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Assay Detail

CHEMBL4322503

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 mammalian expression system by kinome scan assay
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

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.
Borsari C, Rageot D, Dall'Asen A, Bohnacker T, Melone A, Sele AM, Jackson E, Langlois JB, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Wymann MP.
J Med Chem (2019) 62 : 8609 -8630
PubMed 31465220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 8.36 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4286698 1 9.57
CHEMBL4574759 1 8.46
CHEMBL4551080 1 8.46
CHEMBL4436124 1 7.85
CHEMBL4594206 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4286698 Kd = 0.27 nM 9.57
CHEMBL4574759 Kd = 3.5 nM 8.46
CHEMBL4551080 Kd = 3.5 nM 8.46
CHEMBL4436124 Kd = 14.0 nM 7.85
CHEMBL4594206 Kd = 34.0 nM 7.47