Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4723569

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

Binding
Binding affinity to wild-type human partial length MTOR (L1382 to W2549 residues) expressed in HEK293 cells measured after 1 hr by Kinomescan method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.
Borsari C,Keles E,Rageot D,Treyer A,Bohnacker T,Bissegger L,De Pascale M,Melone A,Sriramaratnam R,Beaufils F,Hamburger M,Hebeisen P,Löscher W,Fabbro D,Hillmann P,Wymann MP
J Med Chem (2020) 63 : 13595 -13617
PubMed 33166139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 9.12 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749352 1 9.17
CHEMBL4741511 1 9.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749352 Kd = 0.67 nM 9.17
CHEMBL4741511 Kd = 0.88 nM 9.06