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mitogen-activated protein kinase kinase kinase 6

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Target not currently curated in GtoImmuPdb

Target id: 2081

Nomenclature: mitogen-activated protein kinase kinase kinase 6

Abbreviated Name: MEKK6

Family: STE11 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1288 1p36.11 MAP3K6 mitogen-activated protein kinase kinase kinase 6
Mouse - 1291 4 D2.3 Map3k6 mitogen-activated protein kinase kinase kinase 6
Rat - 1292 5 q36 Map3k6 mitogen-activated protein kinase kinase kinase 6
Previous and Unofficial Names Click here for help
apoptosis signal regulating kinase 2 | ASK2 | MAPKKK6
Database Links Click here for help
Alphafold O95382 (Hs), Q9WTR2 (Mm)
BRENDA 2.7.11.25
CATH/Gene3D 1.25.40.10
ChEMBL Target CHEMBL1163123 (Hs)
Ensembl Gene ENSG00000142733 (Hs), ENSMUSG00000028862 (Mm), ENSRNOG00000008936 (Rn)
Entrez Gene 9064 (Hs), 53608 (Mm), 313022 (Rn)
Human Protein Atlas ENSG00000142733 (Hs)
KEGG Enzyme 2.7.11.25
KEGG Gene hsa:9064 (Hs), mmu:53608 (Mm), rno:313022 (Rn)
OMIM 604468 (Hs)
Pharos O95382 (Hs)
RefSeq Nucleotide NM_004672 (Hs), NM_016693 (Mm), NM_001107909 (Rn)
RefSeq Protein NP_004663 (Hs), NP_057902 (Mm), NP_001101379 (Rn)
UniProtKB O95382 (Hs), Q9WTR2 (Mm)
Wikipedia MAP3K6 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.25

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 10 [PMID: 23147077] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 2
⤷ pIC50 6.3 (IC50 5.1x10-7 M) [2]
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: ASK2
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition <5.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 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. Terao Y, Suzuki H, Yoshikawa M, Yashiro H, Takekawa S, Fujitani Y, Okada K, Inoue Y, Yamamoto Y, Nakagawa H et al.. (2012) Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. Bioorg Med Chem Lett, 22 (24): 7326-9. [PMID:23147077]

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

STE11 family: mitogen-activated protein kinase kinase kinase 6. Last modified on 09/02/2015. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2081.