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doublecortin like kinase 3

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Target not currently curated in GtoImmuPdb

Target id: 2007

Nomenclature: doublecortin like kinase 3

Abbreviated Name: DCAMKL3

Family: DCAMKL family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 648 3p22.2 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 Click here for help
doublecortin and CaM kinase-like 3
Database Links Click here for help
Alphafold Q9C098 (Hs), Q8BWQ5 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL6123 (Hs)
Ensembl Gene ENSG00000163673 (Hs), ENSMUSG00000032500 (Mm), ENSRNOG00000033026 (Rn)
Entrez Gene 85443 (Hs), 245038 (Mm), 316023 (Rn)
Human Protein Atlas ENSG00000163673 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:85443 (Hs), mmu:245038 (Mm), rno:316023 (Rn)
OMIM 613167 (Hs)
Pharos Q9C098 (Hs)
RefSeq Nucleotide NM_033403 (Hs), NM_172928 (Mm), NM_001191800 (Rn)
RefSeq Protein NP_208382 (Hs), NP_766516 (Mm), NP_001178729 (Rn)
UniProtKB Q9C098 (Hs), Q8BWQ5 (Mm)
Wikipedia DCLK3 (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
compound 5n [PMID: 20483621] Small molecule or natural product Click here for species-specific activity table 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 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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: DCAMKL3
Ligand Sp. Type Action Value Parameter
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand 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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2007.