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casein kinase 1 alpha 1

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Target not currently curated in GtoImmuPdb

Target id: 1995

Nomenclature: casein kinase 1 alpha 1

Abbreviated Name: CK1-A

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 - 337 5q32 CSNK1A1 casein kinase 1 alpha 1
Mouse - 337 18 E1 Csnk1a1 casein kinase 1, alpha 1
Rat - 325 18q12.1 Csnk1a1 casein kinase 1, alpha 1
Previous and Unofficial Names Click here for help
CK1 | CK1a | CK1alpha | CKI-alpha | clock regulator kinase | casein kinase 1
Database Links Click here for help
Alphafold P48729 (Hs), Q8BK63 (Mm), P97633 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2793 (Hs), CHEMBL5148 (Mm)
Ensembl Gene ENSG00000113712 (Hs), ENSMUSG00000024576 (Mm), ENSRNOG00000063313 (Rn)
Entrez Gene 1452 (Hs), 93687 (Mm), 113927 (Rn)
Human Protein Atlas ENSG00000113712 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:1452 (Hs), mmu:93687 (Mm), rno:113927 (Rn)
OMIM 600505 (Hs)
Pharos P48729 (Hs)
RefSeq Nucleotide NM_001025105 (Hs), NM_146087 (Mm), NM_053615 (Rn)
RefSeq Protein NP_001020276 (Hs), NP_666199 (Mm), NP_446067 (Rn)
UniProtKB P48729 (Hs), Q8BK63 (Mm), P97633 (Rn)
Wikipedia CSNK1A1 (Hs)
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
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 6
⤷ pIC50 6.5 (IC50 3x10-7 M) [6]
compound 14 [PMID: 24900428] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 3
⤷ pIC50 6.3 (IC50 4.42x10-7 M) [3]
IC261 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.8 pIC50 4
⤷ pIC50 4.8 (IC50 1.6x10-5 M) [4]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1A1
Ligand Sp. Type Action Value Parameter
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
BMS-387032 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.9 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.7 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
Key to terms and symbols Click column headers to sort
Target used in screen: nd/CK1a1
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 2.8
D4476 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 37.1
PD 169316 Small molecule or natural product Hs Inhibitor Inhibition 44.7
JNK inhibitor, negative control Small molecule or natural product Hs Inhibitor Inhibition 47.8
SP600125 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 47.9
indirubin-3'-monoxime Small molecule or natural product Hs Inhibitor Inhibition 48.2
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 49.5
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 51.6
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 53.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 54.0
Displaying the top 10 most potent ligands  View all ligands in screen »

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. 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]

3. 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]

4. 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]

5. 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]

6. Yang LL, Li GB, Yan HX, Sun QZ, Ma S, Ji P, Wang ZR, Feng S, Zou J, Yang SY. (2012) Discovery of N6-phenyl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors using common-feature pharmacophore model based virtual screening and hit-to-lead optimization. Eur J Med Chem, 56: 30-8. [PMID:22944772]

How to cite this page

Casein kinase 1 (CK1) family: casein kinase 1 alpha 1. Last modified on 29/01/2016. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1995.