mitogen-activated protein kinase 15 | Erk7 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase 15

Target not currently curated in GtoImmuPdb

Target id: 2090

Nomenclature: mitogen-activated protein kinase 15

Abbreviated Name: ERK7

Family: Erk7 subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 544 8q24.3 MAPK15 mitogen-activated protein kinase 15
Mouse - 549 15 D3 Mapk15 mitogen-activated protein kinase 15
Rat - 547 7 q34 Mapk15 mitogen-activated protein kinase 15
Previous and Unofficial Names
ERK8 | extracellular signal regulated kinase 8 | extracellular signal-regulated kinase 7 | MAP kinase 15
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 Value Parameter Reference
BS-194 Hs Inhibition 6.5 pIC50 2
pIC50 6.5 (IC50 3.3x10-7 M) [2]
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: ERK8
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 8.3 pKd
staurosporine Hs Inhibitor Inhibition 7.5 pKd
sorafenib Hs Inhibitor Inhibition 7.3 pKd
R547 Hs Inhibitor Inhibition 7.2 pKd
foretinib Hs Inhibitor Inhibition 7.1 pKd
enzastaurin Hs Inhibitor Inhibition 7.1 pKd
ruboxistaurin Hs Inhibitor Inhibition 7.1 pKd
A-674563 Hs Inhibitor Inhibition 7.1 pKd
AST-487 Hs Inhibitor Inhibition 7.0 pKd
BMS-387032 Hs Inhibitor Inhibition 6.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0031398 positive regulation of protein ubiquitination ISO

References

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1. 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]

2. Heathcote DA, Patel H, Kroll SH, Hazel P, Periyasamy M, Alikian M, Kanneganti SK, Jogalekar AS, Scheiper B, Barbazanges M et al.. (2010) A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J. Med. Chem., 53 (24): 8508-22. [PMID:21080703]

3. 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

Erk7 subfamily: mitogen-activated protein kinase 15. Last modified on 18/02/2015. Accessed on 21/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2090.