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Assay Detail

CHEMBL2352069

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

Binding
Inhibition of recombinant mTOR (unknown origin) using GST-p70S6 as substrate after 60 mins by TR-FRET analysis
4
Total Activities
4
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

Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.
Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.
Bioorg Med Chem Lett (2013) 23 : 1588 -1591
PubMed 23414803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.63 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2348865 1 8.70
CHEMBL2348864 1 8.10
CHEMBL2348862 1 6.97
CHEMBL2348863 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2348865 IC50 = 2.0 nM 8.70
CHEMBL2348864 IC50 = 8.0 nM 8.10
CHEMBL2348862 IC50 = 106.0 nM 6.97
CHEMBL2348863 IC50 = 176.0 nM 6.75