src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites | Src family | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

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src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites

Target id: 2207

Nomenclature: src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites

Abbreviated Name: Srm

Family: Src family

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 488 20q13.33 SRMS src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites
Mouse - 507 2 H4 Srms src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites
Rat - 507 3 q43 Srms src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites
Previous and Unofficial Names
SRM
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.10.2

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
compound 66 [PMID: 21802293] Hs Inhibition - - 3
[3]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
SRMS activity is inhibited by 98% in the presence of 1μM compound 66 [PMID 21802293] [3].
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: SRMS
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 7.9 pKd
foretinib Hs Inhibitor Inhibition 7.7 pKd
PLX-4720 Hs Inhibitor Inhibition 7.7 pKd
SU-14813 Hs Inhibitor Inhibition 7.2 pKd
AST-487 Hs Inhibitor Inhibition 7.1 pKd
bosutinib Hs Inhibitor Inhibition 7.0 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
Ki-20227 Hs Inhibitor Inhibition 6.4 pKd
PD-173955 Hs Inhibitor Inhibition 6.2 pKd
tamatinib Hs Inhibitor Inhibition 6.2 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

Key to terms and symbols Click column headers to sort
Target used in screen: nd/SRMS
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 6.3
Lck inhibitor Hs Inhibitor Inhibition 14.2
dasatinib Hs Inhibitor Inhibition 17.0
Src kinase inhibitor I Hs Inhibitor Inhibition 31.6
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 78.6
bohemine Hs Inhibitor Inhibition 82.0
bisindolylmaleimide IV Hs Inhibitor Inhibition 82.4
Cdk4 inhibitor III Hs Inhibitor Inhibition 82.4
Chk2 inhibitor II Hs Inhibitor Inhibition 83.1
Cdk4 inhibitor II Hs Inhibitor Inhibition 83.5
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. Wenglowsky S, Ahrendt KA, Buckmelter AJ, Feng B, Gloor SL, Gradl S, Grina J, Hansen JD, Laird ER, Lunghofer P et al.. (2011) Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships. Bioorg. Med. Chem. Lett., 21 (18): 5533-7. [PMID:21802293]

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

Src family: src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites. Last modified on 24/02/2015. Accessed on 24/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2207.