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mitogen-activated protein kinase kinase kinase 15

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Target not currently curated in GtoImmuPdb

Target id: 2075

Nomenclature: mitogen-activated protein kinase kinase kinase 15

Abbreviated Name: MAP3K15

Family: STE11 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1313 Xp22.12 MAP3K15 mitogen-activated protein kinase kinase kinase 15
Mouse - 1331 X F4 Map3k15 mitogen-activated protein kinase kinase kinase 15
Rat - - Xq21 Map3k15 mitogen-activated protein kinase kinase kinase 15
Previous and Unofficial Names Click here for help
apoptosis signal-regulating kinase 3 | ASK3
Database Links Click here for help
Alphafold Q6ZN16 (Hs), A2AQW0 (Mm)
BRENDA 2.7.11.25
ChEMBL Target CHEMBL1163127 (Hs)
Ensembl Gene ENSG00000180815 (Hs), ENSMUSG00000031303 (Mm), ENSRNOG00000025290 (Rn)
Entrez Gene 389840 (Hs), 270672 (Mm), 501558 (Rn)
Human Protein Atlas ENSG00000180815 (Hs)
KEGG Enzyme 2.7.11.25
KEGG Gene hsa:389840 (Hs), mmu:270672 (Mm), rno:501558 (Rn)
OMIM 300820 (Hs)
Pharos Q6ZN16 (Hs)
RefSeq Nucleotide NM_001001671 (Hs), NM_001163085 (Mm)
RefSeq Protein NP_001001671 (Hs), NP_001156557 (Mm)
UniProtKB Q6ZN16 (Hs), A2AQW0 (Mm)
Wikipedia MAP3K15 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.25
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: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: MAP3K15
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.5 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 5.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 5.6 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.6 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin 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. 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 15. Last modified on 18/08/2014. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2075.