Compound name
AZD 2014
Protein family
Protein Kinase
Target name
MTOR
Affinity biochemical (nM)
2.81
Affinity on-target cellular (nM)
78
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001788a
SMILES
CNC(=O)c1cccc(-c2ccc3c(N4CCOC[C@@H]4C)nc(N4CCOC[C@@H]4C)nc3n2)c1
InChIKey
JUSFANSTBFGBAF-IRXDYDNUSA-N
NCBI gene ID
2475
UniProt ID
P42345
Synonyms
RAFT1, RAPT1, FLJ44809
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay (FLAG-tagged mTOR (aa1362-2549) expressed in HEK 293 cells using biotinylated p70S6K peptide substrate)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26358751/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
MTOR cellular activity assay (measured in MDAMB468 cells, using an Acumen laser scanning cytometer (TTP Labtech) to analyze the levels of phosphorylation of AKT at Ser473)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/26358751/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Ambit)
Selectivity platform number of targets
393
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: DYRK2 (47%9, IKBKB(34%), PIK3CA(24%), PIK3CA(E545A, 19%), PIK3CA(Q546K, 21%), PIK3CA(E542K, 21%);
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26358751/
Selectivity Number of Off-targets
0