MAPK activated protein kinase 3 | MAPKAPK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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MAPK activated protein kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2095

Nomenclature: MAPK activated protein kinase 3

Abbreviated Name: MAPKAPK3

Family: MAPKAPK subfamily

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 382 3p21.3 MAPKAPK3 MAPK activated protein kinase 3
Mouse - 384 9 F1 Mapkapk3 mitogen-activated protein kinase-activated protein kinase 3
Rat - 384 8 q32 Mapkapk3 MAPK activated protein kinase 3
Previous and Unofficial Names
MAPKAP kinase 3 | mitogen-activated protein kinase-activated protein kinase 3
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
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:  High resolution crystal structure of mitogen-activated protein kinase-activated protein kinase 3 (MK3)-inhibitor complex
PDB Id:  3FHR
Resolution:  1.9Å
Species:  Human
References:  3
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 Value Parameter Reference
compound 16 [PMID: 17480064] Hs Inhibition 6.7 pIC50 2
pIC50 6.7 (IC50 2.1x10-7 M) [2]
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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: MAPKAP-K3/MAPKAPK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 54.7 47.0 2.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 76.0 105.0 108.0
Cdk4 inhibitor III Hs Inhibitor Inhibition 76.5 85.0 61.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 81.0 100.0 91.0
chelerythrine Hs Inhibitor Inhibition 83.0 99.0 53.0
Gö 6976 Hs Inhibitor Inhibition 83.7 131.0 77.0
staurosporine Hs Inhibitor Inhibition 85.1 97.0 44.5
Chk2 inhibitor II Hs Inhibitor Inhibition 85.3 111.0 127.0
purvalanol A Hs Inhibitor Inhibition 85.4 124.0 84.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 86.3 107.0 82.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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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. Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J. Med. Chem., 50 (11): 2647-54. [PMID:17480064]

3. Cheng R, Felicetti B, Palan S, Toogood-Johnson I, Scheich C, Barker J, Whittaker M, Hesterkamp T. (2010) High-resolution crystal structure of human Mapkap kinase 3 in complex with a high affinity ligand. Protein Sci., 19 (1): 168-73. [PMID:19937655]

4. 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]

How to cite this page

MAPKAPK subfamily: MAPK activated protein kinase 3. Last modified on 30/04/2019. Accessed on 18/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2095.