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Assay Detail

CHEMBL2185837

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

Binding
Inhibition of PI3Kalpha in human PC3 cells assessed as reduction in pAKT level by immunoblotting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-3
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.
Heffron TP, Salphati L, Alicke B, Cheong J, Dotson J, Edgar K, Goldsmith R, Gould SE, Lee LB, Lesnick JD, Lewis C, Ndubaku C, Nonomiya J, Olivero AG, Pang J, Plise EG, Sideris S, Trapp S, Wallin J, Wang L, Zhang X.
J Med Chem (2012) 55 : 8007 -8020
PubMed 22946614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.29 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178608 1 7.52
CHEMBL2178606 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178608 IC50 = 30.0 nM 7.52
CHEMBL2178606 IC50 = 90.0 nM 7.05