Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	-	778	19q13.42	BRSK1	BR serine/threonine kinase 1
Mouse	-	778	7 A1	Brsk1	BR serine/threonine kinase 1
Rat	-	778	1q12	Brsk1	BR serine/threonine kinase 1

Previous and Unofficial Names

SAD-B

Database Links
Alphafold	Q8TDC3 (Hs), Q5RJI5 (Mm), B2DD29 (Rn)
BRENDA	2.7.11.1
ChEMBL Target	CHEMBL5650 (Hs)
Ensembl Gene	ENSG00000160469 (Hs), ENSMUSG00000035390 (Mm), ENSRNOG00000017673 (Rn)
Entrez Gene	84446 (Hs), 381979 (Mm), 499073 (Rn)
Human Protein Atlas	ENSG00000160469 (Hs)
KEGG Enzyme	2.7.11.1
KEGG Gene	hsa:84446 (Hs), mmu:381979 (Mm), rno:499073 (Rn)
OMIM	609235 (Hs)
Pharos	Q8TDC3 (Hs)
RefSeq Nucleotide	NM_032430 (Hs), NM_001168572 (Mm), NM_001127337 (Rn)
RefSeq Protein	NP_115806 (Hs), NP_001003920 (Mm), NP_001120809 (Rn)
UniProtKB	Q8TDC3 (Hs), Q5RJI5 (Mm), B2DD29 (Rn)
Wikipedia	BRSK1 (Hs)

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 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 Value Parameter 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
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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
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