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

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AP2 associated kinase 1

target has curated data 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
ChEMBL Target
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

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
Ligand Sp. Action Value Parameter Reference
compound 21b [PMID: 31136173] Hs Inhibition 8.4 pIC50 2
pIC50 8.4 (IC50 4x10-9 M) [2]
Description: Inhibition of kinase activity in a LanthaScreen® assay.
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: AAK1
Ligand Sp. Type Action Value 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 »
Immunopharmacology Comments
AAK1 is an antiviral drug target. Its inhibition by small molecules has the potential to offer promising broad-spectrum antiviral activity [2].
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 3 GO processes
GO:0030100 regulation of endocytosis IBA
GO:2000369 regulation of clathrin-dependent endocytosis IDA
click arrow to show/hide IEA associations
GO:0006897 endocytosis IEA

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. Verdonck S, Pu SY, Sorrell FJ, Elkins JM, Froeyen M, Gao LJ, Prugar LI, Dorosky DE, Brannan JM, Barouch-Bentov R et al.. (2019) Synthesis and structure-activity relationships of 3,5-disubstituted-pyrrolo[2,3- b]pyridines as inhibitors of adaptor associated kinase 1 (AAK1) with antiviral activity. J. Med. Chem., [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.9b00136 [PMID:31136173]

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

NAK family: AP2 associated kinase 1. Last modified on 06/06/2019. Accessed on 16/06/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1921.