Reaction Details
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Target
Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q]
Ligand
BDBM23497
Substrate
BDBM23453
Meas. Tech.
TACE Inhibition Assay
Ki
80±n/a nM
Citation
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More Info.:
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:
BDBM23497
Synonyms:
(1R,2S)-1-{[4-(but-2-yn-1-yloxy)phenyl]methyl}-2-N-hydroxycyclopropane-1,2-dicarboxamide | hydroxamate deriv., 88
Type:
Small organic molecule
Emp. Form.:
C16H18N2O4
Mol. Mass.:
302.3251
SMILES:
CC#CCOc1ccc(C[C@@]2(C[C@@H]2C(=O)NO)C(N)=O)cc1 |r|