Compound name
XMD8-92
Protein family
Protein Kinase
Target name
MAPK7
Affinity biochemical (nM)
80
Affinity on-target cellular (nM)
1500
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000122b
SMILES
OC1CCN(C2=CC(OCC)=C(NC3=NC=C(N(C)C(C(C=CC=C4)=C4N5C)=O)C5=N3)C=C2)CC1
InChIKey
QAPAJIZPZGWAND-UHFFFAOYSA-N
NCBI gene ID
5598
UniProt ID
Q13164
Synonyms
BMK1, ERK5
Mode of action
Inhibitor
Affinity biochemical definition
KD
Affinity biochemical assay type
ATP-binding displacement assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.ccr.2010.08.008
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
KiNativ assay (HeLa cell lysate)
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel, literature
Selectivity platform number of targets
402
Selectivity remarks
Screened at 10 µM, ATP-site competition binding assay, S(10) = 0.012, closest targets: Kd(BMK1) = 80 nM, Kd(DCAMKL2) = 190 nM, Kd(TNK1) = 890 nM, Kd(PLK4) = 600 nM; Cellular selectivity profiling using KiNativ method against 181 kinases in HeLa cells, closest targets: IC50(TNK1/2) = 10/ 18 µM, IC50(RSK1/2) = 29/ 47 µM, IC50(FAK) = 39 µM, IC50(PIK4CA/L) = 36 µM, others >50 µM;
Selectivity Source Knowledge
https://doi.org/10.1016/j.ccr.2010.08.008
Selectivity Number of Off-targets
3