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Assay Detail

CHEMBL2186306

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

Binding
Inhibition of human recombinant mTOR (1360 to 2549 amino acids) assessed as reduction in phosphorylation of (GFP)-4-EBP1 after 30 mins by FRET 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

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.
Heffron TP, Salphati L, Alicke B, Cheong J, Dotson J, Edgar K, Goldsmith R, Gould SE, Lee LB, Lesnick JD, Lewis C, Ndubaku C, Nonomiya J, Olivero AG, Pang J, Plise EG, Sideris S, Trapp S, Wallin J, Wang L, Zhang X.
J Med Chem (2012) 55 : 8007 -8020
PubMed 22946614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.83 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178608 1 8.05
CHEMBL2178606 1 8.00
CHEMBL2178613 1 7.89
CHEMBL2178614 1 7.68
CHEMBL1084926 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178608 Ki = 9.0 nM 8.05
CHEMBL2178606 Ki = 10.0 nM 8.00
CHEMBL2178613 Ki = 13.0 nM 7.89
CHEMBL2178614 Ki = 21.0 nM 7.68
CHEMBL1084926 Ki = 30.0 nM 7.52