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casein kinase 1 gamma 3

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Target not currently curated in GtoImmuPdb

Target id: 2001

Nomenclature: casein kinase 1 gamma 3

Abbreviated Name: CK1-G3

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 - 447 5q23.2 CSNK1G3 casein kinase 1 gamma 3
Mouse - 424 18 D1 Csnk1g3 casein kinase 1, gamma 3
Rat - 448 18q11 Csnk1g3 casein kinase 1, gamma 3
Previous and Unofficial Names Click here for help
CKI-gamma 3 | casein kinase 1
Database Links Click here for help
Alphafold Q9Y6M4 (Hs), Q8C4X2 (Mm), Q62763 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5084 (Hs)
Ensembl Gene ENSG00000151292 (Hs), ENSMUSG00000073563 (Mm), ENSRNOG00000016677 (Rn)
Entrez Gene 1456 (Hs), 70425 (Mm), 64823 (Rn)
Human Protein Atlas ENSG00000151292 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:1456 (Hs), mmu:70425 (Mm), rno:64823 (Rn)
OMIM 604253 (Hs)
Pharos Q9Y6M4 (Hs)
RefSeq Nucleotide NM_001031812 (Hs), NM_152809 (Mm), NM_022855 (Rn)
RefSeq Protein NP_001026982 (Hs), NP_690022 (Mm), NP_074046 (Rn)
UniProtKB Q9Y6M4 (Hs), Q8C4X2 (Mm), Q62763 (Rn)
Wikipedia CSNK1G3 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of casein kinase 1 gamma 3
PDB Id:  2CHL
Resolution:  1.95Å
Species:  Human
References: 
Image of receptor 3D structure from RCSB PDB
Description:  Structure of casein kinase gamma 3 in complex with inhibitor
PDB Id:  2IZR
Resolution:  1.3Å
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 14k [PMID: 21982499] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 4
⤷ [4]
Description: Measured as % inhibition using 0.5μM compound.
Inhibitor Comments
CSNK1G3 activity is inhibited by 79% in the presence of 0.5μM compound 14k [PMID 21982499] [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: CSNK1G3
Ligand Sp. Type Action Value Parameter
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
A-674563 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
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
PP-242 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: CK1γ3/CK1g3
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 6.9 56.0 13.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 13.4 75.0 16.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 17.3 72.0 13.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.8 29.0 7.0
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 30.0
CGP74514A Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 45.9 88.0 34.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 47.7 42.0 11.0
p38 MAP kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 58.4 96.0 21.0
IRAK-1/4 inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 58.7 89.0 67.0
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 58.8 51.0 11.0
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. Pierre F, Stefan E, Nédellec AS, Chevrel MC, Regan CF, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M et al.. (2011) 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett, 21 (22): 6687-92. [PMID:21982499]

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 3. Last modified on 29/01/2016. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2001.