Compound name
Trametinib
Protein family
Protein Kinase
Target name
MAP2K2
Affinity biochemical (nM)
0.92
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000124b
SMILES
CC(NC1=CC(N2C(C(C(N(C3CC3)C2=O)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C(C)C5=O)=CC=C1)=O
InChIKey
LIRYPHYGHXZJBZ-UHFFFAOYSA-N
NCBI gene ID
5605
UniProt ID
P36507
Synonyms
MEK2
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
ELISA (Raf-MEK-ERK cascade kinase assay, activated with c-Raf, 10 µM ATP)
Affinity Biochemical Source Knowledge
https://www.spandidos-publications.com/10.3892/ijo.2011.1015
Affinity biochemical relation
=
Selectivity platform
Millipor'e kinase profiler
Selectivity platform number of targets
99
Selectivity remarks
Screened at 10 µM, closest targets as % of contr.: NTRK1 (59%); Screened against 300 proteins in Kinobeads assays, in-vitro potencies of closest targets: Kdapp(BRD4) = 1915 nM, Kdapp(MAP2K1) = 62 nM, Kdapp(MAP2K2) = 9 nM (https://www.science.org/doi/10.1126/science.aan4368)
Selectivity Source Knowledge
https://www.spandidos-publications.com/10.3892/ijo.2011.1015