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casein kinase 1 gamma 1

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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

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 422 15q22.31 CSNK1G1 casein kinase 1 gamma 1
Mouse - 459 9 C Csnk1g1 casein kinase 1, gamma 1
Rat - 390 8q24 Csnk1g1 casein kinase 1, gamma 1
Previous and Unofficial Names Click here for help
CKI-gamma 1 | casein kinase 1
Database Links Click here for help
Alphafold Q9HCP0 (Hs), Q8BTH8 (Mm), Q62761 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2426 (Hs)
Ensembl Gene ENSG00000169118 (Hs), ENSMUSG00000032384 (Mm), ENSRNOG00000016620 (Rn)
Entrez Gene 53944 (Hs), 214897 (Mm), 64086 (Rn)
Human Protein Atlas ENSG00000169118 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:53944 (Hs), mmu:214897 (Mm), rno:64086 (Rn)
OMIM 606274 (Hs)
Pharos Q9HCP0 (Hs)
RefSeq Nucleotide NM_022048 (Hs), NM_173185 (Mm), NM_022288 (Rn)
RefSeq Protein NP_071331 (Hs), NP_775277 (Mm), NP_071624 (Rn)
UniProtKB Q9HCP0 (Hs), Q8BTH8 (Mm), Q62761 (Rn)
Wikipedia CSNK1G1 (Hs)
Selected 3D Structures Click here for help
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 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
voruciclib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 5
⤷ pIC50 7.0 (IC50 1.1x10-7 M) [5]
compound 33 [PMID: 19364658] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 4
⤷ pIC50 6.8 (IC50 1.6x10-7 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: 2,6
Key to terms and symbols Click column headers to sort
Target used in screen: CSNK1G1
Ligand Sp. Type Action Value Parameter
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.9 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product 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 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: 1,3
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] Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.0 8.0 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.7 4.0 1.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 26.4 17.0 1.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 28.0 10.0 1.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 55.9
CGP74514A Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 56.8 30.0 6.0
IRAK-1/4 inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 59.2 58.0 67.0
p38 MAP kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 67.2 62.0 11.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 68.4 58.0 40.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 68.5 42.0 7.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation

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 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1999.