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cyclin G associated kinase

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Target not currently curated in GtoImmuPdb

Target id: 2027

Nomenclature: cyclin G associated kinase

Abbreviated Name: GAK

Family: Numb-associated kinase (NAK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1311 4p16.3 GAK cyclin G associated kinase
Mouse - 1305 5 F Gak cyclin G associated kinase
Rat - 1305 14p22 Gak cyclin G associated kinase
Previous and Unofficial Names Click here for help
auxilin-2
Database Links Click here for help
Alphafold O14976 (Hs), Q99KY4 (Mm), P97874 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 1.10.287.110, 3.90.190.10
ChEMBL Target CHEMBL4355 (Hs)
Ensembl Gene ENSG00000178950 (Hs), ENSMUSG00000062234 (Mm), ENSRNOG00000000048 (Rn)
Entrez Gene 2580 (Hs), 231580 (Mm), 81659 (Rn)
Human Protein Atlas ENSG00000178950 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:2580 (Hs), mmu:231580 (Mm), rno:81659 (Rn)
OMIM 602052 (Hs)
Pharos O14976 (Hs)
RefSeq Nucleotide NM_005255 (Hs), XM_132229 (Mm), NM_031030 (Rn)
RefSeq Protein NP_005246 (Hs), NP_705797 (Mm), NP_112292 (Rn)
UniProtKB O14976 (Hs), Q99KY4 (Mm), P97874 (Rn)
Wikipedia GAK (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the human cyclin G associated kinase (GAK)
PDB Id:  3LL6
Resolution:  2.1Å
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
baricitinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.9 pKd 2
⤷ pKd 6.9 (Kd 1.36x10-7 M) [2]
Description: Binding affinity determined in a cell-free biochemical assay.
SB203580 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.9 pIC50
⤷ pIC50 6.9 (IC50 1.35x10-7 M)
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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: GAK
Ligand Sp. Type Action Value Parameter
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.9 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.6 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
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. 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]

2. Stebbing J, Phelan A, Griffin I, Tucker C, Oechsle O, Smith D, Richardson P. (2020) COVID-19: combining antiviral and anti-inflammatory treatments. Lancet Infect Dis, 20 (4): 400-402. [PMID:32113509]

3. 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

Numb-associated kinase (NAK) family: cyclin G associated kinase. Last modified on 09/03/2020. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2027.