Reaction Details
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Target
Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Ligand
BDBM23470
Substrate
BDBM23453
Meas. Tech.
TACE Inhibition Assay
pH
7.3±n/a
Temperature
295.15±n/a K
Ki
50±n/a nM
Citation
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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:
BDBM23470
Synonyms:
hydroxamate deriv., 62 | methyl (1R,2R)-1-[3-(2-{3-[(1Z)-buta-1,3-dien-1-yl]phenyl}ethoxy)phenyl]-2-(hydroxycarbamoyl)cyclopropane-1-carboxylate
Type:
Small organic molecule
Emp. Form.:
C24H25NO5
Mol. Mass.:
407.459
SMILES:
COC(=O)[C@@]1(C[C@H]1C(=O)NO)c1cccc(OCCc2cccc(\C=C/C=C)c2)c1 |r|