VS-5584 1.0 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3218576 COPANLISIB IC50 = 1.72 nM 8.76
CHEMBL5170300 IC50 = 4.52 nM 8.35
CHEMBL1879463 DACTOLISIB IC50 = 7.0 nM 8.15
CHEMBL4749655 IC50 = 37.0 nM 7.43
CHEMBL4297181 SAMOTOLISIB IC50 = 38.0 nM 7.42
CHEMBL3393066 VS-5584 IC50 = 42.0 nM 7.38