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cyclin dependent kinase like 1

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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

Contents:

Gene and Protein Information Click here for help
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
Rat - 352 6q24 Cdkl1 cyclin dependent kinase like 1
Previous and Unofficial Names Click here for help
KKIALRE | cyclin-dependent kinase-like 1 (CDC2-related kinase)
Database Links Click here for help
Alphafold Q00532 (Hs), Q8CEQ0 (Mm), Q66HE7 (Rn)
BRENDA 2.7.11.22
ChEMBL Target CHEMBL5789 (Hs)
Ensembl Gene ENSG00000100490 (Hs), ENSMUSG00000020990 (Mm), ENSRNOG00000038720 (Rn)
Entrez Gene 8814 (Hs), 71091 (Mm), 314198 (Rn)
Human Protein Atlas ENSG00000100490 (Hs)
KEGG Enzyme 2.7.11.22
KEGG Gene hsa:8814 (Hs), mmu:71091 (Mm), rno:314198 (Rn)
OMIM 603441 (Hs)
Pharos Q00532 (Hs)
RefSeq Nucleotide NM_004196 (Hs), NM_183294 (Mm), NM_001025121 (Rn)
RefSeq Protein NP_004187 (Hs), NP_899117 (Mm), NP_001020292 (Rn)
UniProtKB Q00532 (Hs), Q8CEQ0 (Mm), Q66HE7 (Rn)
Wikipedia CDKL1 (Hs)
Selected 3D Structures Click here for help
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 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
compound 9b [PMID: 18986805] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 2
⤷ pIC50 7.2 (IC50 6x10-8 M) [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: CDKL1
Ligand Sp. Type Action Value Parameter
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.7 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand 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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1982.