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mitogen-activated protein kinase kinase kinase 13

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Target id: 2073

Nomenclature: mitogen-activated protein kinase kinase kinase 13

Abbreviated Name: LZK

Family: LZK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 966 3q27.2 MAP3K13 mitogen-activated protein kinase kinase kinase 13
Mouse - 959 16 B1 Map3k13 mitogen-activated protein kinase kinase kinase 13
Rat - 958 11 q23 Map3k13 mitogen-activated protein kinase kinase kinase 13
Previous and Unofficial Names Click here for help
LZK | MEKK13
Database Links Click here for help
Alphafold O43283 (Hs), Q1HKZ5 (Mm)
BRENDA 2.7.11.25
ChEMBL Target CHEMBL1163124 (Hs)
Ensembl Gene ENSG00000073803 (Hs), ENSMUSG00000033618 (Mm), ENSRNOG00000025423 (Rn)
Entrez Gene 9175 (Hs), 71751 (Mm), 303823 (Rn)
Human Protein Atlas ENSG00000073803 (Hs)
KEGG Enzyme 2.7.11.25
KEGG Gene hsa:9175 (Hs), mmu:71751 (Mm), rno:303823 (Rn)
OMIM 604915 (Hs)
Pharos O43283 (Hs)
RefSeq Nucleotide NM_001242314 (Hs), NM_172821 (Mm), NM_001013978 (Rn)
RefSeq Protein NP_004712 (Hs), NP_766409 (Mm), NP_001014000 (Rn)
UniProtKB O43283 (Hs), Q1HKZ5 (Mm)
Wikipedia MAP3K13 (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
GNE-3511 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >9.3 pKi 2
⤷ pKi >9.3 (Ki <5x10-10 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: LZK
Ligand Sp. Type Action Value Parameter
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 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. Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP et al.. (2015) Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. J Med Chem, 58 (1): 401-18. [PMID:25341110]

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

LZK subfamily: mitogen-activated protein kinase kinase kinase 13. Last modified on 04/11/2016. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2073.