protein tyrosine kinase 6 | Src family | IUPHAR/BPS Guide to PHARMACOLOGY

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protein tyrosine kinase 6

Target not currently curated in GtoImmuPdb

Target id: 2182

Nomenclature: protein tyrosine kinase 6

Abbreviated Name: Brk

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 451 20q13.3 PTK6 protein tyrosine kinase 6
Mouse - 451 2 H4 Ptk6 PTK6 protein tyrosine kinase 6
Rat - 451 3 q43 Ptk6 protein tyrosine kinase 6
Previous and Unofficial Names
Sik | Tksk
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:  Solution Structure and Backbone Dynamics of the Nonreceptor Tyrosine Kinase PTK6/Brk SH2 Domain
PDB Id:  1RJA
Resolution:  0.0Å
Species:  Human
References:  4
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 19a [PMID: 21855335] Hs Inhibition 8.7 pIC50 7
pIC50 8.7 (IC50 2x10-9 M) [7]
tilfrinib Hs Inhibition 8.5 pIC50 5
pIC50 8.5 (IC50 3.15x10-9 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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: BRK
Ligand Sp. Type Action Value Parameter
foretinib Hs Inhibitor Inhibition 8.4 pKd
dasatinib Hs Inhibitor Inhibition 8.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.4 pKd
PD-173955 Hs Inhibitor Inhibition 7.3 pKd
PLX-4720 Hs Inhibitor Inhibition 7.3 pKd
Ki-20227 Hs Inhibitor Inhibition 7.2 pKd
vandetanib Hs Inhibitor Inhibition 6.8 pKd
tamatinib Hs Inhibitor Inhibition 6.4 pKd
cediranib Hs Inhibitor Inhibition 6.3 pKd
PP-242 Hs Inhibitor Inhibition 6.0 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: BRK/BRK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Src kinase inhibitor I Hs Inhibitor Inhibition 0.0 7.0 4.0
Lck inhibitor Hs Inhibitor Inhibition 0.8 0.0 -1.0
dasatinib Hs Inhibitor Inhibition 4.6
vandetanib Hs Inhibitor Inhibition 7.3
TWS119 Hs Inhibitor Inhibition 11.1 0.0 0.0
PP1 analog II Hs Inhibitor Inhibition 19.2 5.0 -1.0
JAK3 inhibitor II Hs Inhibitor Inhibition 20.1 18.0 1.0
K-252a Hs Inhibitor Inhibition 23.2 19.0 1.0
compound 56 [PMID: 8568816] Hs Inhibitor Inhibition 27.7 18.0 2.0
aloisine A Hs Inhibitor Inhibition 29.7 31.0 29.0
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. 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. Hong E, Shin J, Kim HI, Lee ST, Lee W. (2004) Solution structure and backbone dynamics of the non-receptor protein-tyrosine kinase-6 Src homology 2 domain. J. Biol. Chem., 279 (28): 29700-8. [PMID:15056653]

5. Mahmoud KA, Krug M, Wersig T, Slynko I, Schächtele C, Totzke F, Sippl W, Hilgeroth A. (2014) Discovery of 4-anilino α-carbolines as novel Brk inhibitors. Bioorg. Med. Chem. Lett., 24 (8): 1948-51. [PMID:24650640]

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]

7. Zeng H, Belanger DB, Curran PJ, Shipps Jr GW, Miao H, Bracken JB, Arshad Siddiqui M, Malkowski M, Wang Y. (2011) Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors. Bioorg. Med. Chem. Lett., 21 (19): 5870-5. [PMID:21855335]

How to cite this page

Src family: protein tyrosine kinase 6. Last modified on 25/02/2016. Accessed on 12/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2182.