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TargetTNF-alpha-Converting Enzyme
LigandBDBM23465
Substrate/CompetitorBDBM23453
Meas. Tech.TACE Inhibition Assay
pH7.3±n/a
Temperature295.15±n/a K
Ki 50±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 Chem 51:725-36 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
TNF-alpha-Converting Enzyme
Name:TNF-alpha-Converting Enzyme
Synonyms:A disintegrin and metalloproteinase domain 17 | ADAM 17 | CD156b antigen | Snake venom-like protease
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:
BDBM23465
BDBM23453
NameBDBM23465
Synonyms:hydroxamate deriv., 57 | methyl (1R,2R)-1-{3-[(4-chlorophenyl)methoxy]phenyl}-2-(hydroxycarbamoyl)cyclopropane-1-carboxylate
TypeSmall organic molecule
Emp. Form.C19H18ClNO5
Mol. Mass.375.803
SMILESCOC(=O)[C@@]1(C[C@H]1C(=O)NO)c1cccc(OCc2ccc(Cl)cc2)c1 |r|
Structure
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