Top ▲

cyclin dependent kinase 3

Click here for help

Target id: 1975

Nomenclature: cyclin dependent kinase 3

Abbreviated Name: CDK3

Family: CDK1 subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 305 17q25.1 CDK3 cyclin dependent kinase 3
Mouse - 303 11 E2 Cdk3 cyclin dependent kinase 3
Previous and Unofficial Names Click here for help
Cdkn3 | Cell division protein kinase 3 | cyclin-dependent kinase 3 | cyclin-dependent kinase 3, pseudogene | Cdk3-ps
Database Links Click here for help
Alphafold Q00526 (Hs), Q80YP0 (Mm)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL4442 (Hs)
Ensembl Gene ENSG00000250506 (Hs), ENSMUSG00000092300 (Mm)
Entrez Gene 1018 (Hs), 69681 (Mm)
Human Protein Atlas ENSG00000250506 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:1018 (Hs), mmu:69681 (Mm)
OMIM 123828 (Hs)
Pharos Q00526 (Hs)
RefSeq Nucleotide NM_001258 (Hs), NR_004853 (Mm)
RefSeq Protein NP_001249 (Hs)
UniProtKB Q00526 (Hs), Q80YP0 (Mm)
Wikipedia CDK3 (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
RGB-286638 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 2
⤷ pIC50 8.3 (IC50 5x10-9 M) [2]
Description: in association with cyclin E
zotiraciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 5
⤷ pIC50 8.1 (IC50 8x10-9 M) [5]
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: 3,6
Key to terms and symbols Click column headers to sort
Target used in screen: CDK3
Ligand Sp. Type Action Value Parameter
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.4 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
A-674563 Small molecule or natural product 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: CDK3-cyclin E/CDK3-cyclin E
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -1.6 1.0 -1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -0.9 -2.0 0.0
Cdk/Crk inhibitor Small molecule or natural product Hs Inhibitor Inhibition 6.1 -1.0 -1.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 1.5 2.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 25.2 0.0 1.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 31.9 45.0 6.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 32.4 3.0 0.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 34.5 14.0 3.0
SU9516 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 35.2 7.0 4.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 36.2 10.0 1.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G et al.. (2013) Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia, 27 (12): 2366-75. [PMID:23807770]

3. 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]

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. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia, 26 (2): 236-43. [PMID:21860433]

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

CDK1 subfamily: cyclin dependent kinase 3. Last modified on 11/04/2016. Accessed on 11/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1975.