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cyclin dependent kinase 18

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Target not currently curated in GtoImmuPdb

Target id: 1971

Nomenclature: cyclin dependent kinase 18

Abbreviated Name: CDK18

Family: TAIRE subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 474 1q32.1 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 Click here for help
cell division protein kinase 18 | PCTAIRE protein kinase 3 | PCTAIRE3
Database Links Click here for help
Alphafold Q07002 (Hs), Q04899 (Mm), O35832 (Rn)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL5316 (Hs)
Ensembl Gene ENSG00000117266 (Hs), ENSMUSG00000026437 (Mm), ENSRNOG00000008137 (Rn)
Entrez Gene 5129 (Hs), 18557 (Mm), 289019 (Rn)
Human Protein Atlas ENSG00000117266 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:5129 (Hs), mmu:18557 (Mm), rno:289019 (Rn)
OMIM 169190 (Hs)
Pharos Q07002 (Hs)
RefSeq Nucleotide NM_002596 (Hs), NM_008795 (Mm), NM_001100506 (Rn)
RefSeq Protein NP_002587 (Hs), NP_032821 (Mm), NP_001093976 (Rn)
UniProtKB Q07002 (Hs), Q04899 (Mm), O35832 (Rn)
Wikipedia CDK18 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.22

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 77 [PMID: 24793884] Small molecule or natural product Click here for species-specific activity table 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 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: PCTK3
Ligand Sp. Type Action Value Parameter
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1971.