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protein kinase AMP-activated catalytic subunit alpha 1

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Target not currently curated in GtoImmuPdb

Target id: 1541

Nomenclature: protein kinase AMP-activated catalytic subunit alpha 1

Abbreviated Name: AMPKA1

Family: AMPK subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 559 5p13.1 PRKAA1 protein kinase AMP-activated catalytic subunit alpha 1
Mouse - 559 15 Prkaa1 protein kinase, AMP-activated, alpha 1 catalytic subunit
Rat - 548 2q16 Prkaa1 protein kinase AMP-activated catalytic subunit alpha 1
Previous and Unofficial Names Click here for help
AMPK, alpha, 1 | AMPK alpha-1 chain | AMPK subunit alpha-1 | tau-protein kinase PRKAA1 | ACACA kinase | acetyl-CoA carboxylase kinase | HMGCR kinase | hydroxymethylglutaryl-CoA reductase kinase | AMPKa1 | protein kinase, AMP-activated, alpha 1 catalytic subunit | protein kinase
Database Links Click here for help
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.11.1
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: AMPK-alpha1
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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: 2...

Key to terms and symbols Click column headers to sort
Target used in screen: AMPKα1/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -2.0 -1.0
Tpl2 kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition -2.0 -1.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition -1.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition -0.5 0.0
indirubin-3'-monoxime Small molecule or natural product Hs Inhibitor Inhibition 2.0 0.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 2.0 10.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 4.0 4.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 6.0 1.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 3.0
Syk inhibitor Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 4.0
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. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

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

AMPK subfamily: protein kinase AMP-activated catalytic subunit alpha 1. Last modified on 30/03/2016. Accessed on 24/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1541.