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

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casein kinase 1 delta

Target not currently curated in GtoImmuPdb

Target id: 1997

Nomenclature: casein kinase 1 delta

Abbreviated Name: CK1-D

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 - 415 17q25 CSNK1D casein kinase 1 delta
Mouse - 409 11 E2 Csnk1d casein kinase 1, delta
Rat - 415 10 q32.3 Csnk1d casein kinase 1
Previous and Unofficial Names
CKID | casein kinase 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of apo human CK1δ.
PDB Id:  3UYS
Resolution:  2.3Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of CK1δ with compound 13.
PDB Id:  4HGT
Resolution:  1.8Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of CK1delta with PF670462 from P1 crystal form
PDB Id:  3UYT
Ligand:  PF-670462
Resolution:  2.0Å
Species:  Human
References:  8
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
PF-670462 Hs Inhibition 7.8 pIC50 2
pIC50 7.8 (IC50 1.4x10-8 M) [2]
Description: In a biochemical kinase assay.
CDK inhibitor 4.35 Hs Inhibition 7.3 pIC50 7
pIC50 7.3 (IC50 4.5x10-8 M) [7]
compound 14 [PMID: 24900428] Hs Inhibition 7.2 pIC50 6
pIC50 7.2 (IC50 5.9x10-8 M) [6]
D4476 Hs Inhibition 6.5 pIC50 3
pIC50 6.5 (IC50 3x10-7 M) [3]
PF-4800567 Hs Inhibition 6.2 pIC50 10
pIC50 6.2 (IC50 7.11x10-7 M) [10]
IC261 Hs Inhibition 6.0 pIC50 9
pIC50 6.0 (IC50 1x10-6 M) [9]
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: 4,11

Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1D
Ligand Sp. Type Action Value Parameter
sunitinib Hs Inhibitor Inhibition 7.8 pKd
SB203580 Hs Inhibitor Inhibition 7.4 pKd
A-674563 Hs Inhibitor Inhibition 6.7 pKd
bosutinib Hs Inhibitor Inhibition 6.6 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
PP-242 Hs Inhibitor Inhibition 6.5 pKd
pictilisib Hs Inhibitor Inhibition 5.9 pKd
TG-100-115 Hs Inhibitor Inhibition 5.9 pKd
GDC-0879 Hs Inhibitor Inhibition 5.8 pKd
BI-2536 Hs Inhibitor Inhibition 5.8 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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: CK1δ/CK1d
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SB220025 Hs Inhibitor Inhibition 1.2 -2.0 1.0
SKF-86002 Hs Inhibitor Inhibition 7.0 3.0 1.0
PD 169316 Hs Inhibitor Inhibition 7.4 1.0 4.0
bosutinib Hs Inhibitor Inhibition 10.9
SP600125 Hs Inhibitor Inhibition 13.1 5.0 1.0
SB203580 Hs Inhibitor Inhibition 13.9 11.0 5.0
SB202190 Hs Inhibitor Inhibition 16.8 7.0 -1.0
isogranulatimide Hs Inhibitor Inhibition 17.2 15.0 9.0
JNK inhibitor, negative control Hs Inhibitor Inhibition 20.8 15.0 1.0
dorsomorphin Hs Inhibitor Inhibition 22.6 21.0 3.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Advanced sleep-phase syndrome, familial, 2; FASPS2
Synonyms: Advanced sleep phase syndrome [Disease Ontology: DOID:0050628]
Familial advanced sleep-phase syndrome [Orphanet: ORPHA164736]
Disease Ontology: DOID:0050628
OMIM: 615224
Orphanet: ORPHA164736

References

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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. Bain J, Plater L, Elliott M, Shpiro N, Hastie CJ, McLauchlan H, Klevernic I, Arthur JS, Alessi DR, Cohen P. (2007) The selectivity of protein kinase inhibitors: a further update. Biochem. J., 408 (3): 297-315. [PMID:17850214]

4. 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]

5. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

6. Huang H, Acquaviva L, Berry V, Bregman H, Chakka N, O'Connor A, DiMauro EF, Dovey J, Epstein O, Grubinska B et al.. (2012) Structure-Based Design of Potent and Selective CK1γ Inhibitors. ACS Med Chem Lett, 3 (12): 1059-64. [PMID:24900428]

7. Jorda R, Havlicek L, Sturc A, Tuskova D, Daumova L, Alam M, Skerlova J, Nekardova M, Perina M, Pospíšil T et al.. (2019) 3,5,7-Substituted pyrazolo[4,3-d]pyrimidine inhibitors of cyclindependent kinases and their evaluation in lymphoma models. Journal of Medicinal Chemistry, Just Accepted Manuscript. DOI: 10.1021/acs.jmedchem.9b00189

8. Long A, Zhao H, Huang X. (2012) Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor. J. Med. Chem., 55 (2): 956-60. [PMID:22168824]

9. 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]

10. 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]

11. 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 delta. Last modified on 05/04/2019. Accessed on 19/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1997.