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casein kinase 1 gamma 2

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Target not currently curated in GtoImmuPdb

Target id: 2000

Nomenclature: casein kinase 1 gamma 2

Abbreviated Name: CK1-G2

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 19p13.3 CSNK1G2 casein kinase 1 gamma 2
Mouse - 415 10 C1 Csnk1g2 casein kinase 1, gamma 2
Rat - 415 7q11 Csnk1g2 casein kinase 1, gamma 2
Previous and Unofficial Names Click here for help
CKI-gamma 2 | casein kinase 1
Database Links Click here for help
Alphafold P78368 (Hs), Q8BVP5 (Mm), Q62762 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL2543 (Hs)
Ensembl Gene ENSG00000133275 (Hs), ENSMUSG00000003345 (Mm), ENSRNOG00000018529 (Rn)
Entrez Gene 1455 (Hs), 103236 (Mm), 65278 (Rn)
Human Protein Atlas ENSG00000133275 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:1455 (Hs), mmu:103236 (Mm), rno:65278 (Rn)
OMIM 602214 (Hs)
Pharos P78368 (Hs)
RefSeq Nucleotide NM_001319 (Hs), NM_001159591 (Mm), NM_001033870 (Rn)
RefSeq Protein NP_001310 (Hs), NP_001153063 (Mm), NP_001029042 (Rn)
UniProtKB P78368 (Hs), Q8BVP5 (Mm), Q62762 (Rn)
Wikipedia CSNK1G2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of casein kinase 1 gamma 2
PDB Id:  2C47
Resolution:  2.4Å
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
compound 14 [PMID: 24900428] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 4
⤷ pIC50 8.5 (IC50 3x10-9 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: CSNK1G2
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.1 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
TG-100-115 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 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
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: CK1γ2/CK1g2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 14.8 -6.0 -9.0
compound 52 [PMID: 9677190] Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.6 4.0 -9.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 32.4 22.0 -13.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 35.2 19.0 -12.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 45.2 30.0 0.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.9 26.0 -5.0
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 59.6 42.0 1.0
Cdk2 inhibitor IV Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 59.8 33.0 -6.0
IRAK-1/4 inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 62.7 37.0 11.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 63.4 40.0 8.0
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. 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]

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]

How to cite this page

Casein kinase 1 (CK1) family: casein kinase 1 gamma 2. Last modified on 29/01/2016. Accessed on 03/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2000.