cyclin dependent kinase 18 | TAIRE subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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cyclin dependent kinase 18

Target not currently curated in GtoImmuPdb

Target id: 1971

Nomenclature: cyclin dependent kinase 18

Abbreviated Name: CDK18

Family: TAIRE subfamily

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 474 1q31-q32 CDK18 cyclin dependent kinase 18
Mouse - 451 1 E4 Cdk18 cyclin-dependent kinase 18
Rat - 451 13q13 Cdk18 cyclin-dependent kinase 18
Previous and Unofficial Names
cell division protein kinase 18 | PCTAIRE protein kinase 3 | PCTAIRE3
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.22

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 77 [PMID: 24793884] Hs Inhibition - - 2
[2]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
CDK18 activity is completely inhibited in the presence of 1μM compound 77 [PMID 24793884] [2] (note that CDK18 is referred to by its synonym PCTK3 in the article's Supplementary data table).
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: PCTK3
Ligand Sp. Type Action Value Parameter
AT-7519 Hs Inhibitor Inhibition 7.8 pKd
R547 Hs Inhibitor Inhibition 7.7 pKd
BMS-387032 Hs Inhibitor Inhibition 7.4 pKd
AST-487 Hs Inhibitor Inhibition 7.3 pKd
foretinib Hs Inhibitor Inhibition 6.6 pKd
staurosporine Hs Inhibitor Inhibition 6.6 pKd
alvocidib Hs Inhibitor Inhibition 6.0 pKd
PHA-665752 Hs Inhibitor Inhibition 5.8 pKd
sunitinib Hs Inhibitor Inhibition 5.8 pKd
fedratinib Hs Inhibitor Inhibition 5.6 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. 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]

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

TAIRE subfamily: cyclin dependent kinase 18. Last modified on 25/02/2015. Accessed on 24/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1971.