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Target not currently curated in GtoImmuPdb
Target id: 1933
Nomenclature: A-Raf proto-oncogene, serine/threonine kinase
Abbreviated Name: A-Raf
Family: RAF family
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 606 | Xp11.3 | ARAF | A-Raf proto-oncogene, serine/threonine kinase | |
Mouse | - | 604 | X 16.3 cM | Araf | Araf proto-oncogene, serine/threonine kinase | |
Rat | - | 604 | Xq11 | Araf | A-Raf proto-oncogene, serine/threonine kinase |
Previous and Unofficial Names ![]() |
ARAF1 | proto-oncogene A-Raf-1 | Raf related protein | Ras-binding protein | A-Raf proto-oncogene | Araf proto-oncogene, serine/threonine kinase | Araf proto-oncogene |
Database Links ![]() |
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Alphafold | P10398 (Hs), P04627 (Mm), P14056 (Rn) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL1169596 (Hs) |
Ensembl Gene | ENSG00000078061 (Hs), ENSMUSG00000001127 (Mm), ENSRNOG00000010838 (Rn) |
Entrez Gene | 369 (Hs), 11836 (Mm), 64363 (Rn) |
Human Protein Atlas | ENSG00000078061 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:369 (Hs), mmu:11836 (Mm), rno:64363 (Rn) |
OMIM | 311010 (Hs) |
Pharos | P10398 (Hs) |
RefSeq Nucleotide | NM_001256196 (Hs), NM_009703 (Mm), NM_022532 (Rn) |
RefSeq Protein | NP_001645 (Hs), NP_033833 (Mm), NP_071977 (Rn) |
UniProtKB | P10398 (Hs), P04627 (Mm), P14056 (Rn) |
Wikipedia | ARAF (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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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/ARAF | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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. Chen YK, Kanouni T, Arnold LD, Cox JM, Gardiner E, Grandinetti K, Jiang P, Kaldor SW, Lee C, Li C et al.. (2024) The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition. J Med Chem,. DOI: 10.1021/acs.jmedchem.3c01830
3. Peng SB, Henry JR, Kaufman MD, Lu WP, Smith BD, Vogeti S, Rutkoski TJ, Wise S, Chun L, Zhang Y et al.. (2015) Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. Cancer Cell, 28 (3): 384-98. [PMID:26343583]
4. Tang Z, Yuan X, Du R, Cheung SH, Zhang G, Wei J, Zhao Y, Feng Y, Peng H, Zhang Y et al.. (2015) BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther, 14 (10): 2187-97. [PMID:26208524]
RAF family: A-Raf proto-oncogene, serine/threonine kinase. Last modified on 17/01/2024. Accessed on 08/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1933.