mitogen-activated protein kinase kinase kinase 10 | MLK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

mitogen-activated protein kinase kinase kinase 10

Target id: 2070

Nomenclature: mitogen-activated protein kinase kinase kinase 10

Abbreviated Name: MLK2

Family: MLK subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for mitogen-activated protein kinase kinase kinase 10 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 940 19q13.2 MAP3K10 mitogen-activated protein kinase kinase kinase 10
Mouse - 942 7 A3 Map3k10 mitogen-activated protein kinase kinase kinase 10
Rat - 942 1 q21 Map3k10 mitogen activated protein kinase kinase kinase 10
Previous and Unofficial Names
mixed lineage kinase 2 | MKN28 kinase | MLK2 | MST
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human mixed lineage kinase MAP3K10 SH3 domain
PDB Id:  2RF0
Resolution:  2.0Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.25

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 Affinity Units Reference
CEP-1347 Hs Inhibition 7.3 – 8.7 pIC50 3-4
pIC50 7.3 – 8.7 (IC50 5.1x10-8 – 2x10-9 M) [3-4]
URMC-099 Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4.2x10-8 M) [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: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: MLK2
Ligand Sp. Type Action Affinity Units
tamatinib Hs Inhibitor Inhibition 8.4 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
staurosporine Hs Inhibitor Inhibition 7.3 pKd
foretinib Hs Inhibitor Inhibition 6.3 pKd
midostaurin Hs Inhibitor Inhibition 6.1 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.0 pKd
KW-2449 Hs Inhibitor Inhibition 5.8 pKd
tozasertib Hs Inhibitor Inhibition 5.7 pKd
pazopanib Hs Inhibitor Inhibition 5.7 pKd
SB203580 Hs Inhibitor Inhibition <5.5 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/MLK2(MAP3K10)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 2.5
SB 218078 Hs Inhibitor Inhibition 2.7
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 3.0
midostaurin Hs Inhibitor Inhibition 3.1
staurosporine Hs Inhibitor Inhibition 3.3
Cdk2 inhibitor IV Hs Inhibitor Inhibition 15.2
bosutinib Hs Inhibitor Inhibition 22.9
Gö 6976 Hs Inhibitor Inhibition 25.8
pazopanib Hs Inhibitor Inhibition 28.5
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 30.0
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. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J. Med. Chem., 56 (20): 8032-48. [PMID:24044867]

4. Maroney AC, Finn JP, Connors TJ, Durkin JT, Angeles T, Gessner G, Xu Z, Meyer SL, Savage MJ, Greene LA et al.. (2001) Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. J. Biol. Chem., 276 (27): 25302-8. [PMID:11325962]

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

MLK subfamily: mitogen-activated protein kinase kinase kinase 10. Last modified on 18/02/2015. Accessed on 15/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2070.