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Assay Detail

CHEMBL5347353

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

Binding
Inhibition of mTOR (unknown origin)
10
Total Activities
10
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

Target

Serine/threonine-protein kinase mTOR (CHEMBL2842)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents.
Occhiuzzi MA, Lico G, Ioele G, De Luca M, Garofalo A, Grande F.
Eur J Med Chem (2023) 246 : 114971 -114971
PubMed 36462440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.69 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2336325 VISTUSERTIB 2.0 1 8.55
CHEMBL589258 1 8.52
CHEMBL5278435 1 7.92
CHEMBL3544966 GSK-1059615 1.0 1 7.92
CHEMBL5439799 1 7.80
CHEMBL4071083 1 7.80
CHEMBL1922094 APITOLISIB 2.0 1 7.77
CHEMBL1879463 DACTOLISIB 3.0 1 7.68
CHEMBL3813842 PAXALISIB 2.0 1 7.16
CHEMBL1234429 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2336325 VISTUSERTIB IC50 = 2.8 nM 8.55
CHEMBL589258 IC50 = 3.0 nM 8.52
CHEMBL5278435 IC50 = 12.0 nM 7.92
CHEMBL3544966 GSK-1059615 IC50 = 12.0 nM 7.92
CHEMBL5439799 IC50 = 16.0 nM 7.80
CHEMBL4071083 IC50 = 16.0 nM 7.80
CHEMBL1922094 APITOLISIB IC50 = 17.0 nM 7.77
CHEMBL1879463 DACTOLISIB IC50 = 20.7 nM 7.68
CHEMBL3813842 PAXALISIB IC50 = 70.0 nM 7.16
CHEMBL1234429 IC50 = 1760.0 nM 5.75