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Assay Detail

CHEMBL2067907

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

Binding
Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L.
J Med Chem (2012) 55 : 4788 -4805
PubMed 22524426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.76 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064328 1 8.52
CHEMBL1972466 1 8.00
CHEMBL2064331 1 7.39
CHEMBL2064330 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064328 IC50 = 3.0 nM 8.52
CHEMBL1972466 IC50 = 10.0 nM 8.00
CHEMBL2064331 IC50 = 41.0 nM 7.39
CHEMBL2064330 IC50 = 76.0 nM 7.12