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

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casein kinase 1 alpha 1

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

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 - 365 5q32 CSNK1A1 casein kinase 1 alpha 1
Mouse - 325 18 D3 Csnk1a1 casein kinase 1
Rat - 325 18 q12.1 Csnk1a1 casein kinase 1
Previous and Unofficial Names
CK1 | CK1a | CK1alpha | CKI-alpha | clock regulator kinase | 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
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
D4476 Hs Inhibition 6.5 pIC50 6
pIC50 6.5 (IC50 3x10-7 M) [6]
compound 14 [PMID: 24900428] Hs Inhibition 6.3 pIC50 3
pIC50 6.3 (IC50 4.42x10-7 M) [3]
IC261 Hs Inhibition 4.8 pIC50 4
pIC50 4.8 (IC50 1.6x10-5 M) [4]
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1A1
Ligand Sp. Type Action Value Parameter
SB203580 Hs Inhibitor Inhibition 7.1 pKd
sunitinib Hs Inhibitor Inhibition 7.0 pKd
bosutinib Hs Inhibitor Inhibition 6.6 pKd
PP-242 Hs Inhibitor Inhibition 6.4 pKd
SU-14813 Hs Inhibitor Inhibition 6.4 pKd
TG-100-115 Hs Inhibitor Inhibition 6.1 pKd
staurosporine Hs Inhibitor Inhibition 6.0 pKd
BMS-387032 Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Hs Inhibitor Inhibition 5.9 pKd
ruxolitinib 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
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 Hs Inhibitor Inhibition 2.8
D4476 Hs Inhibitor Inhibition 37.1
PD 169316 Hs Inhibitor Inhibition 44.7
JNK inhibitor, negative control Hs Inhibitor Inhibition 47.8
SP600125 Hs Inhibitor Inhibition 47.9
indirubin-3'-monoxime Hs Inhibitor Inhibition 48.2
bosutinib Hs Inhibitor Inhibition 49.5
isogranulatimide Hs Inhibitor Inhibition 51.6
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 53.0
sunitinib 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 27/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1995.