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doublecortin like kinase 2

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Target not currently curated in GtoImmuPdb

Target id: 2006

Nomenclature: doublecortin like kinase 2

Abbreviated Name: DCAMKL2

Family: DCAMKL family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 766 4q31.23-q31.3 DCLK2 doublecortin like kinase 2
Mouse - 756 3 F1 Dclk2 doublecortin-like kinase 2
Rat - 767 2q34 Dclk2 doublecortin-like kinase 2
Previous and Unofficial Names Click here for help
CaMK-like CREB regulatory kinase 2 | CLICK2 | CLICK-II | DCK2 | doublecortin and CaM kinase-like 2
Database Links Click here for help
Alphafold Q8N568 (Hs), Q6PGN3 (Mm), Q5MPA9 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 3.10.20.230
ChEMBL Target CHEMBL5519 (Hs)
Ensembl Gene ENSG00000170390 (Hs), ENSMUSG00000028078 (Mm), ENSRNOG00000016550 (Rn)
Entrez Gene 166614 (Hs), 70762 (Mm), 310698 (Rn)
Human Protein Atlas ENSG00000170390 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:166614 (Hs), mmu:70762 (Mm), rno:310698 (Rn)
OMIM 613166 (Hs)
Pharos Q8N568 (Hs)
RefSeq Nucleotide NM_001040260 (Hs), NM_001195496 (Mm), NM_001009691 (Rn)
RefSeq Protein NP_001035350 (Hs), NP_001182425 (Mm), NP_001009691 (Rn)
UniProtKB Q8N568 (Hs), Q6PGN3 (Mm), Q5MPA9 (Rn)
Wikipedia DCLK2 (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
XMD8-92 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pKd 6
⤷ pKd 6.7 (Kd 1.9x10-7 M) [6]
DCLK1-IN-1 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 3
⤷ pIC50 7.5 (IC50 3.1x10-8 M) [3]
Description: Determined in a KinomeScan binding assay.
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: DCAMKL2
Ligand Sp. Type Action Value Parameter
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 7.1 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 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: DCAMKL2/DCAMKL2
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 11.0 5.5 2.5
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.4 13.0 2.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 65.8 38.0 27.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 69.8 55.0 17.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 72.0 55.0 55.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 74.4 75.0 41.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 82.3 96.0 85.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.8 68.0 24.0
fasudil Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 83.9 120.0 105.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 84.7 56.0 60.0
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. Ferguson FM, Nabet B, Raghavan S, Liu Y, Leggett AL, Kuljanin M, Kalekar RL, Yang A, He S, Wang J et al.. (2020) Discovery of a selective inhibitor of doublecortin like kinase 1. Nat Chem Biol, 16 (6): 635-643. [PMID:32251410]

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. 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]

6. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell, 18 (3): 258-67. [PMID:20832753]

How to cite this page

DCAMKL family: doublecortin like kinase 2. Last modified on 14/07/2020. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2006.