Compound name
PF 3644022
Protein family
Protein Kinase
Target name
MAPKAPK2
Affinity biochemical (nM)
5
Affinity on-target cellular (nM)
201
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000056c
SMILES
O=C(N[C@H](C)CN4)C3=C4C1=C(S3)C=CC2=C1C=CC(C5=CC=C(C)N=C5)=N2
InChIKey
CMWRPDHVGMHLSZ-GFCCVEGCSA-N
NCBI gene ID
9261
UniProt ID
P49137
Synonyms
MK2
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic activity assay (Ustate kinase profiler Service; Millipore)
Affinity Biochemical Source Knowledge
https://doi.org/10.1124/jpet.110.166173
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot (phosphorylation of the MK2 substrate HSP27 in U937 cells)
Affinity on-target cellular relation
=
Selectivity platform
Upstate Kinase Profiler service (Millipore)
Selectivity platform number of targets
170
Selectivity remarks
Screened at 1 µM, closest targets: IC50(AMPK) = 117 nM, IC50(BRSK1) = 187 nM, IC50(BRSK2) = 90 nM, IC50(CAMK2B) = 70 nM, IC50(DRAK1) = 71 nM, IC50(MNK2) = 148 nM, IC50(PHKG2) = 528 nM , IC50(PIM1) = 88 nM ,IC50(CDK1) = 354 nM, IC50(CDK5) = 902 nM, IC50(MAP3K5) = 60 nM, IC50(AXL) = 428 nM, IC50(MERTK) = 76 nM, IC50(RIPK2) = 590 nM;
Selectivity Source Knowledge
https://doi.org/10.1124/jpet.110.166173
Selectivity Number of Off-targets
6