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mitogen-activated protein kinase 15

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Target id: 2090

Nomenclature: mitogen-activated protein kinase 15

Abbreviated Name: ERK7

Family: Erk7 subfamily

Contents:

Gene and Protein Information Click here for help
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 7q34 Mapk15 mitogen-activated protein kinase 15
Previous and Unofficial Names Click here for help
ERK8 | extracellular signal regulated kinase 8 | extracellular signal-regulated kinase 7 | MAP kinase 15
Database Links Click here for help
Alphafold Q8TD08 (Hs), Q80Y86 (Mm), Q9Z2A6 (Rn)
BRENDA 2.7.11.24
ChEMBL Target CHEMBL5198 (Hs)
Ensembl Gene ENSG00000181085 (Hs), ENSMUSG00000063704 (Mm), ENSRNOG00000009336 (Rn)
Entrez Gene 225689 (Hs), 332110 (Mm), 286997 (Rn)
Human Protein Atlas ENSG00000181085 (Hs)
KEGG Enzyme 2.7.11.24
KEGG Gene hsa:225689 (Hs), mmu:332110 (Mm), rno:286997 (Rn)
Pharos Q8TD08 (Hs)
RefSeq Nucleotide NM_139021 (Hs), NM_177922 (Mm), NM_173331 (Rn)
RefSeq Protein NP_620590 (Hs), NP_808590 (Mm), NP_775453 (Rn)
UniProtKB Q8TD08 (Hs), Q80Y86 (Mm), Q9Z2A6 (Rn)
Wikipedia MAPK15 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.24

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BS-194 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.5 pIC50 2
⤷ pIC50 6.5 (IC50 3.3x10-7 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure 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

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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2090.