TRAF2 and NCK interacting kinase | MSN subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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TRAF2 and NCK interacting kinase

Target not currently curated in GtoImmuPdb

Target id: 2244

Nomenclature: TRAF2 and NCK interacting kinase

Abbreviated Name: TNIK

Family: MSN subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1352 3q26.31 TNIK TRAF2 and NCK interacting kinase
Mouse - 1352 3 A3 Tnik TRAF2 and NCK interacting kinase
Rat - 1354 2 q24 Tnik TRAF2 and NCK interacting kinase
Database Links
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ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
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KEGG Gene
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RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the kinase domain of human Traf2- and Nck-Interacting kinase with Wee1Chk1 Inhibitor.
PDB Id:  2X7F
Resolution:  2.8Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.1

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
staurosporine Hs Inhibition 8.9 pIC50 2
pIC50 8.9 (IC50 1.4x10-9 M) [2]
compound 5 [PMID: 23232060] Hs Inhibition 8.5 pIC50 2
pIC50 8.5 (IC50 3x10-9 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: TNIK
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.3 pKd
lestaurtinib Hs Inhibitor Inhibition 8.3 pKd
dovitinib Hs Inhibitor Inhibition 7.6 pKd
sunitinib Hs Inhibitor Inhibition 7.6 pKd
KW-2449 Hs Inhibitor Inhibition 7.6 pKd
bosutinib Hs Inhibitor Inhibition 7.5 pKd
AST-487 Hs Inhibitor Inhibition 7.2 pKd
SU-14813 Hs Inhibitor Inhibition 7.1 pKd
doramapimod Hs Inhibitor Inhibition 6.8 pKd
neratinib 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. Ho KK, Parnell KM, Yuan Y, Xu Y, Kultgen SG, Hamblin S, Hendrickson TF, Luo B, Foulks JM, McCullar MV et al.. (2013) Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors. Bioorg. Med. Chem. Lett., 23 (2): 569-73. [PMID:23232060]

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]

How to cite this page

MSN subfamily: TRAF2 and NCK interacting kinase. Last modified on 20/02/2015. Accessed on 25/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2244.