Compound name
XMD17-109
Protein family
Protein Kinase
Target name
MAPK7
Affinity biochemical (nM)
162
Affinity on-target cellular (nM)
90
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000687a
SMILES
CN1CCN(C2CCN(C(C3=CC(OCC)=C(NC4=NC=C(N(C)C(C(C=CC=C5)=C5N6C7CCCC7)=O)C6=N4)C=C3)=O)CC2)CC1
InChIKey
XVBGRTMNFNMINE-UHFFFAOYSA-N
NCBI gene ID
5598
UniProt ID
Q13164
Synonyms
BMK1, ERK5
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.ejmech.2013.10.052
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
EGF-stimulated autophosphorylation of ERK5 in HeLa cells
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (Ambit)
Selectivity platform number of targets
442
Selectivity remarks
Screened at 10 µM, S(10) = 0.007, closest targets as % of contr.: DCAMK2 (3.6%), PLK4 (5.1%); Cellular selectivity profiling at 10 µM using KiNativ method, only ERK5 inhibited with90 % higher target occupancy;
Selectivity Source Knowledge
https://doi.org/10.1016/j.ejmech.2013.10.052
Selectivity Number of Off-targets
2