mitogen-activated protein kinase 7 | ERK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase 7

Target not currently curated in GtoImmuPdb

Target id: 2093

Nomenclature: mitogen-activated protein kinase 7

Abbreviated Name: ERK5

Family: ERK 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 - 816 17p11.2 MAPK7 mitogen-activated protein kinase 7
Mouse - 806 11 B2 Mapk7 mitogen-activated protein kinase 7
Rat - 812 10 q23 Mapk7 mitogen-activated protein kinase 7
Previous and Unofficial Names
big MAP kinase 1 | BMK1 | MAP kinase 7 | PRKM7 | extracellular signal-regulated kinase 5
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of MAPK7 (ERK5) with inhibitor
PDB Id:  4B99
Resolution:  2.8Å
Species:  Human
References:  3
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
XMD8-92 Hs Inhibition 7.1 pKd 7
pKd 7.1 (Kd 8x10-8 M) [7]
BAY-885 Hs Inhibition 7.5 pIC50 4
pIC50 7.5 (IC50 3.5x10-8 M) [4]
Description: Biochemical inhibition of phosphorylation of a synthetic peptide substrate.
BIX02189 Hs Inhibition 7.2 pIC50 5
pIC50 7.2 (IC50 5.9x10-8 M) [5]
XMD17-109 Hs Inhibition 6.8 pIC50 2
pIC50 6.8 (IC50 1.62x10-7 M) [2]
Description: In a cell-free biochemical assay.
BIX02188 Hs Inhibition 6.1 pIC50 5
pIC50 6.1 (IC50 8.1x10-7 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: 1,6

Key to terms and symbols Click column headers to sort
Target used in screen: ERK5
Ligand Sp. Type Action Value Parameter
AT-7519 Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd
fedratinib Hs Inhibitor Inhibition 7.2 pKd
R547 Hs Inhibitor Inhibition 7.0 pKd
crizotinib Hs Inhibitor Inhibition 6.3 pKd
alvocidib Hs Inhibitor Inhibition 6.2 pKd
BMS-345541 Hs Inhibitor Inhibition 6.2 pKd
BMS-387032 Hs Inhibitor Inhibition 6.2 pKd
lestaurtinib Hs Inhibitor Inhibition 6.0 pKd
staurosporine Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0050728 negative regulation of inflammatory response TAS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0050728 negative regulation of inflammatory response TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0060761 negative regulation of response to cytokine stimulus IGI

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. Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD et al.. (2013) Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem, 70: 758-67. [PMID:24239623]

3. Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J. Med. Chem., 56 (11): 4413-21. [PMID:23656407]

4. Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C et al.. (2019) Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5. J. Med. Chem., 62 (2): 928-940. [PMID:30563338]

5. Tatake RJ, O'Neill MM, Kennedy CA, Wayne AL, Jakes S, Wu D, Kugler Jr SZ, Kashem MA, Kaplita P, Snow RJ. (2008) Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem. Biophys. Res. Commun., 377 (1): 120-5. [PMID:18834865]

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]

7. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell, 18 (3): 258-67. [PMID:20832753]

How to cite this page

ERK subfamily: mitogen-activated protein kinase 7. Last modified on 16/01/2019. Accessed on 02/06/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2093.