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TAO kinase 3

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Target not currently curated in GtoImmuPdb

Target id: 2235

Nomenclature: TAO kinase 3

Abbreviated Name: TAO3

Family: TAO subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 898 12q24.23 TAOK3 TAO kinase 3
Mouse - 898 5 F Taok3 TAO kinase 3
Rat - 898 12q16 Taok3 TAO kinase 3
Previous and Unofficial Names Click here for help
axotomy-related gene 357 protein | DPK | JIK | JNK/SAPK-inhibitory kinase | MAP3K18 | thousand and one amino acid protein 3
Database Links Click here for help
Alphafold Q9H2K8 (Hs), Q8BYC6 (Mm), Q53UA7 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5701 (Hs)
Ensembl Gene ENSG00000135090 (Hs), ENSMUSG00000061288 (Mm), ENSRNOG00000001138 (Rn)
Entrez Gene 51347 (Hs), 330177 (Mm), 304530 (Rn)
Human Protein Atlas ENSG00000135090 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:51347 (Hs), mmu:330177 (Mm), rno:304530 (Rn)
Pharos Q9H2K8 (Hs)
RefSeq Nucleotide NM_016281 (Hs), NM_001081308 (Mm), NM_001024254 (Rn)
RefSeq Protein NP_057365 (Hs), NP_001074777 (Mm), NP_001019425 (Rn)
UniProtKB Q9H2K8 (Hs), Q8BYC6 (Mm), Q53UA7 (Rn)
Wikipedia TAOK3 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
AMG28 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 3
⤷ pIC50 7.3 (IC50 4.5x10-8 M) [3]
compound 89S [PMID: 19115845] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 5
⤷ pIC50 6.9 (IC50 1.26x10-7 M) [5]
compound 1 [PMID: 24793884] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 6
⤷ [6]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
TAOK2 activity is completely abolished in the presence of 1μM compound 1 [PMID 24793884] [6].
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: 2,7
Key to terms and symbols Click column headers to sort
Target used in screen: TAOK3
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.7 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.2 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 7.3 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 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: 1,4
Key to terms and symbols Click column headers to sort
Target used in screen: TAO3/TAOK3(JIK)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.1 -0.5 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 10.0 0.0 2.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 16.0 10.0 3.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 18.6 17.0 6.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 21.1 13.0 3.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 24.5 96.0 94.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 38.1 42.0 29.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 39.9 18.0 4.0
SU9516 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 44.0 59.0 12.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 45.5 79.0 24.0
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. Drewry DH, Potjewyd FM, Bayati A, Smith JL, Dickmander RJ, Howell S, Taft-Benz S, Min SM, Hossain MA, Heise M et al.. (2022) Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses. J Med Chem, 65 (19): 12860-12882. [PMID:36111834]

4. 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]

5. Menichincheri M, Bargiotti A, Berthelsen J, Bertrand JA, Bossi R, Ciavolella A, Cirla A, Cristiani C, Croci V, D'Alessio R et al.. (2009) First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem, 52 (2): 293-307. [PMID:19115845]

6. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH. (2014) Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem, 80: 364-82. [PMID:24793884]

7. 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 3. Last modified on 20/09/2022. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2235.