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protein tyrosine kinase 6

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Target not currently curated in GtoImmuPdb

Target id: 2182

Nomenclature: protein tyrosine kinase 6

Abbreviated Name: Brk

Family: Src family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 451 20q13.33 PTK6 protein tyrosine kinase 6
Mouse - 451 2 103.62 cM Ptk6 PTK6 protein tyrosine kinase 6
Rat - 451 3 q43 Ptk6 protein tyrosine kinase 6
Previous and Unofficial Names Click here for help
Sik | Tksk
Database Links Click here for help
Alphafold Q13882 (Hs), Q64434 (Mm)
BRENDA 2.7.10.2
CATH/Gene3D 3.30.505.10
ChEMBL Target CHEMBL4601 (Hs)
Ensembl Gene ENSG00000101213 (Hs), ENSMUSG00000038751 (Mm), ENSRNOG00000012987 (Rn)
Entrez Gene 5753 (Hs), 20459 (Mm), 366275 (Rn)
Human Protein Atlas ENSG00000101213 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:5753 (Hs), mmu:20459 (Mm), rno:366275 (Rn)
OMIM 602004 (Hs)
Pharos Q13882 (Hs)
RefSeq Nucleotide NM_001256358 (Hs), NM_009184 (Mm), NM_001108968 (Rn)
RefSeq Protein NP_005966 (Hs), NP_033210 (Mm), NP_001102438 (Rn)
UniProtKB Q13882 (Hs), Q64434 (Mm)
Wikipedia PTK6 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.10.2

Download all structure-activity data for this target as a CSV file go icon to follow link

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] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 7
⤷ pIC50 8.7 (IC50 2x10-9 M) [7]
tilfrinib Small molecule or natural product Primary target of this compound Hs Inhibition 8.5 pIC50 5
⤷ pIC50 8.5 (IC50 3.15x10-9 M) [5]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
PLX-4720 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.0 7.0 4.0
Lck inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.8 0.0 -1.0
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 4.6
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 11.1 0.0 0.0
PP1 analog II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 19.2 5.0 -1.0
JAK3 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 20.1 18.0 1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 23.2 19.0 1.0
compound 56 [PMID: 8568816] Small molecule or natural product Hs Inhibitor Inhibition 27.7 18.0 2.0
aloisine A Small molecule or natural product 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 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2182.