cyclin dependent kinase like 1 | Cyclin-dependent kinase-like (CDKL) family | IUPHAR/BPS Guide to PHARMACOLOGY

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cyclin dependent kinase like 1

Target not currently curated in GtoImmuPdb

Target id: 1982

Nomenclature: cyclin dependent kinase like 1

Abbreviated Name: CdkL1

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 - 358 14q21.3 CDKL1 cyclin dependent kinase like 1
Mouse - 352 12 C2 Cdkl1 cyclin-dependent kinase-like 1 (CDC2-related kinase)
Rat - 352 6 q24 Cdkl1 cyclin dependent kinase like 1
Previous and Unofficial Names
KKIALRE | cyclin-dependent kinase-like 1 (CDC2-related kinase)
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the human CDKL1 kinase domain
PDB Id:  4AGU
Resolution:  2.4Å
Species:  Human
References: 
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
compound 9b [PMID: 18986805] Hs Inhibition 7.2 pIC50 2
pIC50 7.2 (IC50 6x10-8 M) [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: CDKL1
Ligand Sp. Type Action Value Parameter
AST-487 Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 6.5 pKd
lestaurtinib Hs Inhibitor Inhibition 6.3 pKd
tamatinib Hs Inhibitor Inhibition 5.7 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
A-674563 Hs Inhibitor Inhibition <5.5 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. Jones CD, Andrews DM, Barker AJ, Blades K, Byth KF, Finlay MR, Geh C, Green CP, Johannsen M, Walker M et al.. (2008) Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg. Med. Chem. Lett., 18 (24): 6486-9. [PMID:18986805]

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 1. Last modified on 29/01/2016. Accessed on 08/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1982.