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Assay Detail

CHEMBL4392573

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

Binding
Inhibition of mTOR (unknown origin) assessed as reduction in p70S6K phosphorylation
5
Total Activities
5
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

Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.
Bahekar R, Dave B, Soman S, Patel D, Chopade R, Funde R, Kumar J, Sachchidanand S, Giri P, Chatterjee A, Mahapatra J, Vyas P, Ghoshdastidar K, Bandyopadhyay D, Desai RC.
Bioorg Med Chem Lett (2019) 29 : 1313 -1319
PubMed 30975623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.75 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1879463 DACTOLISIB 3.0 1 7.85
CHEMBL4550603 1 6.24
CHEMBL4454741 1 6.17
CHEMBL2216870 IDELALISIB 4.0 1 -
CHEMBL4560054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1879463 DACTOLISIB IC50 = 14.0 nM 7.85
CHEMBL4550603 IC50 = 580.0 nM 6.24
CHEMBL4454741 IC50 = 676.0 nM 6.17
CHEMBL2216870 IDELALISIB IC50 > 1000.0 nM -
CHEMBL4560054 IC50 > 1000.0 nM -