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mitogen-activated protein kinase 6

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Target id: 2092

Nomenclature: mitogen-activated protein kinase 6

Abbreviated Name: ERK3

Family: ERK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 721 15q21.2 MAPK6 mitogen-activated protein kinase 6
Mouse - 720 9 42.3 cM Mapk6 mitogen-activated protein kinase 6
Rat - 720 8q24 Mapk6 mitogen-activated protein kinase 6
Previous and Unofficial Names Click here for help
MAP kinase 6 | p55-MAPK | p97-MAPK | Prkm4 | PRKM6 | extracellular signal-regulated kinase 3
Database Links Click here for help
Alphafold Q16659 (Hs), Q61532 (Mm), P27704 (Rn)
BRENDA 2.7.11.24
ChEMBL Target CHEMBL5121 (Hs)
Ensembl Gene ENSG00000069956 (Hs), ENSMUSG00000042688 (Mm), ENSRNOG00000009381 (Rn)
Entrez Gene 5597 (Hs), 50772 (Mm), 58840 (Rn)
Human Protein Atlas ENSG00000069956 (Hs)
KEGG Enzyme 2.7.11.24
KEGG Gene hsa:5597 (Hs), mmu:50772 (Mm), rno:58840 (Rn)
OMIM 602904 (Hs)
Pharos Q16659 (Hs)
RefSeq Nucleotide NM_002748 (Hs), NM_015806 (Mm), NM_031622 (Rn)
RefSeq Protein NP_002739 (Hs), NP_056621 (Mm), NP_113810 (Rn)
UniProtKB Q16659 (Hs), Q61532 (Mm), P27704 (Rn)
Wikipedia MAPK6 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human mitogen activated protein kinase 6 (MAPK6)
PDB Id:  2I6L
Resolution:  2.25Å
Species:  Human
References: 
Enzyme Reaction Click here for help
EC Number: 2.7.11.24
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: ERK3
Ligand Sp. Type Action Value Parameter
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
canertinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 5.8 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 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. 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

ERK subfamily: mitogen-activated protein kinase 6. Last modified on 19/01/2015. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2092.