EUB0000250b_MAPK7

Chemical structure of compound EUB0000250b
Compound name
BAY-885
Protein family
Protein Kinase
Target name
MAPK7
Affinity biochemical (nM)
35
Affinity on-target cellular (nM)
115
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000250b
SMILES
CN1CCN(c2cnc3c(C4CCN(C(=O)c5ccc(OC(F)(F)F)cc5N)CC4)ncnc3c2)CC1
InChIKey
QXURFIGBRGWPQD-UHFFFAOYSA-N
NCBI gene ID
5598
UniProt ID
Q13164
Synonyms
BMK1, ERK5
Mode of action
Inhibitor
Negative control
BAY-693
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay (250 µM ATP)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acs.jmedchem.8b01606
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-885
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cellular luciferase reporter assay (using the SN12C-MEF2-luc cell line and ONE-Glo)
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (Eurofins)
Selectivity platform number of targets
358
Selectivity remarks
Screened at 1 µM, closest targets as % of contr.: FER (38%), EPHB3 (42%), EPHA5 (57%); Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: EPHB6 (18%), EGFR(S752-I759del) (38%), LTK (49%); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki(SIGMAR1) = 2.50 µM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-885
Selectivity Number of Off-targets
0