mitogen-activated protein kinase kinase kinase 11 | MLK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 11

Target not currently curated in GtoImmuPdb

Target id: 2071

Nomenclature: mitogen-activated protein kinase kinase kinase 11

Abbreviated Name: MLK3

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 847 11q13.1-q13.3 MAP3K11 mitogen-activated protein kinase kinase kinase 11
Mouse - 850 19 A Map3k11 mitogen-activated protein kinase kinase kinase 11
Rat - 850 1 q43 Map3k11 mitogen-activated protein kinase kinase kinase 11
Previous and Unofficial Names
MEKK11 | mixed lineage kinase 3 | MLK3 | PTK1 | RHOE | SPRK | Src-homology 3 domain-containing proline-rich kinase
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 Value Parameter Reference
compound 8 [PMID: 24044867] Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3x10-9 M) [3]
CEP-1347 Hs Inhibition 7.6 – 8.2 pIC50 3-4
pIC50 7.6 – 8.2 (IC50 2.3x10-8 – 6x10-9 M) [3-4]
URMC-099 Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.4x10-8 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: MLK3
Ligand Sp. Type Action Value Parameter
tamatinib Hs Inhibitor Inhibition 8.0 pKd
midostaurin Hs Inhibitor Inhibition 7.8 pKd
lestaurtinib Hs Inhibitor Inhibition 7.7 pKd
staurosporine Hs Inhibitor Inhibition 7.7 pKd
KW-2449 Hs Inhibitor Inhibition 6.6 pKd
foretinib Hs Inhibitor Inhibition 6.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.4 pKd
PD-173955 Hs Inhibitor Inhibition 6.3 pKd
tozasertib Hs Inhibitor Inhibition 6.2 pKd
pazopanib Hs Inhibitor Inhibition 6.1 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/MLK3(MAP3K11)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 0.7
staurosporine Hs Inhibitor Inhibition 1.1
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 1.3
midostaurin Hs Inhibitor Inhibition 1.4
SB 218078 Hs Inhibitor Inhibition 1.4
Gö 6976 Hs Inhibitor Inhibition 2.2
Cdk2 inhibitor IV Hs Inhibitor Inhibition 5.6
JAK3 inhibitor VI Hs Inhibitor Inhibition 8.7
Syk inhibitor Hs Inhibitor Inhibition 9.9
indirubin derivative E804 Hs Inhibitor Inhibition 10.5
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. 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 11. Last modified on 20/02/2015. Accessed on 21/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2071.