casein kinase 1 gamma 3 | Casein kinase 1 (CK1) family | IUPHAR/BPS Guide to PHARMACOLOGY

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casein kinase 1 gamma 3

Target id: 2001

Nomenclature: casein kinase 1 gamma 3

Abbreviated Name: CK1-G3

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

   GtoImmuPdb view: OFF :     Currently no data for casein kinase 1 gamma 3 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 423 5q23 CSNK1G3 casein kinase 1 gamma 3
Mouse - 424 18 D1-D2 Csnk1g3 casein kinase 1, gamma 3
Rat - 448 18 q11 Csnk1g3 casein kinase 1, gamma 3
Previous and Unofficial Names
CKI-gamma 3 | casein kinase 1
Database Links
BRENDA
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 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
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 Affinity Units Reference
compound 14k [PMID: 21982499] 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
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 Affinity Units
AST-487 Hs Inhibitor Inhibition 7.0 pKd
sunitinib Hs Inhibitor Inhibition 6.6 pKd
SU-14813 Hs Inhibitor Inhibition 6.2 pKd
A-674563 Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Hs Inhibitor Inhibition 5.9 pKd
BI-2536 Hs Inhibitor Inhibition 5.6 pKd
PP-242 Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib 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: CK1γ3/CK1g3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 6.9 56.0 13.0
aminopurvalanol A Hs Inhibitor Inhibition 13.4 75.0 16.0
purvalanol A Hs Inhibitor Inhibition 17.3 72.0 13.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 20.8 29.0 7.0
sunitinib Hs Inhibitor Inhibition 30.0
CGP74514A Hs Inhibitor Inhibition 45.9 88.0 34.0
SU11652 Hs Inhibitor Inhibition 47.7 42.0 11.0
p38 MAP kinase inhibitor III Hs Inhibitor Inhibition 58.4 96.0 21.0
IRAK-1/4 inhibitor Hs Inhibitor Inhibition 58.7 89.0 67.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 58.8 51.0 11.0
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. 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 13/12/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2001.