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Target
Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Ligand
BDBM92441
Substrate
n/a
Meas. Tech.
Enzyme Assay
pH
6.8±0
Temperature
298.15±0 K
Ki
>10000±0.0 nM
Citation
 Devel, L; Garcia, S; Czarny, B; Beau, F; LaJeunesse, E; Vera, L; Georgiadis, D; Stura, E; Dive, V Insights from selective non-phosphinic inhibitors of MMP-12 tailored to fit with an S1' loop canonical conformation. J Biol Chem 285:35900-9 (2010) [PubMed]  Article 
Target
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:
RADPDPMKNTCKLLVVADHRFYRYMGRGEESTTTNYLIELIDRVDDIYRNTAWDNAGFKGYGIQIEQIRILKSPQEVKPGEKHYNMAKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGLAECAPNEDQGGKYVMYPIAVSGDHENNKMFSQCSKQSIYKTIESKAQECFQERSNKV
  
Inhibitor
Name:
BDBM92441
Synonyms:
RXP470, 1 | RXP470, Compound 4
Type:
Peptide
Emp. Form.:
C35H35BrClN4O10P
Mol. Mass.:
818.004
SMILES:
NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)C(Cc1cc(no1)-c1ccc(cc1)-c1cccc(Cl)c1)CP(O)(=O)c1ccc(Br)cc1 |r|
Structure:
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