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cyclin dependent kinase 16

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Target id: 1969

Nomenclature: cyclin dependent kinase 16

Abbreviated Name: CDK16

Family: TAIRE subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 496 Xp11.3 CDK16 cyclin dependent kinase 16
Mouse - 496 X 16.18 cM Cdk16 cyclin dependent kinase 16
Rat - 496 Xq11 Cdk16 cyclin-dependent kinase 16
Previous and Unofficial Names Click here for help
cell division protein kinase 16 | CRK5 | PCTAIRE protein kinase 1 | PCTAIRE1
Database Links Click here for help
Alphafold Q00536 (Hs), Q04735 (Mm), Q63686 (Rn)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL4597 (Hs)
Ensembl Gene ENSG00000102225 (Hs), ENSMUSG00000031065 (Mm), ENSRNOG00000008578 (Rn)
Entrez Gene 5127 (Hs), 18555 (Mm), 81741 (Rn)
Human Protein Atlas ENSG00000102225 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:5127 (Hs), mmu:18555 (Mm), rno:81741 (Rn)
OMIM 311550 (Hs)
Pharos Q00536 (Hs)
RefSeq Nucleotide NM_001170460 (Hs), NM_011049 (Mm), NM_001004132 (Rn)
RefSeq Protein NP_006192 (Hs), NP_035179 (Mm), NP_001004132 (Rn)
UniProtKB Q00536 (Hs), Q04735 (Mm), Q63686 (Rn)
Wikipedia CDK16 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the PCTAIRE1 kinase in complex with Indirubin E804
PDB Id:  3MTL
Resolution:  2.4Å
Species:  Human
References: 
Enzyme Reaction Click here for help
EC Number: 2.7.11.22
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: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: PCTK1
Ligand Sp. Type Action Value Parameter
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 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. 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 16. Last modified on 22/03/2013. Accessed on 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1969.