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

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protein tyrosine kinase 6

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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
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
Resolution:  0.0Å
Species:  Human
References:  4
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

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.
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.

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 »


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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 16/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,