fyn related Src family tyrosine kinase | Src family | IUPHAR/BPS Guide to PHARMACOLOGY

fyn related Src family tyrosine kinase

Target id: 2025

Nomenclature: fyn related Src family tyrosine kinase

Abbreviated Name: FRK

Family: Src family

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

   GtoImmuPdb view: OFF :     Currently no data for fyn related Src family tyrosine kinase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 505 6q21-q22.3 FRK fyn related Src family tyrosine kinase
Mouse - 512 10 B1 Frk fyn-related kinase
Rat - 506 20 q12 Frk fyn-related Src family tyrosine kinase
Previous and Unofficial Names
BSK/IYK | FYN-related kinase | GASK | gastrointestinal-associated kinase | PTK5 | RAK | fyn-related Src family tyrosine kinase
Database Links
BRENDA
CATH/Gene3D
DrugBank 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:  Solution structure of the SH2 domain of murine Fyn-related kinase
PDB Id:  2DLY
Resolution:  0.0Å
Species:  Mouse
References: 
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 Affinity Units Reference
bosutinib Hs Inhibition 8.7 pIC50 5
pIC50 8.7 (IC50 2.2x10-9 M) [5]
eCF506 Hs Inhibition 8.6 pIC50 3
pIC50 8.6 (IC50 2.8x10-9 M) [3]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: FRK
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 9.5 pKd
bosutinib Hs Inhibitor Inhibition 8.9 pKd
foretinib Hs Inhibitor Inhibition 8.4 pKd
PD-173955 Hs Inhibitor Inhibition 8.4 pKd
AST-487 Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd
staurosporine Hs Inhibitor Inhibition 7.3 pKd
tamatinib Hs Inhibitor Inhibition 7.2 pKd
nilotinib Hs Inhibitor Inhibition 7.1 pKd
masitinib Hs Inhibitor Inhibition 7.1 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: PTK5/FRK(PTK5)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition -0.9
staurosporine Hs Inhibitor Inhibition 5.5 1.5 0.0
Lck inhibitor Hs Inhibitor Inhibition 6.3 2.0 2.0
TWS119 Hs Inhibitor Inhibition 7.0 1.0 0.0
nilotinib Hs Inhibitor Inhibition 16.2
GSK-3 inhibitor IX Hs Inhibitor Inhibition 23.2 2.0 0.0
masitinib Hs Inhibitor Inhibition 25.8
PDGF RTK inhibitor Hs Inhibitor Inhibition 27.5 6.0 1.0
bosutinib Hs Inhibitor Inhibition 29.2
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 33.9 95.0 84.0
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. Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC et al.. (2016) Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J. Med. Chem., 59 (10): 4697-710. [PMID:27115835]

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. Remsing Rix LL, Rix U, Colinge J, Hantschel O, Bennett KL, Stranzl T, Müller A, Baumgartner C, Valent P, Augustin M et al.. (2009) Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia, 23 (3): 477-85. [PMID:19039322]

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]

How to cite this page

Src family: fyn related Src family tyrosine kinase. Last modified on 24/05/2016. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2025.