mitogen-activated protein kinase 12 | p38 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

mitogen-activated protein kinase 12

Target id: 1501

Nomenclature: mitogen-activated protein kinase 12

Abbreviated Name: p38γ

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 12 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 367 22q13.3 MAPK12 mitogen-activated protein kinase 12
Mouse - 367 15 Mapk12 mitogen-activated protein kinase 12
Rat - 367 7q34 Mapk12 mitogen-activated protein kinase 12
Previous and Unofficial Names
ERK5 | SAPK3 | extracellular signal-regulated kinase 6 | MAP kinase 12 | MAP kinase p38 gamma | MAPK 12 | mitogen-activated protein kinase p38 gamma | SAP kinase-3 | stress-activated protein kinase 3 | ERK6 | p38gamma | PRKM12
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:  PHOSPHORYLATED MAP KINASE P38-GAMMA
PDB Id:  1CM8
Resolution:  2.4Å
Species:  Human
References:  2
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
doramapimod Hs Inhibition 7.5 pIC50 5
pIC50 7.5 (IC50 3x10-8 M) [5]
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: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: p38-gamma
Ligand Sp. Type Action Affinity Units
doramapimod Hs Inhibitor Inhibition 8.5 pKd
AST-487 Hs Inhibitor Inhibition 7.5 pKd
staurosporine Hs Inhibitor Inhibition 7.4 pKd
lestaurtinib Hs Inhibitor Inhibition 6.4 pKd
tamatinib Hs Inhibitor Inhibition 6.4 pKd
foretinib Hs Inhibitor Inhibition 6.4 pKd
SB203580 Hs Inhibitor Inhibition 5.8 pKd
linifanib Hs Inhibitor Inhibition 5.7 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: SAPK3/P38g
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
VEGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 61.9
DNA-PK inhibitor III Hs Inhibitor Inhibition 78.7 110.0 102.0
Gö 6983 Hs Inhibitor Inhibition 84.8 100.0 100.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 85.2 96.0 69.0
GSK-3 inhibitor X Hs Inhibitor Inhibition 85.2 94.0 92.0
Gö 6976 Hs Inhibitor Inhibition 85.8 61.0 61.0
isogranulatimide Hs Inhibitor Inhibition 85.9 95.0 87.0
PP1 analog II Hs Inhibitor Inhibition 86.6 100.0 98.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 86.8 103.0 91.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 86.8 103.0 91.0
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. Bellon S, Fitzgibbon MJ, Fox T, Hsiao HM, Wilson KP. (1999) The structure of phosphorylated p38gamma is monomeric and reveals a conserved activation-loop conformation. Structure, 7 (9): 1057-65. [PMID:10508788]

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. 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]

6. 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 12. Last modified on 18/02/2015. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1501.