mitogen-activated protein kinase kinase kinase 3 | STE11 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 3

Target not currently curated in GtoImmuPdb

Target id: 2078

Nomenclature: mitogen-activated protein kinase kinase kinase 3

Abbreviated Name: MEKK3

Family: STE11 family

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 - 626 17q MAP3K3 mitogen-activated protein kinase kinase kinase 3
Mouse - 626 11 E1 Map3k3 mitogen-activated protein kinase kinase kinase 3
Rat - 626 10 q32.1 Map3k3 mitogen activated protein kinase kinase kinase 3
Previous and Unofficial Names
MAP/ERK kinase kinase 3 | MAPKKK3
Database Links
BRENDA
ChEMBL Target
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 the Complex of Human Mitogen Activated Protein Kinase Kinase 5 Phox Domain (MAP2K5-phox) with Human Mitogen Activated Protein Kinase Kinase Kinase 3 (MAP3K3B-phox)
PDB Id:  2O2V
Resolution:  1.83Å
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 Parameter Reference
compound 5n [PMID: 20483621] Hs Inhibition - - 3
[3]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
1μM compound 5n [PMID 20483621] inhibits MAP3K3 activity by 88% [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: MAP3K3
Ligand Sp. Type Action Affinity Parameter
lestaurtinib Hs Inhibitor Inhibition 8.2 pKd
bosutinib Hs Inhibitor Inhibition 7.3 pKd
crizotinib Hs Inhibitor Inhibition 7.0 pKd
KW-2449 Hs Inhibitor Inhibition 6.9 pKd
neratinib Hs Inhibitor Inhibition 6.9 pKd
tamatinib Hs Inhibitor Inhibition 6.8 pKd
ruxolitinib Hs Inhibitor Inhibition 6.8 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.8 pKd
midostaurin Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.7 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/MEKK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 5.4
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 5.4
Gö 6976 Hs Inhibitor Inhibition 5.9
K-252a Hs Inhibitor Inhibition 6.9
bosutinib Hs Inhibitor Inhibition 11.8
SB 218078 Hs Inhibitor Inhibition 18.4
JNJ-7706621 Hs Inhibitor Inhibition 27.5
SU11652 Hs Inhibitor Inhibition 30.6
midostaurin Hs Inhibitor Inhibition 31.0
sunitinib Hs Inhibitor Inhibition 42.0
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. Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA et al.. (2010) Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg. Med. Chem., 18 (12): 4351-62. [PMID:20483621]

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

STE11 family: mitogen-activated protein kinase kinase kinase 3. Last modified on 24/02/2015. Accessed on 24/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2078.