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Assay Detail

CHEMBL4005478

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

Binding
Inhibition of PI3K p110beta in PTEN-deficient human PC3 cells assessed as decrease in AKT phosphorylation at ser473 after 2 hrs by TR-FRET assay
7
Total Activities
7
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

Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Perreault S, Chandrasekhar J, Cui ZH, Evarts J, Hao J, Kaplan JA, Kashishian A, Keegan KS, Kenney T, Koditek D, Lad L, Lepist EI, McGrath ME, Patel L, Phillips B, Therrien J, Treiberg J, Yahiaoui A, Phillips G.
J Med Chem (2017) 60 : 1555 -1567
PubMed 28106991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.88 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081433 1 8.43
CHEMBL4074361 1 8.38
CHEMBL4101102 1 8.12
CHEMBL4085918 1 7.82
CHEMBL4082978 1 7.70
CHEMBL4102306 1 7.38
CHEMBL4079545 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081433 EC50 = 3.7 nM 8.43
CHEMBL4074361 EC50 = 4.2 nM 8.38
CHEMBL4101102 EC50 = 7.6 nM 8.12
CHEMBL4085918 EC50 = 15.0 nM 7.82
CHEMBL4082978 EC50 = 20.0 nM 7.70
CHEMBL4102306 EC50 = 42.0 nM 7.38
CHEMBL4079545 EC50 = 45.0 nM 7.35