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Target id: 2289
Nomenclature: ZAK sterile alpha motif and leucine zipper containing kinase AZK
Abbreviated Name: ZAK
Family: MLK subfamily
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 800 | 2q31.1 | MAP3K20 | mitogen-activated protein kinase kinase kinase 20 | |
Mouse | - | 802 | 2 C3 | Map3k20 | mitogen-activated protein kinase kinase kinase 20 | |
Rat | - | 802 | 3q22 | Map3k20 | mitogen-activated protein kinase kinase kinase 20 |
Database Links ![]() |
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Alphafold | Q9NYL2 (Hs), Q9ESL4 (Mm) |
BRENDA | 2.7.11.25 |
ChEMBL Target | CHEMBL3886 (Hs), CHEMBL4523452 (Mm) |
Ensembl Gene | ENSG00000091436 (Hs), ENSMUSG00000004085 (Mm), ENSRNOG00000001515 (Rn) |
Entrez Gene | 51776 (Hs), 65964 (Mm), 311743 (Rn) |
Human Protein Atlas | ENSG00000091436 (Hs) |
KEGG Enzyme | 2.7.11.25 |
KEGG Gene | hsa:51776 (Hs), mmu:65964 (Mm), rno:311743 (Rn) |
OMIM | 609479 (Hs) |
Pharos | Q9NYL2 (Hs) |
RefSeq Nucleotide | NM_016653 (Hs), NM_023057 (Mm), XM_002729174 (Rn) |
RefSeq Protein | NP_057737 (Hs), NP_075544 (Mm), XP_001059755 (Rn) |
UniProtKB | Q9NYL2 (Hs), Q9ESL4 (Mm) |
Wikipedia | MAP3K20 (Hs) |
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: 2,4 |
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Target used in screen: ZAK | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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/ZAK(MLTK) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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. Li HY, Wang Y, Heap CR, King CH, Mundla SR, Voss M, Clawson DK, Yan L, Campbell RM, Anderson BD et al.. (2006) Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7. J Med Chem, 49 (6): 2138-42. [PMID:16539403]
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]
5. Yang J, Shibu MA, Kong L, Luo J, BadrealamKhan F, Huang Y, Tu ZC, Yun CH, Huang CY, Ding K et al.. (2020) Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors. J Med Chem, 63 (5): 2114-2130. [PMID:31244114]
6. Zhou Y, Yu H, Vind AC, Kong L, Liu Y, Song X, Tu Z, Yun C, Smaill JB, Zhang QW et al.. (2023) Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov). J Med Chem, 66 (11): 7405-7420. [PMID:37220641]
MLK subfamily: ZAK sterile alpha motif and leucine zipper containing kinase AZK. Last modified on 02/08/2023. Accessed on 20/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2289.