doublecortin like kinase 3 | DCAMKL family | IUPHAR/BPS Guide to PHARMACOLOGY

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doublecortin like kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2007

Nomenclature: doublecortin like kinase 3

Abbreviated Name: DCAMKL3

Family: DCAMKL 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 - 648 3p22.3 DCLK3 doublecortin like kinase 3
Mouse - 790 9 F3 Dclk3 doublecortin-like kinase 3
Rat - 807 8 q32 Dclk3 doublecortin-like kinase 3
Previous and Unofficial Names
doublecortin and CaM kinase-like 3
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: 2.7.11.1

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
compound 5n [PMID: 20483621] Hs Inhibition - -

Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
1μM compound 5n [PMID 20483621] almost completely abolishes DCLK3 activity [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: DCAMKL3
Ligand Sp. Type Action Value Parameter
tofacitinib Hs Inhibitor Inhibition 7.9 pKd
fedratinib Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.8 pKd
staurosporine Hs Inhibitor Inhibition 7.8 pKd
KW-2449 Hs Inhibitor Inhibition 7.1 pKd
sunitinib Hs Inhibitor Inhibition 7.0 pKd
GSK690693 Hs Inhibitor Inhibition 7.0 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
ruxolitinib Hs Inhibitor Inhibition 6.6 pKd
tamatinib Hs Inhibitor Inhibition 6.2 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. Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA et al.. (2010) Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg. Med. Chem., 18 (12): 4351-62. [PMID:20483621]

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

DCAMKL family: doublecortin like kinase 3. Last modified on 29/01/2016. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2007.