cyclin G associated kinase | Numb-associated kinase (NAK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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cyclin G associated kinase

Target not currently curated in GtoImmuPdb

Target id: 2027

Nomenclature: cyclin G associated kinase

Abbreviated Name: GAK

Family: Numb-associated kinase (NAK) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1311 4p16 GAK cyclin G associated kinase
Mouse - 1305 5 F Gak cyclin G associated kinase
Rat - 1305 14 p22 Gak cyclin G associated kinase
Previous and Unofficial Names
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
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
Enzyme Reaction
EC Number:

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Ligand Sp. Action Affinity Parameter Reference
SB203580 Hs Inhibition 6.9 pIC50
pIC50 6.9 (IC50 1.35x10-7 M)
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: GAK
Ligand Sp. Type Action Affinity Parameter
fedratinib Hs Inhibitor Inhibition 9.0 pKd
bosutinib Hs Inhibitor Inhibition 8.9 pKd
dasatinib Hs Inhibitor Inhibition 8.6 pKd
erlotinib Hs Inhibitor Inhibition 8.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.3 pKd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd
PD-173955 Hs Inhibitor Inhibition 8.1 pKd
gefitinib Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 7.8 pKd
SB203580 Hs Inhibitor Inhibition 7.7 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »


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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. 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 06/02/2015. Accessed on 21/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY,