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casein kinase 1 delta

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Target not currently curated in GtoImmuPdb

Target id: 1997

Nomenclature: casein kinase 1 delta

Abbreviated Name: CK1-D

Family: Casein kinase 1 (CK1) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 415 17q25.3 CSNK1D casein kinase 1 delta
Mouse - 415 11 E2 Csnk1d casein kinase 1, delta
Rat - 415 10q32.3 Csnk1d casein kinase 1, delta
Previous and Unofficial Names Click here for help
CKID | casein kinase 1
Database Links Click here for help
Alphafold P48730 (Hs), Q9DC28 (Mm), Q06486 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2828 (Hs), CHEMBL5175 (Mm), CHEMBL4484 (Rn)
Ensembl Gene ENSG00000141551 (Hs), ENSMUSG00000025162 (Mm), ENSRNOG00000036676 (Rn)
Entrez Gene 1453 (Hs), 104318 (Mm), 64462 (Rn)
Human Protein Atlas ENSG00000141551 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:1453 (Hs), mmu:104318 (Mm), rno:64462 (Rn)
OMIM 600864 (Hs)
Orphanet ORPHA165845 (Hs)
Pharos P48730 (Hs)
RefSeq Nucleotide NM_001893 (Hs), NM_027874 (Mm), NM_139060 (Rn)
RefSeq Protein NP_001884 (Hs), NP_082150 (Mm), NP_620691 (Rn)
SynPHARM 81080 (in complex with PF-4800567)
83964 (in complex with PF-670462)
UniProtKB P48730 (Hs), Q9DC28 (Mm), Q06486 (Rn)
Wikipedia CSNK1D (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.1

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
PF-670462 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 7
⤷ pIC50 7.3 (IC50 4.5x10-8 M) [7]
compound 14 [PMID: 24900428] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 6
⤷ pIC50 7.2 (IC50 5.9x10-8 M) [6]
JNJ-6204 Small molecule or natural product Hs Inhibition 7.2 pIC50 10
⤷ pIC50 7.2 (IC50 6.2x10-8 M) [10]
Description: Potency determined in a nanoBRET cellular competition binding assay- this value is for the non-deuterated analogue (compound 15)
D4476 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.5 pIC50 3
⤷ pIC50 6.5 (IC50 3x10-7 M) [3]
PF-4800567 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 11
⤷ pIC50 6.2 (IC50 7.11x10-7 M) [11]
IC261 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.0 pIC50 9
⤷ pIC50 6.0 (IC50 1x10-6 M) [9]
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: 4,12
Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1D
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
pictilisib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
GDC-0879 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.2 -2.0 1.0
SKF-86002 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 3.0 1.0
PD 169316 Small molecule or natural product Hs Inhibitor Inhibition 7.4 1.0 4.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.9
SP600125 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 13.1 5.0 1.0
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 13.9 11.0 5.0
SB202190 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 16.8 7.0 -1.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 17.2 15.0 9.0
JNK inhibitor, negative control Small molecule or natural product Hs Inhibitor Inhibition 20.8 15.0 1.0
dorsomorphin Small molecule or natural product Ligand has a PDB structure 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 Click here for help
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, Havlíček L, Šturc A, Tušková D, Daumová L, Alam M, Škerlová J, Nekardová M, Peřina M, Pospíšil T et al.. (2019) 3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models. J Med Chem, 62 (9): 4606-4623. DOI: 10.1021/acs.jmedchem.9b00189 [PMID:30943029]

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. McCarver S, Hanna L, Samant A, Thompson AA, Seierstad M, Saha A, Wu D, Lord B, Sutton SW, Shah V et al.. (2024) Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions. ACS Med Chem Lett, 15 (4): 486-492. [PMID:38628796]

11. 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]

12. 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 22/04/2024. Accessed on 02/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1997.