Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4832751

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

Binding
Inhibition of human PI3Kdelta expressed in rat fibroblast cells assessed as reduction in AKT phosphorylation at Ser473 residue incubated for 1 hr by AlphaScreen assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery and Toxicological Profiling of Aminopyridines as Orally Bioavailable Selective Inhibitors of PI3-Kinase γ.
Bellenie BR, Hall E, Bruce I, Spendiff M, Culshaw A, McDonald S, Ambarkhane A, Chinn C, Thomas M, Rosner E, Bracher M, Nicklin P, Marshall S, Coote J, Cullen E, Tessier C, Wuersch K, Lal A, Wallis G, Hollingworth GJ, Neef J.
J Med Chem (2021) 64 : 12304 -12321
PubMed 34384024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.70 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4859017 1 6.17
CHEMBL4857001 1 5.54
CHEMBL2071342 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4859017 IC50 = 680.0 nM 6.17
CHEMBL4857001 IC50 = 2879.0 nM 5.54
CHEMBL2071342 IC50 = 4030.0 nM 5.39