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tyrosine kinase non receptor 1

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Target not currently curated in GtoImmuPdb

Target id: 2245

Nomenclature: tyrosine kinase non receptor 1

Abbreviated Name: Tnk1

Family: Ack family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 666 17p13.1 TNK1 tyrosine kinase non receptor 1
Mouse - 666 11 B3 Tnk1 tyrosine kinase, non-receptor, 1
Rat - 667 10 q24 Tnk1 tyrosine kinase, non-receptor, 1
Previous and Unofficial Names Click here for help
Kos1 | Tnk1a | Tnk1b | tyrosine kinase
Database Links Click here for help
Alphafold Q13470 (Hs), Q99ML2 (Mm)
BRENDA 2.7.10.2
ChEMBL Target CHEMBL5334 (Hs)
Ensembl Gene ENSG00000174292 (Hs), ENSMUSG00000001583 (Mm), ENSRNOG00000015578 (Rn)
Entrez Gene 8711 (Hs), 83813 (Mm), 303247 (Rn)
Human Protein Atlas ENSG00000174292 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:8711 (Hs), mmu:83813 (Mm), rno:303247 (Rn)
OMIM 608076 (Hs)
Pharos Q13470 (Hs)
RefSeq Nucleotide NM_003985 (Hs), NM_031880 (Mm), NM_001107012 (Rn)
RefSeq Protein NP_003976 (Hs), NP_114086 (Mm), NP_001100482 (Rn)
UniProtKB Q13470 (Hs), Q99ML2 (Mm)
Wikipedia TNK1 (Hs)
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
XMD8-92 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pKd 4
⤷ pKd 6.1 (Kd 8.9x10-7 M) [4]
xiliertinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 2
⤷ pIC50 6.6 (IC50 2.56x10-7 M) [2]
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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: TNK1
Ligand Sp. Type Action Value Parameter
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.9 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. Ren Y, Zheng J, Fan S, Wang L, Cheng M, Shi D, Zhang W, Tang R, Yu Y, Jiao L et al.. (2017) Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget, 8 (31): 50832-50844. [PMID:28881608]

3. 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]

4. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell, 18 (3): 258-67. [PMID:20832753]

How to cite this page

Ack family: tyrosine kinase non receptor 1. Last modified on 26/04/2018. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2245.