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TargetDisintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
LigandBDBM23478
Substrate/CompetitorBDBM23453
Meas. Tech.TACE Inhibition Assay
pH7.3±n/a
Temperature295.15±n/a K
Ki 100±n/a nM
Citation Zhu, ZMazzola, RSinning, LMcKittrick, BNiu, XLundell, DSun, JOrth, PGuo, ZMadison, VIngram, RBeyer, BM Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors: Part I--discovery of two binding modes. J Med Chem51:725-36 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Name:Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Synonyms:A disintegrin and metalloproteinase domain 17 | ADA17_HUMAN | ADAM 17 | ADAM17 | CD156b antigen | CSVP | Snake venom-like protease | TACE | TNF-alpha-Converting Enzyme
Type:Single-pass type I membrane protein; metalloprotease
Mol. Mass.:29695.98
Organism:Homo sapiens (Human)
Description:The catalytic domain of recombinant human TNF-converting enzyme (residues 215-477) with two mutations (S266A and N452Q) and a 6xHis was purified from the baculovirus/Hi5 cells expression system.
Residue:263
Sequence:
RADPDPMKNTCKLLVVADHRFYRYMGRGEESTTTNYLIELIDRVDDIYRNTAWDNAGFKG
YGIQIEQIRILKSPQEVKPGEKHYNMAKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCL
AHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTI
LTKEADLVTTHELGHNFGAEHDPDGLAECAPNEDQGGKYVMYPIAVSGDHENNKMFSQCS
KQSIYKTIESKAQECFQERSNKV
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  Blast E-value cutoff:
BDBM23478
BDBM23453
NameBDBM23478
Synonyms:(1R,2R)-2-N-hydroxy-1-N-methyl-1-{3-[(2-methylquinolin-4-yl)methoxy]phenyl}cyclopropane-1,2-dicarboxamide | hydroxamate deriv., 70
TypeSmall organic molecule
Emp. Form.C23H23N3O4
Mol. Mass.405.4464
SMILESCNC(=O)[C@@]1(C[C@H]1C(=O)NO)c1cccc(OCc2cc(C)nc3ccccc23)c1 |r|
Structure
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