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Target not currently curated in GtoImmuPdb
Target id: 2077
Nomenclature: mitogen-activated protein kinase kinase kinase 2
Abbreviated Name: MEKK2
Family: STE11 family
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 619 | 2q14.3 | MAP3K2 | mitogen-activated protein kinase kinase kinase 2 | |
Mouse | - | 619 | 18 B1 | Map3k2 | mitogen-activated protein kinase kinase kinase 2 | |
Rat | - | 619 | 18 p12 | Map3k2 | mitogen activated protein kinase kinase kinase 2 |
Previous and Unofficial Names |
MAP/ERK kinase kinase 2 | MAPKKK2 | MEK kinase 2 |
Database Links | |
Alphafold | Q9Y2U5 (Hs), Q61083 (Mm) |
BRENDA | 2.7.11.25 |
ChEMBL Target | CHEMBL5914 (Hs) |
Ensembl Gene | ENSG00000169967 (Hs), ENSMUSG00000024383 (Mm), ENSRNOG00000014089 (Rn) |
Entrez Gene | 10746 (Hs), 26405 (Mm), 171492 (Rn) |
Human Protein Atlas | ENSG00000169967 (Hs) |
KEGG Enzyme | 2.7.11.25 |
KEGG Gene | hsa:10746 (Hs), mmu:26405 (Mm), rno:171492 (Rn) |
OMIM | 609487 (Hs) |
Pharos | Q9Y2U5 (Hs) |
RefSeq Nucleotide | NM_006609 (Hs), NM_011946 (Mm), NM_138503 (Rn) |
RefSeq Protein | NP_006600 (Hs), NP_036076 (Mm), NP_612512 (Rn) |
UniProtKB | Q9Y2U5 (Hs), Q61083 (Mm) |
Wikipedia | MAP3K2 (Hs) |
Selected 3D Structures | |||||||||||
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Enzyme Reaction | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||
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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: 2,4 |
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Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: MAP3K2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: ...1 |
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Target used in screen: nd/MEKK2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]
2. 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]
3. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem, 56 (20): 8032-48. [PMID:24044867]
4. 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]
STE11 family: mitogen-activated protein kinase kinase kinase 2. Last modified on 18/02/2015. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2077.