FES proto-oncogene, tyrosine kinase | Fer family | IUPHAR/BPS Guide to PHARMACOLOGY

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FES proto-oncogene, tyrosine kinase

Target not currently curated in GtoImmuPdb

Target id: 2023

Nomenclature: FES proto-oncogene, tyrosine kinase

Abbreviated Name: Fes

Family: Fer family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 822 15q25-qter FES FES proto-oncogene, tyrosine kinase
Mouse - 822 7 D3 Fes feline sarcoma oncogene
Rat - 822 1 q31 Fes FES proto-oncogene
Previous and Unofficial Names
FPS | FES proto-oncogene
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human Feline Sarcoma Viral Oncogene Homologue (v-FES)
PDB Id:  3BKB
Ligand:  staurosporine
Resolution:  1.78Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.10.2

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
Ligand Sp. Action Value Parameter Reference
compound 8e [PMID: 24432909] Hs Inhibition 8.3 pIC50 6
pIC50 8.3 (IC50 5x10-9 M) [6]
lorlatinib Hs Inhibition 8.2 pIC50 7
pIC50 8.2 (IC50 6x10-9 M) [7]
compound 25b [PMID: 22564207] Hs Inhibition 7.0 pIC50 5
pIC50 7.0 (IC50 9.9x10-8 M) [5]
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: 2,8

Key to terms and symbols Click column headers to sort
Target used in screen: FES
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Hs Inhibitor Inhibition 8.3 pKd
staurosporine Hs Inhibitor Inhibition 7.6 pKd
GSK-1838705A Hs Inhibitor Inhibition 7.3 pKd
foretinib Hs Inhibitor Inhibition 7.0 pKd
tamatinib Hs Inhibitor Inhibition 6.7 pKd
bosutinib Hs Inhibitor Inhibition 6.5 pKd
AST-487 Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Hs Inhibitor Inhibition 6.4 pKd
crizotinib Hs Inhibitor Inhibition 6.3 pKd
fedratinib Hs Inhibitor Inhibition 6.3 pKd
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

Key to terms and symbols Click column headers to sort
Target used in screen: Fes/FES
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 4.1 0.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 10.2 2.0 1.0
SU11652 Hs Inhibitor Inhibition 22.1 14.0 2.0
sunitinib Hs Inhibitor Inhibition 33.7
bosutinib Hs Inhibitor Inhibition 35.7
K-252a Hs Inhibitor Inhibition 36.4 7.0 1.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 37.9 16.0 5.0
SB 218078 Hs Inhibitor Inhibition 42.1 90.0 99.0
alsterpaullone Hs Inhibitor Inhibition 46.3 35.0 43.0
midostaurin Hs Inhibitor Inhibition 48.3 15.0 9.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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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. 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. Filippakopoulos P, Kofler M, Hantschel O, Gish GD, Grebien F, Salah E, Neudecker P, Kay LE, Turk BE, Superti-Furga G et al.. (2008) Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation. Cell, 134 (5): 793-803. [PMID:18775312]

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. Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D et al.. (2014) Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J. Med. Chem., 57 (11): 4720-44. [PMID:24819116]

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]

How to cite this page

Fer family: FES proto-oncogene, tyrosine kinase. Last modified on 11/02/2015. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2023.