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

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casein kinase 1 gamma 1

Target not currently curated in GtoImmuPdb

Target id: 1999

Nomenclature: casein kinase 1 gamma 1

Abbreviated Name: CK1-G1

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 - 422 15q22.1-q22.31 CSNK1G1 casein kinase 1 gamma 1
Mouse - 459 9 C Csnk1g1 casein kinase 1, gamma 1
Rat - 390 8 q24 Csnk1g1 casein kinase 1
Previous and Unofficial Names
CKI-gamma 1 | casein kinase 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of human casein kinase 1 gamma-1 in complex with 2-(2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine (CASP target)
PDB Id:  2CMW
Resolution:  1.75Å
Species:  Human
References: 
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
voruciclib Hs Inhibition 7.0 pIC50 5
pIC50 7.0 (IC50 1.1x10-7 M) [5]
compound 33 [PMID: 19364658] Hs Inhibition 6.8 pIC50 4
pIC50 6.8 (IC50 1.6x10-7 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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1G1
Ligand Sp. Type Action Value Parameter
A-674563 Hs Inhibitor Inhibition 6.3 pKd
sunitinib Hs Inhibitor Inhibition 6.0 pKd
AST-487 Hs Inhibitor Inhibition 6.0 pKd
SU-14813 Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Hs Inhibitor Inhibition 5.9 pKd
alvocidib Hs Inhibitor Inhibition 5.9 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: CK1γ1/CK1g1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 16.0 8.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 16.7 4.0 1.0
aminopurvalanol A Hs Inhibitor Inhibition 26.4 17.0 1.0
purvalanol A Hs Inhibitor Inhibition 28.0 10.0 1.0
sunitinib Hs Inhibitor Inhibition 55.9
CGP74514A Hs Inhibitor Inhibition 56.8 30.0 6.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 59.2 58.0 67.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 67.2 62.0 11.0
isogranulatimide Hs Inhibitor Inhibition 68.4 58.0 40.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 68.5 42.0 7.0
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. 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]

4. Lovering F, Kirincich S, Wang W, Combs K, Resnick L, Sabalski JE, Butera J, Liu J, Parris K, Telliez JB. (2009) Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg. Med. Chem., 17 (9): 3342-51. [PMID:19364658]

5. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV. (2015) Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. PLoS ONE, 10 (11): e0143685. [PMID:26606677]

6. 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 gamma 1. Last modified on 25/04/2018. Accessed on 17/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1999.