BR serine/threonine kinase 1 | BRSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

BR serine/threonine kinase 1

Target id: 1946

Nomenclature: BR serine/threonine kinase 1

Abbreviated Name: BRSK1

Family: BRSK subfamily

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

   GtoImmuPdb view: OFF :     Currently no data for BR serine/threonine kinase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 778 19q13.4 BRSK1 BR serine/threonine kinase 1
Mouse - 778 7 A1 Brsk1 BR serine/threonine kinase 1
Rat - 778 1 q12 Brsk1 BR serine/threonine kinase 1
Previous and Unofficial Names
SAD-B
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
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 Affinity Units Reference
CCT244747 Hs Inhibition - - 4
[4]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
BRSK1 activity is inhibited by 89% in the presence of 1μM CCT244747 [4].
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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: BRSK1
Ligand Sp. Type Action Affinity Units
PP-242 Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Hs Inhibitor Inhibition 7.6 pKd
staurosporine Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.5 pKd
TG-100-115 Hs Inhibitor Inhibition 6.1 pKd
midostaurin Hs Inhibitor Inhibition 5.9 pKd
KW-2449 Hs Inhibitor Inhibition 5.7 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 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: BrSK1/BRSK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.5 1.0 -0.5
K-252a Hs Inhibitor Inhibition 1.6 -1.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.6 0.0 0.0
PKR inhibitor Hs Inhibitor Inhibition 10.0 2.0 1.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 14.6 33.0 12.0
SB 218078 Hs Inhibitor Inhibition 14.8 98.0 95.0
JAK inhibitor I Hs Inhibitor Inhibition 15.4 32.0 7.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 19.7 1.0 2.0
Gö 6976 Hs Inhibitor Inhibition 20.2 6.0 6.0
midostaurin Hs Inhibitor Inhibition 21.1 3.0 3.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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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. Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, Hayes A, Valenti MR, de Haven Brandon AK, Box G et al.. (2012) Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. J. Med. Chem., 55 (22): 10229-40. [PMID:23082860]

5. 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

BRSK subfamily: BR serine/threonine kinase 1. Last modified on 24/02/2015. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1946.