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Target id: 2001
Nomenclature: casein kinase 1 gamma 3
Abbreviated Name: CK1-G3
Family: Casein kinase 1 (CK1) family
Gene and Protein Information | ||||||
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 |
CKI-gamma 3 | casein kinase 1 |
Database Links | |
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 | |||||||||||
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Enzyme Reaction | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||
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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 |
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Target used in screen: CSNK1G3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 |
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Target used in screen: CK1γ3/CK1g3 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immuno Process Associations | ||
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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]
Casein kinase 1 (CK1) family: casein kinase 1 gamma 3. Last modified on 29/01/2016. Accessed on 10/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2001.