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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 822 | 5q21.3 | FER | FER tyrosine kinase | |
Mouse | - | 823 | 17 E1.1 | Fer | FER tyrosine kinase | |
Rat | - | 823 | 9q37 | Fer | FER tyrosine kinase |
Database Links | |
Alphafold | P16591 (Hs), P70451 (Mm), P09760 (Rn) |
BRENDA | 2.7.10.2 |
CATH/Gene3D | 3.30.505.10 |
ChEMBL Target | CHEMBL3982 (Hs), CHEMBL4523172 (Rn) |
Ensembl Gene | ENSG00000151422 (Hs), ENSMUSG00000000127 (Mm), ENSRNOG00000015898 (Rn) |
Entrez Gene | 2241 (Hs), 14158 (Mm), 301737 (Rn) |
Human Protein Atlas | ENSG00000151422 (Hs) |
KEGG Enzyme | 2.7.10.2 |
KEGG Gene | hsa:2241 (Hs), mmu:14158 (Mm), rno:301737 (Rn) |
OMIM | 176942 (Hs) |
Pharos | P16591 (Hs) |
RefSeq Nucleotide | NM_005246 (Hs), NM_001037997 (Mm), NM_001106928 (Rn) |
RefSeq Protein | NP_005237 (Hs), NP_001033086 (Mm), NP_001100398 (Rn) |
UniProtKB | P16591 (Hs), P70451 (Mm), P09760 (Rn) |
Wikipedia | FER (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: 3,8 |
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Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: FER | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 1,4 |
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Target used in screen: Fer/FER | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
FER acts downstream of the activated high affinity immunoglobulin epsilon receptor (FCεR1) and plays a role in FCεR1-mediated signaling in mast cells, regulation of mast cell degranulation, leukocyte recruitment, and leukocyte extravasation following bacterial lipopolysaccharide (LPS) exposure. |
Cell Type Associations | ||||
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Immuno Process Associations | ||
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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. Chen S, Bartkovitz D, Cai J, Chen Y, Chen Z, Chu XJ, Le K, Le NT, Luk KC, Mischke S et al.. (2012) Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett, 22 (2): 1247-50. [PMID:22172702]
3. 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]
4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]
5. Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD et al.. (2012) Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem, 55 (10): 4580-93. [PMID:22564207]
6. Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN et al.. (2014) Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. J Med Chem, 57 (4): 1170-87. [PMID:24432909]
7. Taniguchi T, Inagaki H, Baba D, Yasumatsu I, Toyota A, Kaneta Y, Kiga M, Iimura S, Odagiri T, Shibata Y et al.. (2019) Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity. ACS Med Chem Lett, 10 (5): 737-742. DOI: 10.1021/acsmedchemlett.8b00631 [PMID:31097992]
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]
Fer family: FER tyrosine kinase. Last modified on 23/04/2019. Accessed on 02/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2022.