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SRSF protein kinase 3

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Target not currently curated in GtoImmuPdb

Target id: 2210

Nomenclature: SRSF protein kinase 3

Abbreviated Name: MSSK1

Family: SRPK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 567 Xq28 SRPK3 SRSF protein kinase 3
Mouse - 565 X A7.3 Srpk3 serine/arginine-rich protein specific kinase 3
Rat - 563 X q37 Srpk3 SRSF protein kinase 3
Previous and Unofficial Names Click here for help
muscle-specific serine kinase 1 | serine/threonine kinase 23 | STK23
Database Links Click here for help
Alphafold Q9UPE1 (Hs), Q9Z0G2 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5415 (Hs)
Ensembl Gene ENSG00000184343 (Hs), ENSMUSG00000002007 (Mm), ENSRNOG00000054548 (Rn)
Entrez Gene 26576 (Hs), 56504 (Mm), 293854 (Rn)
Human Protein Atlas ENSG00000184343 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:26576 (Hs), mmu:56504 (Mm), rno:293854 (Rn)
Pharos Q9UPE1 (Hs)
RefSeq Nucleotide NM_001170760 (Hs), NM_019684 (Mm), NM_184045 (Rn)
RefSeq Protein NP_055185 (Hs), NP_062658 (Mm), NP_908934 (Rn)
UniProtKB Q9UPE1 (Hs), Q9Z0G2 (Mm)
Wikipedia SRPK3 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 25 [PMID: 17935989] Small molecule or natural product Click here for species-specific activity table Hs Inhibition <5.8 pKi 4
⤷ pKi <5.8 (Ki >1.736x10-6 M) [4]
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: 2,5
Key to terms and symbols Click column headers to sort
Target used in screen: SRPK3
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand 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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: MSSK1/MSSK1(STK23)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 26.8 11.0 2.0
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 37.7 40.0 12.0
compound 52 [PMID: 9677190] Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 47.7 61.0 19.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 48.7 37.0 12.0
JAK inhibitor I Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 58.6 79.0 75.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 59.5 62.0 42.0
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 61.5 46.0 16.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 63.6 99.0 96.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 66.9 124.0 100.0
SU6656 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 67.2 98.0 77.0
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. Tao ZF, Chen Z, Bui MH, Kovar P, Johnson E, Bouska J, Zhang H, Rosenberg S, Sowin T, Lin NH. (2007) Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg Med Chem Lett, 17 (23): 6593-601. [PMID:17935989]

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

SRPK family: SRSF protein kinase 3. Last modified on 11/09/2015. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2210.