mitogen-activated protein kinase kinase 3 | STE7 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2064

Nomenclature: mitogen-activated protein kinase kinase 3

Abbreviated Name: MKK3

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 - 347 17q11.2 MAP2K3 mitogen-activated protein kinase kinase 3
Mouse - 347 11 B2 Map2k3 mitogen-activated protein kinase kinase 3
Rat - 347 10 q22 Map2k3 mitogen activated protein kinase kinase 3
Previous and Unofficial Names
dual specificity mitogen activated protein kinase kinase 3 | MAP kinase kinase 3 | MKK3 | PRKMK3
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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
MEK inhibitor I Hs Inhibition <6.0 pIC50 2
pIC50 <6.0 (IC50 >1x10-6 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: MEK3
Ligand Sp. Type Action Value Parameter
lestaurtinib Hs Inhibitor Inhibition 8.3 pKd
staurosporine Hs Inhibitor Inhibition 8.3 pKd
PP-242 Hs Inhibitor Inhibition 7.0 pKd
tamatinib Hs Inhibitor Inhibition 7.0 pKd
KW-2449 Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.4 pKd
ruxolitinib Hs Inhibitor Inhibition 6.3 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.0 pKd
alvocidib Hs Inhibitor Inhibition 5.9 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. Wityak J, Hobbs FW, Gardner DS, Santella 3rd JB, Petraitis JJ, Sun JH, Favata MF, Daulerio AJ, Horiuchi KY, Copeland RA et al.. (2004) Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors. Bioorg. Med. Chem. Lett., 14 (6): 1483-6. [PMID:15006386]

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 3. Last modified on 17/09/2015. Accessed on 16/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2064.