MAP kinase interacting serine/threonine kinase 2 | MKN subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

MAP kinase interacting serine/threonine kinase 2

Target id: 2105

Nomenclature: MAP kinase interacting serine/threonine kinase 2

Abbreviated Name: Mnk2

Family: MKN subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for MAP kinase interacting serine/threonine kinase 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 414 19p13.3 MKNK2 MAP kinase interacting serine/threonine kinase 2
Mouse - 412 10 C1 Mknk2 MAP kinase-interacting serine/threonine kinase 2
Rat - 459 7 q11 Mknk2 MAP kinase-interacting serine/threonine kinase 2
Previous and Unofficial Names
G protein-coupled receptor kinase 7 | MAP kinase signal-integrating kinase 2
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human Mnk2 Kinase Domain
PDB Id:  2AC3
Resolution:  2.1Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
MELK-TI Hs Inhibition 6.1 pIC50 5
pIC50 6.1 (IC50 7.6x10-7 M) [5]
Description: Measured in a MIllipore kinase screening assay
MNK1 inhibitor Hs Inhibition 5.8 pIC50 6
pIC50 5.8 (IC50 1.6x10-6 M) [6]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: MKNK2
Ligand Sp. Type Action Affinity Units
lestaurtinib Hs Inhibitor Inhibition 8.9 pKd
AST-487 Hs Inhibitor Inhibition 8.5 pKd
foretinib Hs Inhibitor Inhibition 8.4 pKd
staurosporine Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.4 pKd
tamatinib Hs Inhibitor Inhibition 6.9 pKd
sorafenib Hs Inhibitor Inhibition 6.9 pKd
ruxolitinib Hs Inhibitor Inhibition 6.7 pKd
linifanib Hs Inhibitor Inhibition 6.6 pKd
fedratinib Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: Mnk2/MNK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 4.2 0.0 0.0
staurosporine Hs Inhibitor Inhibition 5.0 9.5 4.0
SB 218078 Hs Inhibitor Inhibition 9.7 97.0 95.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 17.2 6.0 14.0
PKR inhibitor Hs Inhibitor Inhibition 17.6 9.0 4.0
Gö 6976 Hs Inhibitor Inhibition 18.0 10.0 10.0
JAK3 inhibitor II Hs Inhibitor Inhibition 18.0 10.0 6.0
Flt-3 inhibitor III Hs Inhibitor Inhibition 18.6 21.0 7.0
BPIQ-I Hs Inhibitor Inhibition 32.2 26.0 13.0
PD 158780 Hs Inhibitor Inhibition 32.3 21.0 12.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

4. Jauch R, Jäkel S, Netter C, Schreiter K, Aicher B, Jäckle H, Wahl MC. (2005) Crystal structures of the Mnk2 kinase domain reveal an inhibitory conformation and a zinc binding site. Structure, 13 (10): 1559-68. [PMID:16216586]

5. Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA et al.. (2014) Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase. ACS Med Chem Lett, 6 (1): 25-30. [PMID:25589925]

6. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al.. (2010) Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach. J. Med. Chem., 53 (18): 6618-28. [PMID:20722422]

7. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

MKN subfamily: MAP kinase interacting serine/threonine kinase 2. Last modified on 07/11/2016. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2105.