Reaction Details |
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Target | Disintegrin and metalloproteinase domain-containing protein 17 |
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Ligand | BDBM26806 |
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Substrate/Competitor | TACE substrate peptide |
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Meas. Tech. | Enzyme Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 298.15±n/a K |
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IC50 | 1.4±n/a nM |
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Comments | MMP-1,-2,-9 Ki (nM) >4948, >3333, >2128. |
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Citation | Ott, GR; Asakawa, N; Lu, Z; Anand, R; Liu, RQ; Covington, MB; Vaddi, K; Qian, M; Newton, RC; Christ, DD; Trzaskos, JM; Duan, JJ Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents. Bioorg Med Chem Lett18:1577-82 (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 |
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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: | MLREQFSFDIAEEASKVCLAHLFTYQDFDMGTLGLAYVGSPRANSHGGVCPKAYYSPIGK
KNIYLNSGLTSTKNYGKTILTKEADLVTTHELGHNFGAEHDPDGLAECAPNE
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BDBM26806 |
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TACE substrate peptide |
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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: | MCA-Pro-Leu-Ala-Gln-Ala-Val-Dpa-Arg-Ser-Ser-Ser-Arg-NH2
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