| Reaction Details |
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 | Report a problem with these data |
| Target | Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q] |
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| Ligand | BDBM23487 |
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| Substrate/Competitor | BDBM23453 |
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| Meas. Tech. | TACE Inhibition Assay |
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| Ki | 3±n/a nM |
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| Citation |  Zhu, Z; Mazzola, R; Sinning, L; McKittrick, B; Niu, X; Lundell, D; Sun, J; Orth, P; Guo, Z; Madison, V; Ingram, R; Beyer, 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 |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q] |
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| Name: | Disintegrin and metalloproteinase domain-containing protein 17 [215-477,S266A,N452Q] |
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| Synonyms: | A disintegrin and metalloproteinase domain 17 | ADA17_HUMAN | ADAM 17 | ADAM17 | CD156b antigen | CSVP | Snake venom-like protease | TACE | TNF-alpha-Converting Enzyme |
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| Type: | Single-pass type I membrane protein; metalloprotease |
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| Mol. Mass.: | 29695.98 |
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| Organism: | Homo sapiens (Human) |
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| 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. |
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| Residue: | 263 |
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| Sequence: | RADPDPMKNTCKLLVVADHRFYRYMGRGEESTTTNYLIELIDRVDDIYRNTAWDNAGFKG
YGIQIEQIRILKSPQEVKPGEKHYNMAKSYPNEEKDAWDVKMLLEQFSFDIAEEASKVCL
AHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPVGKKNIYLNSGLTSTKNYGKTI
LTKEADLVTTHELGHNFGAEHDPDGLAECAPNEDQGGKYVMYPIAVSGDHENNKMFSQCS
KQSIYKTIESKAQECFQERSNKV
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| BDBM23487 |
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| BDBM23453 |
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| Name | BDBM23487 |
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| Synonyms: | (1S,2R)-1-N-hydroxy-2-({4-[(2-methylquinolin-4-yl)methoxy]phenyl}methyl)cyclopropane-1,2-dicarboxamide | BMCL1954 Compound 3 | hydroxamate deriv., 78 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H23N3O4 |
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| Mol. Mass. | 405.4464 |
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| SMILES | Cc1cc(COc2ccc(C[C@@]3(C[C@@H]3C(=O)NO)C(N)=O)cc2)c2ccccc2n1 |r| |
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| Structure | 
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