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Assay Detail

CHEMBL4434258

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

Binding
Inhibition of mTOR in mouse TSC1-/- MEF cells assessed as inhibition of S6 Ser240/244 phosphorylation incubated for 2 hrs by fluorescence based assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type MEF
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase mTOR (CHEMBL1255165)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Rapalogs Potential as Practical Alternatives to Rapamycin.
Abdel-Magid AF.
ACS Med Chem Lett (2019) 10 : 843 -845
PubMed 31223435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.06 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413 SIROLIMUS 4.0 1 10.30
CHEMBL4529771 1 9.77
CHEMBL4591064 1 9.56
CHEMBL4465976 1 9.43
CHEMBL4580738 1 8.49
CHEMBL4563398 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413 SIROLIMUS IC50 = 0.05 nM 10.30
CHEMBL4529771 IC50 = 0.17 nM 9.77
CHEMBL4591064 IC50 = 0.274 nM 9.56
CHEMBL4465976 IC50 = 0.374 nM 9.43
CHEMBL4580738 IC50 = 3.2 nM 8.49
CHEMBL4563398 IC50 = 153.0 nM 6.82