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myosin light chain kinase family member 4

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Target not currently curated in GtoImmuPdb

Target id: 2111

Nomenclature: myosin light chain kinase family member 4

Abbreviated Name: Sgk085

Family: Myosin Light Chain Kinase (MLCK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 388 6p25.2 MYLK4 myosin light chain kinase family member 4
Mouse - 386 13 A3.2 Mylk4 myosin light chain kinase family, member 4
Previous and Unofficial Names Click here for help
Sugen kinase 85 | myosin light chain kinase family, member 4 | myosin light chain kinase family
Database Links Click here for help
Alphafold Q86YV6 (Hs), Q5SUV5 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5426 (Hs)
Ensembl Gene ENSG00000145949 (Hs), ENSMUSG00000044951 (Mm)
Entrez Gene 340156 (Hs), 238564 (Mm)
Human Protein Atlas ENSG00000145949 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:340156 (Hs), mmu:238564 (Mm)
Pharos Q86YV6 (Hs)
RefSeq Nucleotide NM_001012418 (Hs), NM_001166030 (Mm)
RefSeq Protein NP_001012418 (Hs), NP_001159502 (Mm)
UniProtKB Q86YV6 (Hs), Q5SUV5 (Mm)
Wikipedia MYLK4 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  The Crystal Structure of the human myosin light chain kinase LOC340156.
PDB Id:  2X4F
Resolution:  2.67Å
Species:  Human
References: 
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 17 [PMID: 36111834] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 2
⤷ pIC50 6.6 (IC50 2.65x10-7 M) [2]
Description: Determined in a cell-based NanoBRET assay
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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: MYLK4
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.5 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
BMS-345541 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. Drewry DH, Potjewyd FM, Bayati A, Smith JL, Dickmander RJ, Howell S, Taft-Benz S, Min SM, Hossain MA, Heise M et al.. (2022) Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses. J Med Chem, 65 (19): 12860-12882. [PMID:36111834]

3. 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

Myosin Light Chain Kinase (MLCK) family: myosin light chain kinase family member 4. Last modified on 20/09/2022. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2111.