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Target not currently curated in GtoImmuPdb
Target id: 2145
Nomenclature: phosphorylase kinase catalytic subunit gamma 1
Abbreviated Name: PHKG1
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 387 | 7p11.2 | PHKG1 | phosphorylase kinase catalytic subunit gamma 1 | |
Mouse | - | 388 | 5 68.26 cM | Phkg1 | phosphorylase kinase gamma 1 | |
Rat | - | 388 | 12q13 | Phkg1 | phosphorylase kinase catalytic subunit gamma 1 |
Previous and Unofficial Names |
gamma phosphorylase kinase | HK-gamma-M | PHKIN01 | phosphorylase kinase, gamma 1 (muscle) | phosphorylase kinase gamma subunit 1 | phosphorylase kinase |
Database Links | |
Alphafold | Q16816 (Hs), P07934 (Mm), P13286 (Rn) |
BRENDA | 2.7.11.19 |
ChEMBL Target | CHEMBL4004 (Hs) |
Ensembl Gene | ENSG00000164776 (Hs), ENSMUSG00000025537 (Mm), ENSRNOG00000000920 (Rn) |
Entrez Gene | 5260 (Hs), 18682 (Mm), 29353 (Rn) |
Human Protein Atlas | ENSG00000164776 (Hs) |
KEGG Enzyme | 2.7.11.19 |
KEGG Gene | hsa:5260 (Hs), mmu:18682 (Mm), rno:29353 (Rn) |
OMIM | 172470 (Hs) |
Orphanet | ORPHA352609 (Hs) |
Pharos | Q16816 (Hs) |
RefSeq Nucleotide | NM_001258459 (Hs), NM_011079 (Mm), NM_031573 (Rn) |
RefSeq Protein | NP_006204 (Hs), NP_035209 (Mm), NP_113761 (Rn) |
UniProtKB | Q16816 (Hs), P07934 (Mm), P13286 (Rn) |
Wikipedia | PHKG1 (Hs) |
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 | |||||||||||||||||||||||||||||||||||||||||||||||||||
A-443654 inhibits PHKG1 activity by approximately 76% using 1μM compound [3]. |
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: 2,4 |
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Target used in screen: PHKG1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 |
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Target used in screen: nd/PHKg1 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Clinically-Relevant Mutations and Pathophysiology | ||||||||||||
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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. Okuzumi T, Fiedler D, Zhang C, Gray DC, Aizenstein B, Hoffman R, Shokat KM. (2009) Inhibitor hijacking of Akt activation. Nat Chem Biol, 5 (7): 484-93. [PMID:19465931]
4. 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]
Phosphorylase kinase (PHK) family: phosphorylase kinase catalytic subunit gamma 1. Last modified on 30/03/2016. Accessed on 18/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2145.