muscle associated receptor tyrosine kinase | Type IX RTKs: MuSK | IUPHAR Guide to IMMUNOPHARMACOLOGY

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muscle associated receptor tyrosine kinase

Target not currently curated in GtoImmuPdb

Target id: 1847

Nomenclature: muscle associated receptor tyrosine kinase

Abbreviated Name: MuSK

Family: Type IX RTKs: MuSK

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 869 9q31.3-q32 MUSK muscle associated receptor tyrosine kinase
Mouse 1 893 4 Musk muscle
Rat 1 868 5q24 Musk muscle associated receptor tyrosine kinase
Previous and Unofficial Names
muscle specific kinase (neural fold/somite kinase 1) | muscle-specific tyrosine protein kinase receptor | Nsk1 | MDK4 | Nsk2 | Nsk3 | muscle, skeletal, receptor tyrosine kinase | muscle
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the MuSK Tyrosine Kinase: Insights into Receptor Autoregulation
Resolution:  2.05Å
Species:  Rat
References:  5
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 25 [PMID: 17935989] Hs Inhibition 5.8 pKi 4
pKi 5.8 (Ki 1.65x10-6 M) [4]
compound 1d [PMID: 21493067] Hs Inhibition 6.7 pIC50 6
pIC50 6.7 (IC50 2.24x10-7 M) [6]
Inhibitor Comments
Compound 25 [PMID 17935989] is a CHK1 inhibitor and interacts with MUSK as an off-target. Inhibiton of CHK1 is >400 times more potent than inhibition of MUSK [4]. Similarly MUSK is an off-target of the JAK2 inhibitor compound 1d [PMID 21493067] [6].
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: MUSK
Ligand Sp. Type Action Value Parameter
AST-487 Hs Inhibitor Inhibition 8.5 pKd
linifanib Hs Inhibitor Inhibition 8.0 pKd
foretinib Hs Inhibitor Inhibition 7.9 pKd
staurosporine Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Hs Inhibitor Inhibition 7.0 pKd
tamatinib Hs Inhibitor Inhibition 7.0 pKd
sorafenib Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Hs Inhibitor Inhibition 6.7 pKd
crizotinib Hs Inhibitor Inhibition 6.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.6 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.

Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: MuSK/MUSK
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 6.1 18.0 2.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 6.1 25.0 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 8.0 0.0 0.0
staurosporine Hs Inhibitor Inhibition 12.2 -1.0 0.5
JNK inhibitor V Hs Inhibitor Inhibition 14.8 90.0 50.0
PI 3-Kg inhibitor Hs Inhibitor Inhibition 16.2 90.0 75.0
PKR inhibitor Hs Inhibitor Inhibition 21.6 53.0 11.0
SB 218078 Hs Inhibitor Inhibition 25.8 103.0 93.0
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 28.4 82.0 75.0
Gö 6976 Hs Inhibitor Inhibition 34.8 32.0 37.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Myasthenic syndrome, congenital, 9, associated with acetylcholine receptor deficiency; CMS9
Synonyms: Congenital myasthenic syndrome [Orphanet: ORPHA590] [Disease Ontology: DOID:3635]
Postsynaptic congenital myasthenic syndromes [Orphanet: ORPHA98913]
Disease Ontology: DOID:3635
OMIM: 616325
Orphanet: ORPHA590, ORPHA98913


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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. Till JH, Becerra M, Watty A, Lu Y, Ma Y, Neubert TA, Burden SJ, Hubbard SR. (2002) Crystal structure of the MuSK tyrosine kinase: insights into receptor autoregulation. Structure, 10 (9): 1187-96. [PMID:12220490]

6. Wang T, Ioannidis S, Almeida L, Block MH, Davies AM, Lamb ML, Scott DA, Su M, Zhang HJ, Alimzhanov M et al.. (2011) In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors. Bioorg. Med. Chem. Lett., 21 (10): 2958-61. [PMID:21493067]

7. 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

Type IX RTKs: MuSK: muscle associated receptor tyrosine kinase. Last modified on 05/05/2015. Accessed on 27/09/2020. IUPHAR/BPS Guide to PHARMACOLOGY,