mitogen-activated protein kinase kinase 5 | STE7 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase 5

Target not currently curated in GtoImmuPdb

Target id: 2066

Nomenclature: mitogen-activated protein kinase kinase 5

Abbreviated Name: MEK5

Family: STE7 family

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 - 483 15q22.31 MAP2K5 mitogen-activated protein kinase kinase 5
Mouse - 448 9 C Map2k5 mitogen-activated protein kinase kinase 5
Rat - 448 8 q24 Map2k5 mitogen activated protein kinase kinase 5
Previous and Unofficial Names
dual specificity mitogen-activated protein kinase kinase 5 | MAP kinase kinase 5 | MAPKK5 | PRKMK5
Database Links
BRENDA
ChEMBL Target
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 the complex of human mitogen activated protein kinase kinase 5 phox domain (MAP2K5-phox) with human mitogen activated protein kinase kinase kinase 2 phox domain (MAP3K2-phox)
PDB Id:  2NPT
Resolution:  1.75Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.12.2

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
BIX02189 Hs Inhibition 8.8 pIC50 2
pIC50 8.8 (IC50 1.5x10-9 M) [2]
BIX02188 Hs Inhibition 8.4 pIC50 2
pIC50 8.4 (IC50 4.3x10-9 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: MEK5
Ligand Sp. Type Action Value Parameter
PLX-4720 Hs Inhibitor Inhibition 9.8 pKd
foretinib Hs Inhibitor Inhibition 8.6 pKd
barasertib-hQPA Hs Inhibitor Inhibition 8.6 pKd
staurosporine Hs Inhibitor Inhibition 8.5 pKd
dasatinib Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
PP-242 Hs Inhibitor Inhibition 8.1 pKd
Ki-20227 Hs Inhibitor Inhibition 8.1 pKd
bosutinib Hs Inhibitor Inhibition 8.1 pKd
dovitinib Hs Inhibitor Inhibition 7.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

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. 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]

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

STE7 family: mitogen-activated protein kinase kinase 5. Last modified on 09/11/2016. Accessed on 21/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2066.