TAO kinase 1

Target id: 2233

Nomenclature: TAO kinase 1

Abbreviated Name: TAO1

Family: TAO subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for TAO kinase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1001 17q11.2 TAOK1 TAO kinase 1
Mouse - 1001 11 B5 Taok1 TAO kinase 1
Rat - 1001 10 q26 Taok1 TAO kinase 1
Previous and Unofficial Names
MAP3K16 | MARKK | PSK2 | thousand and one amino acid protein 1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 Affinity Units Reference
compound 18 [PMID: 20873740] Hs Inhibition 6.4 pIC50 4
pIC50 6.4 (IC50 4.2x10-7 M) [4]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: TAOK1
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd
AST-487 Hs Inhibitor Inhibition 7.5 pKd
lestaurtinib Hs Inhibitor Inhibition 7.2 pKd
AT-7519 Hs Inhibitor Inhibition 6.9 pKd
PP-242 Hs Inhibitor Inhibition 6.9 pKd
alvocidib Hs Inhibitor Inhibition 6.8 pKd
pazopanib Hs Inhibitor Inhibition 6.6 pKd
tozasertib Hs Inhibitor Inhibition 6.5 pKd
linifanib Hs Inhibitor Inhibition 6.5 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.

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: TAO1/TAOK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.9 0.0 0.5
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 11.3 0.0 1.0
aurora kinase/Cdk inhibitor Hs Inhibitor Inhibition 18.8 15.0 4.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 22.6 8.0 2.0
K-252a Hs Inhibitor Inhibition 26.0 5.0 3.0
pazopanib Hs Inhibitor Inhibition 28.9
PKR inhibitor Hs Inhibitor Inhibition 37.5 11.0 0.0
SU11274 Hs Inhibitor Inhibition 41.9 34.0 8.0
Gö 6976 Hs Inhibitor Inhibition 43.9 7.0 10.0
tozasertib Hs Inhibitor Inhibition 44.6
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Menichincheri M, Albanese C, Alli C, Ballinari D, Bargiotti A, Caldarelli M, Ciavolella A, Cirla A, Colombo M, Colotta F et al.. (2010) Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. J. Med. Chem.53 (20): 7296-315. [PMID:20873740]

5. 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

TAO subfamily: TAO kinase 1. Last modified on 19/02/2015. Accessed on 13/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2233.