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Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 1 | 976 | 7q34-q35 | EPHA1 | EPH receptor A1 | |
Mouse | 1 | 977 | 6 B2.1 | Epha1 | Eph receptor A1 | |
Rat | - | 977 | 4q23 | Epha1 | Eph receptor A1 |
Previous and Unofficial Names ![]() |
EPHT1 | ephrin type-A receptor 1 | Embryonic stem cell kinase | tyrosine-protein kinase receptor ESK | Esk |
Database Links ![]() |
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Alphafold | P21709 (Hs), Q60750 (Mm) |
BRENDA | 2.7.10.1 |
CATH/Gene3D | 2.60.120.260, 2.60.40.10 |
ChEMBL Target | CHEMBL5810 (Hs) |
Ensembl Gene | ENSG00000146904 (Hs), ENSMUSG00000029859 (Mm), ENSRNOG00000017525 (Rn) |
Entrez Gene | 2041 (Hs), 13835 (Mm), 312279 (Rn) |
Human Protein Atlas | ENSG00000146904 (Hs) |
KEGG Enzyme | 2.7.10.1 |
KEGG Gene | hsa:2041 (Hs), mmu:13835 (Mm), rno:312279 (Rn) |
OMIM | 179610 (Hs) |
Pharos | P21709 (Hs) |
RefSeq Nucleotide | NM_005232 (Hs), NM_023580 (Mm), NM_001107858 (Rn) |
RefSeq Protein | NP_005223 (Hs), NP_076069 (Mm), NP_001101328 (Rn) |
UniProtKB | P21709 (Hs), Q60750 (Mm) |
Wikipedia | EPHA1 (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: 2,6 |
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Target used in screen: EPHA1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 1,3 |
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Target used in screen: EphA1/EPHA1 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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. 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]
4. Incerti M, Tognolini M, Russo S, Pala D, Giorgio C, Hassan-Mohamed I, Noberini R, Pasquale EB, Vicini P, Piersanti S et al.. (2013) Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor. J Med Chem, 56 (7): 2936-47. [PMID:23489211]
5. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J Med Chem, 52 (20): 6433-46. [PMID:19788238]
6. 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]
Type XIII RTKs: Ephrin receptor family: EPH receptor A1. Last modified on 10/07/2018. Accessed on 20/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1821.