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cyclin dependent kinase like 2

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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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 493 4q21.1 CDKL2 cyclin dependent kinase like 2
Mouse - 568 5 E2 Cdkl2 cyclin dependent kinase like 2
Rat - 507 14p22 Cdkl2 cyclin dependent kinase like 2
Previous and Unofficial Names Click here for help
KKIAMRE | Kkm | P56 | cyclin-dependent kinase-like 2 (CDC2-related kinase)
Database Links Click here for help
Alphafold Q92772 (Hs), Q9QUK0 (Mm), Q5XIT0 (Rn)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL5728 (Hs)
Ensembl Gene ENSG00000138769 (Hs), ENSMUSG00000029403 (Mm), ENSRNOG00000002506 (Rn)
Entrez Gene 8999 (Hs), 53886 (Mm), 305242 (Rn)
Human Protein Atlas ENSG00000138769 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:8999 (Hs), mmu:53886 (Mm), rno:305242 (Rn)
OMIM 603442 (Hs)
Pharos Q92772 (Hs)
RefSeq Nucleotide NM_003948 (Hs), NM_016912 (Mm), NM_001012035 (Rn)
RefSeq Protein NP_003939 (Hs), NP_058608 (Mm), NP_001012035 (Rn)
UniProtKB Q92772 (Hs), Q9QUK0 (Mm), Q5XIT0 (Rn)
Wikipedia CDKL2 (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
URMC-099 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
CDKL2 activity is inhibited by >90% in the presence of 1μM URMC-099 [2].
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: CDKL2
Ligand Sp. Type Action Value Parameter
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 9.3 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.7 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 6.3 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 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. 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 09/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1983.