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

CHEMBL3860722

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

Binding
Inhibition of PI3Kalpha (unknown origin) expressed in Rat1 cells assessed as reduction in Akt phosphorylation at Ser473 residue
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Rat1
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.
Fairhurst RA, Caravatti G, Guagnano V, Aichholz R, Blanz J, Blasco F, Wipfli P, Fritsch C, Maira SM, Schnell C, Seiler FH.
Bioorg Med Chem Lett (2016) 26 : 4729 -4734
PubMed 27575470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.43 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2397186 1 7.44
CHEMBL3975097 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2397186 IC50 = 36.0 nM 7.44
CHEMBL3975097 IC50 = 39.0 nM 7.41