tyrosine kinase non receptor 1 | Ack family | IUPHAR/BPS Guide to PHARMACOLOGY

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tyrosine kinase non receptor 1

Target not currently curated in GtoImmuPdb

Target id: 2245

Nomenclature: tyrosine kinase non receptor 1

Abbreviated Name: Tnk1

Family: Ack 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 - 661 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
Kos1 | Tnk1a | Tnk1b | tyrosine kinase
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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
XMD8-92 Hs Inhibition 6.1 pKd 4
pKd 6.1 (Kd 8.9x10-7 M) [4]
HMPL-309 Hs Inhibition 6.6 pIC50 2
pIC50 6.6 (IC50 2.56x10-7 M) [2]
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: 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 Hs Inhibitor Inhibition 8.7 pKd
staurosporine Hs Inhibitor Inhibition 8.6 pKd
lestaurtinib Hs Inhibitor Inhibition 8.0 pKd
foretinib Hs Inhibitor Inhibition 7.7 pKd
tamatinib Hs Inhibitor Inhibition 7.6 pKd
AST-487 Hs Inhibitor Inhibition 7.2 pKd
tozasertib Hs Inhibitor Inhibition 7.1 pKd
midostaurin Hs Inhibitor Inhibition 7.1 pKd
tofacitinib Hs Inhibitor Inhibition 6.9 pKd
axitinib 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 10/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2245.