mitogen-activated protein kinase 13 | p38 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

mitogen-activated protein kinase 13

Target id: 1502

Nomenclature: mitogen-activated protein kinase 13

Abbreviated Name: p38δ

Family: p38 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 mitogen-activated protein kinase 13 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 365 6p21 MAPK13 mitogen-activated protein kinase 13
Mouse - 366 17 A3-B Mapk13 mitogen-activated protein kinase 13
Rat - 366 20p12 Mapk13 mitogen activated protein kinase 13
Previous and Unofficial Names
SAPK4 | MAP kinase 13 | MAP kinase p38 delta | MAPK 13 | mitogen-activated protein kinase p38 delta | stress-activated protein kinase 4 | Serk4 | p38 delta MAP kinase | p38delta | PRKM13
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:  Crystal structure of p38delta kinase
PDB Id:  3COI
Resolution:  2.09Å
Species:  Human
References: 
Image of receptor 3D structure from RCSB PDB
Description:  MAPK13 Complex with inhibitor
PDB Id:  4EYJ
Resolution:  2.1Å
Species:  Human
References:  1
Enzyme Reaction
EC Number: 2.7.11.24

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
PF-03715455 Hs Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.3x10-8 M) [5]
doramapimod Hs Inhibition 6.5 pIC50 6
pIC50 6.5 (IC50 3x10-7 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: 3,7

Key to terms and symbols Click column headers to sort
Target used in screen: p38-delta
Ligand Sp. Type Action Affinity Units
AST-487 Hs Inhibitor Inhibition 7.9 pKd
foretinib Hs Inhibitor Inhibition 7.3 pKd
doramapimod Hs Inhibitor Inhibition 7.1 pKd
staurosporine Hs Inhibitor Inhibition 6.6 pKd
tamatinib Hs Inhibitor Inhibition 6.2 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: SAPK4/P38d(MAPK13)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 77.1 43.0 46.0
staurosporine Hs Inhibitor Inhibition 86.6 21.5 3.5
GSK-3 inhibitor IX Hs Inhibitor Inhibition 87.5 89.0 92.0
vatalanib Hs Inhibitor Inhibition 88.9
tozasertib Hs Inhibitor Inhibition 89.5
AG 1296 Hs Inhibitor Inhibition 89.6 116.0 105.0
dovitinib Hs Inhibitor Inhibition 90.4
PKR inhibitor Hs Inhibitor Inhibition 90.4 62.0 24.0
nilotinib Hs Inhibitor Inhibition 90.7
GSK-3beta inhibitor VIII Hs Inhibitor Inhibition 91.1 96.0 89.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Alevy YG, Patel AC, Romero AG, Patel DA, Tucker J, Roswit WT, Miller CA, Heier RF, Byers DE, Brett TJ et al.. (2012) IL-13-induced airway mucus production is attenuated by MAPK13 inhibition. J. Clin. Invest., 122 (12): 4555-68. [PMID:23187130]

2. 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]

3. 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]

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]

5. Millan DS, Bunnage ME, Burrows JL, Butcher KJ, Dodd PG, Evans TJ, Fairman DA, Hughes SJ, Kilty IC, Lemaitre A et al.. (2011) Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. J. Med. Chem., 54 (22): 7797-814. [PMID:21888439]

6. Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M et al.. (2011) Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). Bioorg. Med. Chem. Lett., 21 (23): 7155-65. [PMID:22014550]

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

p38 subfamily: mitogen-activated protein kinase 13. Last modified on 18/02/2015. Accessed on 16/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1502.