protein kinase, X-linked

Nomenclature: protein kinase, X-linked

Abbreviated Name: PRKX

Family: Protein kinase A

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Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 358 Xp22.3 PRKX protein kinase, X-linked
Mouse - 355 X A7.3 Prkx protein kinase, X-linked
Rat - 358 X q22 Prkx protein kinase, X-linked
Previous and Unofficial Names
PKX1
serine/threonine-protein kinase PRKX
Pkare
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: PRKX
Ligand Sp. Type Action Affinity Units
GSK690693 Hs Inhibitor Inhibition 8.14 pKd
staurosporine Hs Inhibitor Inhibition 7.89 pKd
lestaurtinib Hs Inhibitor Inhibition 7.38 pKd
A-674563 Hs Inhibitor Inhibition 7.01 pKd
midostaurin Hs Inhibitor Inhibition 6.02 pKd
KW-2449 Hs Inhibitor Inhibition 5.92 pKd
SB203580 Hs Inhibitor Inhibition <5.52 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.52 pKd
erlotinib Hs Inhibitor Inhibition <5.52 pKd
linifanib Hs Inhibitor Inhibition <5.52 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: PrKX/PRKX
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
H-89 Hs Inhibitor Inhibition -2.5 0.0 0.0
staurosporine Hs Inhibitor Inhibition 3.5 0.0 0.0
K-252a Hs Inhibitor Inhibition 7.2 2.0 0.0
SB 218078 Hs Inhibitor Inhibition 17.5 84.0 53.0
fasudil Hs Inhibitor Inhibition 23.5 21.0 2.0
PKR inhibitor Hs Inhibitor Inhibition 28.2 24.0 6.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 43.5 37.0 4.0
Rho kinase inhibitor IV Hs Inhibitor Inhibition 54.2 57.0 13.0
Rho kinase inhibitor III Hs Inhibitor Inhibition 54.3 48.0 16.0
midostaurin Hs Inhibitor Inhibition 55.4 24.0 12.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol.29 (11): 1039-45. [PMID:22037377]

2. 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]

3. 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]

4. 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

Protein kinase A: protein kinase, X-linked. Last modified on 21/11/2013. Accessed on 25/10/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2175.