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Assay Detail

CHEMBL5356231

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

Binding
Inhibition of mTOR (unknown origin) using ULight-4E-BP1 (Thr37/46) as peptide substrate incubated for 30 mins in presence of ATP by LANCE Ultra assay
3
Total Activities
3
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

Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.
Li C, Han Y, Wang Z, Yu Y, Wang C, Ren Z, Guo Y, Zhu T, Li X, Dong S, Ma M.
Eur J Med Chem (2023) 247 : 115030 -115030
PubMed 36586298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.85 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5395998 1 8.51
CHEMBL4440406 1 7.68
CHEMBL3218576 COPANLISIB 4.0 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5395998 IC50 = 3.12 nM 8.51
CHEMBL4440406 IC50 = 21.0 nM 7.68
CHEMBL3218576 COPANLISIB IC50 = 45.0 nM 7.35