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Assay Detail

CHEMBL4478189

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

Binding
Inhibition of C-terminal FLAG-tagged recombinant mTOR (1362 to 2549 residues) (unknown origin) using Biotin-Ahx-Lys-Lys-Ala-Asn-Gln-Val-Phe-Leu-Gly-Phe-Thr-Tyr-Val-Ala-Pro-Ser-Val-Leu-Glu-Ser-Val-Lys-Glu-NH2 as substrate after 90 mins by AlphaScreen assay
8
Total Activities
8
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 Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Degorce SL, Barlaam B, Cadogan E, Dishington A, Ducray R, Glossop SC, Hassall LA, Lach F, Lau A, McGuire TM, Nowak T, Ouvry G, Pike KG, Thomason AG.
J Med Chem (2016) 59 : 6281 -6292
PubMed 27259031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.68 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4565988 1 6.74
CHEMBL4527822 1 6.07
CHEMBL4166405 1 5.83
CHEMBL4218734 1 5.54
CHEMBL4593348 1 5.46
CHEMBL2143829 1 5.34
CHEMBL222102 KU-55933 1 5.25
CHEMBL2140173 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4565988 IC50 = 181.0 nM 6.74
CHEMBL4527822 IC50 = 846.0 nM 6.07
CHEMBL4166405 IC50 = 1480.0 nM 5.83
CHEMBL4218734 IC50 = 2920.0 nM 5.54
CHEMBL4593348 IC50 = 3450.0 nM 5.46
CHEMBL2143829 IC50 = 4590.0 nM 5.34
CHEMBL222102 KU-55933 IC50 = 5580.0 nM 5.25
CHEMBL2140173 IC50 = 6550.0 nM 5.18