Reaction Details
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Disintegrin and metalloproteinase domain-containing protein 17
Ligand
BDBM26572
Substrate
TACE substrate peptide
Meas. Tech.
Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
2±n/a nM
Citation
Lu, Z; Ott, GR; Anand, R; Liu, RQ; Covington, MB; Vaddi, K; Qian, M; Newton, RC; Christ, DD; Trzaskos, J; Duan, JJ Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents. Bioorg Med Chem Lett 18:1958-62 (2008) [PubMed] Article Target
Name:
Disintegrin and metalloproteinase domain-containing protein 17
Synonyms:
A disintegrin and metalloproteinase domain 17 | ADA17_PIG | ADAM 17 | ADAM17 | Snake venom-like protease | TACE | TNF-alpha-Converting Enzyme
Type:
Metalloprotease
Mol. Mass.:
12197.99
Organism:
Sus scrofa (pig)
Description:
Partially purified TACE was obtained from porcine spleen.
Residue:
112
Sequence:
MLREQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPIGKKNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGLAECAPNE
Inhibitor
Name:
BDBM26572
Synonyms:
(3R,4R)-4-N-[4-({2-ethylpyrazolo[1,5-a]pyridin-3-yl}methyl)benzene]-3-N-hydroxyoxane-3,4-dicarboxamide | pyrazolopyridine, 46
Type:
Small organic molecule
Emp. Form.:
C23H26N4O4
Mol. Mass.:
422.4769
SMILES:
CCc1nn2ccccc2c1Cc1ccc(cc1)C(=O)N[C@@H]1CCOC[C@@H]1C(=O)NO |r|
Structure:
Substrate
Name:
TACE substrate peptide
Synonyms:
n/a
Type:
Internally quenched peptide
Mol. Mass.:
4119.10
Organism:
n/a
Description:
MCA, (7-methoxycoumarin-4-yl)acetyl. Dpa, N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl.
Residue:
39
Sequence:
MCAPRLEALAGLNALAVALDPAARGSERSERSERARGNH