mitogen-activated protein kinase kinase kinase 4 | STE11 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 4

Target not currently curated in GtoImmuPdb

Target id: 2079

Nomenclature: mitogen-activated protein kinase kinase kinase 4

Abbreviated Name: MEKK4

Family: STE11 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 - 1608 6q26 MAP3K4 mitogen-activated protein kinase kinase kinase 4
Mouse - 1597 17 A1 Map3k4 mitogen-activated protein kinase kinase kinase 4
Rat - 1387 1 q11 Map3k4 mitogen activated protein kinase kinase kinase 4
Previous and Unofficial Names
MAP three kinase 1 | MAPK/ERK kinase kinase 4 | MAPKKK4 | MTK1 | RP17 | Tas
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: 2.7.11.25
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: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: MAP3K4
Ligand Sp. Type Action Value Parameter
neratinib Hs Inhibitor Inhibition 7.4 pKd
PD-173955 Hs Inhibitor Inhibition 7.3 pKd
bosutinib Hs Inhibitor Inhibition 7.0 pKd
dasatinib Hs Inhibitor Inhibition 6.5 pKd
tamatinib Hs Inhibitor Inhibition 6.1 pKd
staurosporine Hs Inhibitor Inhibition 5.9 pKd
KW-2449 Hs Inhibitor Inhibition 5.8 pKd
PHA-665752 Hs Inhibitor Inhibition 5.7 pKd
foretinib Hs Inhibitor Inhibition 5.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.7 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. 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

STE11 family: mitogen-activated protein kinase kinase kinase 4. Last modified on 18/08/2014. Accessed on 18/06/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2079.