BR serine/threonine kinase 2 | BRSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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BR serine/threonine kinase 2

Target not currently curated in GtoImmuPdb

Target id: 1947

Nomenclature: BR serine/threonine kinase 2

Abbreviated Name: BRSK2

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 668 11p15.5 BRSK2 BR serine/threonine kinase 2
Mouse - 675 7 F5 Brsk2 BR serine/threonine kinase 2
Rat - - 1q41 Brsk2 BR serine/threonine kinase 2
Previous and Unofficial Names
PEN11B | SAD-A | serine/threonine kinase 29 | STK29
Database Links
BRENDA
ChEMBL Target
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 Value Parameter Reference
SU6656 Hs Inhibition 7.0 pIC50 2
pIC50 7.0 (IC50 1x10-7 M) [2]
CCT244747 Hs Inhibition - - 5
[5]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
BRSK2 activity is inhibited by 77% in the presence of 1μM CCT244747 [5].
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: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: BRSK2
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
PP-242 Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
midostaurin Hs Inhibitor Inhibition 6.2 pKd
sunitinib Hs Inhibitor Inhibition 6.0 pKd
TG-100-115 Hs Inhibitor Inhibition 5.9 pKd
KW-2449 Hs Inhibitor Inhibition 5.9 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: BrSK2/BRSK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 3.5 0.0 -1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 9.0 0.0 1.0
K-252a Hs Inhibitor Inhibition 9.8 1.0 0.0
PKR inhibitor Hs Inhibitor Inhibition 10.2 11.0 1.0
SB 218078 Hs Inhibitor Inhibition 13.6 53.0 52.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 15.9 10.0 1.0
midostaurin Hs Inhibitor Inhibition 16.4 4.0 3.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 19.4 4.0 6.0
JAK inhibitor I Hs Inhibitor Inhibition 21.4 13.0 4.0
Gö 6976 Hs Inhibitor Inhibition 26.3 7.0 6.0
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. Bain J, Plater L, Elliott M, Shpiro N, Hastie CJ, McLauchlan H, Klevernic I, Arthur JS, Alessi DR, Cohen P. (2007) The selectivity of protein kinase inhibitors: a further update. Biochem. J., 408 (3): 297-315. [PMID:17850214]

3. 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]

4. 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]

5. 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]

6. 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 2. Last modified on 24/02/2015. Accessed on 18/06/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1947.