cyclin-dependent kinase 5

Nomenclature: cyclin-dependent kinase 5

Abbreviated Name: CDK5

Family: CDK5 subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 292 7q36 CDK5 cyclin-dependent kinase 5
Mouse - 292 5 A3-B1 Cdk5 cyclin-dependent kinase 5
Rat - 292 4 q11 Cdk5 cyclin-dependent kinase 5
Previous and Unofficial Names
PSSALRE
TPKII catalytic subunit
cell division protein kinase 5
serine/threonine-protein kinase PSSALRE
tau protein kinase II catalytic subunit
Crk6
CRK6
CR6 protein kinase
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  STRUCTURE AND REGULATION OF THE CDK5-P25(NCK5A) COMPLEX
PDB Id:  1H4L
Resolution:  2.65Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.7.11.22
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
dinaciclib Hs Inhibition 9.0 pIC50 4
pIC50 9.0 (IC50 1x10-9 M) [4]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: CDK5
Ligand Sp. Type Action Affinity Units
R547 Hs Inhibitor Inhibition 8.13 pKd
staurosporine Hs Inhibitor Inhibition 7.08 pKd
alvocidib Hs Inhibitor Inhibition 6.96 pKd
lestaurtinib Hs Inhibitor Inhibition 6.39 pKd
AST-487 Hs Inhibitor Inhibition 6.26 pKd
AT-7519 Hs Inhibitor Inhibition 6.15 pKd
BMS-387032 Hs Inhibitor Inhibition 6.13 pKd
TAE 684 Hs Inhibitor Inhibition 5.8 pKd
doramapimod Hs Inhibitor Inhibition 5.7 pKd
SB203580 Hs Inhibitor Inhibition <5.52 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: CDK5-p25/CDK5-p25
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PKR inhibitor Hs Inhibitor Inhibition 0.1 1.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 0.2 -2.0 -1.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 1.5 1.0 0.0
Cdk/Crk inhibitor Hs Inhibitor Inhibition 2.5 0.0 -1.0
aurora kinase/Cdk inhibitor Hs Inhibitor Inhibition 2.5 0.0 0.0
staurosporine Hs Inhibitor Inhibition 2.8 0.5 1.0
aminopurvalanol A Hs Inhibitor Inhibition 3.3 13.0 1.0
purvalanol A Hs Inhibitor Inhibition 3.9 0.0 0.0
SU9516 Hs Inhibitor Inhibition 4.5 0.0 0.0
Cdk1 inhibitor (CGP74514A) Hs Inhibitor Inhibition 5.2 1.0 0.0
Target used in screen: CDK5-p35/CDK5-p35
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SU9516 Hs Inhibitor Inhibition -0.4 0.0 0.0
aminopurvalanol A Hs Inhibitor Inhibition 0.1 20.0 2.0
aurora kinase/Cdk inhibitor Hs Inhibitor Inhibition 0.2 -1.0 0.0
PKR inhibitor Hs Inhibitor Inhibition 0.9 1.0 -1.0
staurosporine Hs Inhibitor Inhibition 1.9 0.5 -0.5
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 2.6 0.0 0.0
purvalanol A Hs Inhibitor Inhibition 2.6 1.0 0.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 3.2 1.0 0.0
K-252a Hs Inhibitor Inhibition 6.6 3.0 1.0
alsterpaullone Hs Inhibitor Inhibition 8.0 6.0 6.0
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. 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]

4. Martin MP, Olesen SH, Georg GI, Schönbrunn E. (2013) Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chem. Biol.8 (11): 2360-5. [PMID:24007471]

5. Tarricone C, Dhavan R, Peng J, Areces LB, Tsai LH, Musacchio A. (2001) Structure and regulation of the CDK5-p25(nck5a) complex. Mol. Cell8 (3): 657-69. [PMID:11583627]

6. 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

CDK5 subfamily: cyclin-dependent kinase 5. Last modified on 10/04/2014. Accessed on 31/10/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1977.