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Target id: 2104
Nomenclature: MAPK interacting serine/threonine kinase 1
Abbreviated Name: Mnk1
Family: MKN subfamily
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 465 | 1p33 | MKNK1 | MAPK interacting serine/threonine kinase 1 | |
Mouse | - | 427 | 4 D1 | Mknk1 | MAP kinase-interacting serine/threonine kinase 1 | |
Rat | - | 413 | 5q35 | Mknk1 | MAPK interacting serine/threonine kinase 1 |
Previous and Unofficial Names |
MAP kinase signal-integrating kinase 1 | MAP kinase interacting serine/threonine kinase 1 | MAP kinase-interacting serine/threonine kinase 1 |
Database Links | |
Alphafold | Q9BUB5 (Hs), O08605 (Mm), Q4G050 (Rn) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL4718 (Hs), CHEMBL4523120 (Mm) |
Ensembl Gene | ENSG00000079277 (Hs), ENSMUSG00000028708 (Mm), ENSRNOG00000010381 (Rn) |
Entrez Gene | 8569 (Hs), 17346 (Mm), 500526 (Rn) |
Human Protein Atlas | ENSG00000079277 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:8569 (Hs), mmu:17346 (Mm), rno:500526 (Rn) |
OMIM | 606724 (Hs) |
Pharos | Q9BUB5 (Hs) |
RefSeq Nucleotide | NM_001135553 (Hs), NM_021461 (Mm), NM_001044267 (Rn) |
RefSeq Protein | NP_001129025 (Hs), NP_067436 (Mm), NP_001037732 (Rn) |
UniProtKB | Q9BUB5 (Hs), O08605 (Mm), Q4G050 (Rn) |
Wikipedia | MKNK1 (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: 2,8 |
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Target used in screen: MKNK1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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/MNK1 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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. Garai Á, Zeke A, Gógl G, Törő I, Fördős F, Blankenburg H, Bárkai T, Varga J, Alexa A, Emig D et al.. (2012) Specificity of linear motifs that bind to a common mitogen-activated protein kinase docking groove. Sci Signal, 5 (245): ra74. [PMID:23047924]
4. Jauch R, Cho MK, Jäkel S, Netter C, Schreiter K, Aicher B, Zweckstetter M, Jäckle H, Wahl MC. (2006) Mitogen-activated protein kinases interacting kinases are autoinhibited by a reprogrammed activation segment. EMBO J, 25 (17): 4020-32. [PMID:16917500]
5. Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, Klon AE. (2010) The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity. Bioorg Med Chem Lett, 20 (22): 6394-9. [PMID:20932747]
6. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al.. (2010) Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach. J Med Chem, 53 (18): 6618-28. [PMID:20722422]
7. Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK et al.. (2018) Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition. J Med Chem, 61 (8): 3516-3540. [PMID:29526098]
8. 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]
9. Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK et al.. (2018) Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. J Med Chem, 61 (10): 4348-4369. [PMID:29683667]
10. Yuan X, Guan D, Chen C, Guo S, Wu H, Bu H, Yang CY, Wang M, Zhou J, Zhang H. (2024) Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma. J Med Chem, 67 (7): 5437-5457. [PMID:38564512]
MKN subfamily: MAPK interacting serine/threonine kinase 1. Last modified on 04/04/2024. Accessed on 11/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2104.