AP2 associated kinase 1 | NAK family | IUPHAR/BPS Guide to PHARMACOLOGY

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AP2 associated kinase 1

Target not currently curated in GtoImmuPdb

Target id: 1921

Nomenclature: AP2 associated kinase 1

Abbreviated Name: AAK1

Family: 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 - 961 2p13.3 AAK1 AP2 associated kinase 1
Mouse - 959 6 D1 Aak1 AP2 associated kinase 1
Rat - 963 4 q34 Aak1 AP2 associated kinase 1
Previous and Unofficial Names
adaptor-associated kinase 1 | LMTK1
Database Links
BRENDA
CATH/Gene3D
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1
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: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: AAK1
Ligand Sp. Type Action Affinity Parameter
staurosporine Hs Inhibitor Inhibition 8.9 pKd
lestaurtinib Hs Inhibitor Inhibition 8.5 pKd
sunitinib Hs Inhibitor Inhibition 8.0 pKd
fedratinib Hs Inhibitor Inhibition 7.5 pKd
A-674563 Hs Inhibitor Inhibition 7.4 pKd
KW-2449 Hs Inhibitor Inhibition 7.3 pKd
midostaurin Hs Inhibitor Inhibition 7.3 pKd
SU-14813 Hs Inhibitor Inhibition 7.2 pKd
ruxolitinib Hs Inhibitor Inhibition 6.9 pKd
dovitinib Hs Inhibitor Inhibition 6.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

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. 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

NAK family: AP2 associated kinase 1. Last modified on 18/08/2014. Accessed on 26/03/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1921.