Top ▲

GtoPdb is requesting financial support from commercial users. Please see our sustainability page for more information.

mitogen-activated protein kinase kinase kinase 4

Click here for help

Target id: 2079

Nomenclature: mitogen-activated protein kinase kinase kinase 4

Abbreviated Name: MEKK4

Family: STE11 family

Contents:

Gene and Protein Information Click here for help
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 Click here for help
MAP three kinase 1 | MAPK/ERK kinase kinase 4 | MAPKKK4 | MTK1 | RP17 | Tas
Database Links Click here for help
Alphafold Q9Y6R4 (Hs), O08648 (Mm)
BRENDA 2.7.11.25
ChEMBL Target CHEMBL4853 (Hs)
Ensembl Gene ENSG00000085511 (Hs), ENSMUSG00000014426 (Mm), ENSRNOG00000017419 (Rn)
Entrez Gene 4216 (Hs), 26407 (Mm), 308106 (Rn)
Human Protein Atlas ENSG00000085511 (Hs)
KEGG Enzyme 2.7.11.25
KEGG Gene hsa:4216 (Hs), mmu:26407 (Mm), rno:308106 (Rn)
OMIM 602425 (Hs)
Pharos Q9Y6R4 (Hs)
RefSeq Nucleotide NM_005922 (Hs), NM_011948 (Mm), NM_001107456 (Rn)
RefSeq Protein NP_005913 (Hs), NP_036078 (Mm), NP_001100926 (Rn)
UniProtKB Q9Y6R4 (Hs), O08648 (Mm)
Wikipedia MAP3K4 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.25
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: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: MAP3K4
Ligand Sp. Type Action Value Parameter
neratinib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 7.4 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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 25/10/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2079.