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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 961 | 2p13.3 | AAK1 | AP2 associated kinase 1 | |
Mouse | - | 959 | 6 37.75 cM | Aak1 | AP2 associated kinase 1 | |
Rat | - | 962 | 4q34 | Aak1 | AP2 associated kinase 1 |
Previous and Unofficial Names |
adaptor-associated kinase 1 | LMTK1 |
Database Links | |
Alphafold | Q2M2I8 (Hs), Q3UHJ0 (Mm), P0C1X8 (Rn) |
BRENDA | 2.7.11.1 |
CATH/Gene3D | 2.130.10.10 |
ChEMBL Target | CHEMBL3830 (Hs) |
Ensembl Gene | ENSG00000115977 (Hs), ENSMUSG00000057230 (Mm), ENSRNOG00000018317 (Rn) |
Entrez Gene | 22848 (Hs), 269774 (Mm), 500244 (Rn) |
Human Protein Atlas | ENSG00000115977 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:22848 (Hs), mmu:269774 (Mm), rno:500244 (Rn) |
Pharos | Q2M2I8 (Hs) |
RefSeq Nucleotide | NM_014911 (Hs), NM_001040106 (Mm), NM_001173450 (Rn) |
RefSeq Protein | NP_055726 (Hs), NP_001035195 (Mm), NP_001166921 (Rn) |
UniProtKB | Q2M2I8 (Hs), Q3UHJ0 (Mm), P0C1X8 (Rn) |
Wikipedia | AAK1 (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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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: 1,7 |
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Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: AAK1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immuno Process Associations | ||
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General Comments |
Selective inhibition of AAK1 has validated it as a viable target for treating neuropathic pain [3]. It is also an antiviral drug target. Its inhibition by small molecules has the potential to offer promising broad-spectrum antiviral activity [6]. |
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. 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]
3. Hartz RA, Ahuja VT, Nara SJ, Kumar CMV, Brown JM, Bristow LJ, Rajamani R, Muckelbauer JK, Camac D, Kiefer SE et al.. (2021) Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain. J Med Chem, 64 (15): 11090-11128. [PMID:34270254]
4. Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S et al.. (2022) Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain. J Med Chem, 65 (6): 4534-4564. [PMID:35261239]
5. Stebbing J, Phelan A, Griffin I, Tucker C, Oechsle O, Smith D, Richardson P. (2020) COVID-19: combining antiviral and anti-inflammatory treatments. Lancet Infect Dis, 20 (4): 400-402. [PMID:32113509]
6. Verdonck S, Pu SY, Sorrell FJ, Elkins JM, Froeyen M, Gao LJ, Prugar LI, Dorosky DE, Brannan JM, Barouch-Bentov R et al.. (2019) Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. J Med Chem, 62 (12): 5810-5831. [PMID:31136173]
7. 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]
NAK family: AP2 associated kinase 1. Last modified on 29/03/2022. Accessed on 02/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1921.