Compound name
CC-115
Protein family
Protein Kinase
Target name
MTOR
Affinity biochemical (nM)
21
Affinity on-target cellular (nM)
23
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002910aCl
SMILES
[H]Cl.O=C1CN=C2C(N1CC)=NC(C3=C(C)N=C(C4=NN=CN4)C=C3)=CN2
InChIKey
GMYLVKUGJMYTFB-UHFFFAOYSA-N
NCBI gene ID
2475
UniProt ID
P42345
Synonyms
RAFT1, RAPT1, FLJ44809
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTR-FRET assay (using 15 µM ATP)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26102506/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
MesoScale assay (phosphorylation of 70S6K using PC3 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/26102506/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Invitrogen’s SelectScreen™ profiling)
Selectivity platform number of targets
250
Selectivity remarks
Screened at 3 µM, closest targets as % of activity remaining: MTOR (0%), FMS (43%), full screening data are available as supplemental information, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (HTR-FRET assay): IC50(PIK3CA) = 0.852 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATM) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (HTR-FRET assay): IC50(PIK3CA) = 0.852 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATM) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/26102506/
Selectivity Number of Off-targets
0