casein kinase 1 epsilon | Casein kinase 1 (CK1) family | IUPHAR/BPS Guide to PHARMACOLOGY

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casein kinase 1 epsilon

Target not currently curated in GtoImmuPdb

Target id: 1998

Nomenclature: casein kinase 1 epsilon

Abbreviated Name: CK1-E

Family: Casein kinase 1 (CK1) 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 - 416 22q13.1 CSNK1E casein kinase 1 epsilon
Mouse - 416 15 E1 Csnk1e casein kinase 1
Rat - 416 7 q34 Csnk1e casein kinase 1
Previous and Unofficial Names
CKI epsilon | CKIE | casein kinase 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of apo CK1ε.
PDB Id:  4HOK
Resolution:  2.77Å
Species:  Human
References:  5
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of CK1ε in complex with PF-4800567.
PDB Id:  4HNI
Ligand:  PF-4800567
Resolution:  2.74Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.7.11.1

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
umbralisib Hs Inhibition 5.2 pEC50 4
pEC50 5.2 (EC50 6x10-6 M) [4]
PF-670462 Hs Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 7.7x10-9 M) [2]
Description: In a biochemical kinase assay.
PF-4800567 Hs Inhibition 7.5 pIC50 7
pIC50 7.5 (IC50 3.2x10-8 M) [7]
IC261 Hs Inhibition 6.0 pIC50 6
pIC50 6.0 (IC50 1x10-6 M) [6]
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: 3,8

Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1E
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 7.9 pKd
PP-242 Hs Inhibitor Inhibition 7.5 pKd
staurosporine Hs Inhibitor Inhibition 7.1 pKd
SB203580 Hs Inhibitor Inhibition 7.0 pKd
bosutinib Hs Inhibitor Inhibition 7.0 pKd
A-674563 Hs Inhibitor Inhibition 6.9 pKd
GDC-0879 Hs Inhibitor Inhibition 6.9 pKd
neratinib Hs Inhibitor Inhibition 6.5 pKd
SU-14813 Hs Inhibitor Inhibition 6.5 pKd
BI-2536 Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/CK1epsilon
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PP1 analog II Hs Inhibitor Inhibition 1.5
SB220025 Hs Inhibitor Inhibition 2.4
bosutinib Hs Inhibitor Inhibition 11.4
PD 169316 Hs Inhibitor Inhibition 17.3
isogranulatimide Hs Inhibitor Inhibition 18.9
SKF-86002 Hs Inhibitor Inhibition 20.0
Lck inhibitor Hs Inhibitor Inhibition 22.3
SP600125 Hs Inhibitor Inhibition 25.2
SB203580 Hs Inhibitor Inhibition 31.0
SB202190 Hs Inhibitor Inhibition 32.7
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0006897 endocytosis IBA

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. Badura L, Swanson T, Adamowicz W, Adams J, Cianfrogna J, Fisher K, Holland J, Kleiman R, Nelson F, Reynolds L et al.. (2007) An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions. J. Pharmacol. Exp. Ther., 322 (2): 730-8. [PMID:17502429]

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. Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J, Hao Y, Xu X, Deng SX et al.. (2017) Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood, 129 (1): 88-99. [PMID:27784673]

5. Long AM, Zhao H, Huang X. (2012) Structural basis for the potent and selective inhibition of casein kinase 1 epsilon. J. Med. Chem., 55 (22): 10307-11. [PMID:23106386]

6. Mashhoon N, DeMaggio AJ, Tereshko V, Bergmeier SC, Egli M, Hoekstra MF, Kuret J. (2000) Crystal structure of a conformation-selective casein kinase-1 inhibitor. J. Biol. Chem., 275 (26): 20052-60. [PMID:10749871]

7. Walton KM, Fisher K, Rubitski D, Marconi M, Meng QJ, Sládek M, Adams J, Bass M, Chandrasekaran R, Butler T et al.. (2009) Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J. Pharmacol. Exp. Ther., 330 (2): 430-9. [PMID:19458106]

8. 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

Casein kinase 1 (CK1) family: casein kinase 1 epsilon. Last modified on 29/01/2019. Accessed on 26/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1998.