cyclin dependent kinase like 2 | Cyclin-dependent kinase-like (CDKL) family | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

cyclin dependent kinase like 2

Target not currently curated in GtoImmuPdb

Target id: 1983

Nomenclature: cyclin dependent kinase like 2

Abbreviated Name: CdkL2

Family: Cyclin-dependent kinase-like (CDKL) family

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 - 493 4q21.21 CDKL2 cyclin dependent kinase like 2
Mouse - 568 3 E2 Cdkl2 cyclin-dependent kinase-like 2 (CDC2-related kinase)
Rat - 507 14 p22 Cdkl2 cyclin dependent kinase like 2
Previous and Unofficial Names
KKIAMRE | Kkm | P56 | cyclin-dependent kinase-like 2 (CDC2-related kinase)
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
URMC-099 Hs Inhibition - - 2
[2]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
CDKL2 activity is inhibited by >90% in the presence of 1μM URMC-099 [2].
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: CDKL2
Ligand Sp. Type Action Value Parameter
AST-487 Hs Inhibitor Inhibition 9.3 pKd
BMS-387032 Hs Inhibitor Inhibition 7.4 pKd
lestaurtinib Hs Inhibitor Inhibition 7.4 pKd
tozasertib Hs Inhibitor Inhibition 7.3 pKd
sorafenib Hs Inhibitor Inhibition 6.9 pKd
dovitinib Hs Inhibitor Inhibition 6.7 pKd
foretinib Hs Inhibitor Inhibition 6.6 pKd
staurosporine Hs Inhibitor Inhibition 6.3 pKd
axitinib Hs Inhibitor Inhibition 6.3 pKd
A-674563 Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J. Med. Chem., 56 (20): 8032-48. [PMID:24044867]

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

Cyclin-dependent kinase-like (CDKL) family: cyclin dependent kinase like 2. Last modified on 29/01/2016. Accessed on 26/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1983.