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Target id: 2099
Nomenclature: microtubule affinity regulating kinase 3
Abbreviated Name: MARK3
Family: MARK subfamily
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 753 | 14q32.32-q32.33 | MARK3 | microtubule affinity regulating kinase 3 | |
Mouse | - | 753 | 12 F1 | Mark3 | MAP/microtubule affinity regulating kinase 3 | |
Rat | - | 797 | 6q32 | Mark3 | microtubule affinity regulating kinase 3 |
Previous and Unofficial Names ![]() |
CTAK1 | Cdc25C-associated protein kinase 1 | ELKL motif kinase 2 | EMK2 | Par-1a | Protein kinase STK10 | MAP/microtubule affinity-regulating kinase 3 |
Database Links ![]() |
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Alphafold | P27448 (Hs), Q03141 (Mm), Q8VHF0 (Rn) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL5600 (Hs) |
Ensembl Gene | ENSG00000075413 (Hs), ENSMUSG00000007411 (Mm), ENSRNOG00000010330 (Rn) |
Entrez Gene | 4140 (Hs), 17169 (Mm), 170577 (Rn) |
Human Protein Atlas | ENSG00000075413 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:4140 (Hs), mmu:17169 (Mm), rno:170577 (Rn) |
OMIM | 602678 (Hs) |
Pharos | P27448 (Hs) |
RefSeq Nucleotide | NM_001128918 (Hs), NM_021516 (Mm), NM_130749 (Rn) |
RefSeq Protein | NP_001122390 (Hs), NP_067491 (Mm), NP_570105 (Rn) |
UniProtKB | P27448 (Hs), Q03141 (Mm), Q8VHF0 (Rn) |
Wikipedia | MARK3 (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 ![]() |
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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: MARK3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 ![]() |
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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/MARK3 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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. Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD. (2022) Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. J Med Chem, 65 (2): 1313-1328. [PMID:34333981]
4. Li F, Liu Z, Sun H, Li C, Wang W, Ye L, Yan C, Tian J, Wang H. (2020) PCC0208017, a novel small-molecule inhibitor of MARK3/MARK4, suppresses glioma progression in vitro and in vivo. Acta Pharm Sin B, 10 (2): 289-300. [PMID:32082974]
5. McIver EG, Bryans J, Birchall K, Chugh J, Drake T, Lewis SJ, Osborne J, Smiljanic-Hurley E, Tsang W, Kamal A et al.. (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases. Bioorg Med Chem Lett, 22 (23): 7169-73. [PMID:23099093]
6. Murphy JM, Korzhnev DM, Ceccarelli DF, Briant DJ, Zarrine-Afsar A, Sicheri F, Kay LE, Pawson T. (2007) Conformational instability of the MARK3 UBA domain compromises ubiquitin recognition and promotes interaction with the adjacent kinase domain. Proc Natl Acad Sci USA, 104 (36): 14336-41. [PMID:17726107]
7. Shi YQ, Sun ZH, Wang ZZ, Su CY, Zhang W, Yu LY, Xu Y, Gao YL, Wang HB, Tian JW et al.. (2023) A novel role for microtubule affinity-regulating kinases in neuropathic pain. Br J Pharmacol, [Epub ahead of print]. [PMID:38112022]
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]
MARK subfamily: microtubule affinity regulating kinase 3. Last modified on 12/03/2024. Accessed on 20/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2099.