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Target
Stromelysin-1
Ligand
BDBM26567
Substrate
MMP Substrate Peptide
Meas. Tech.
Enzyme Inhibition Assay
Ki
766±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
More Info.:
Target
Name:
Stromelysin-1
Synonyms:
MMP-3 | MMP3 | MMP3_HUMAN | Matrix metalloproteinase (2 and 3) | Matrix metalloproteinase 3 | Matrix metalloproteinase-3 | Matrix metalloproteinase-3 (MMP-3) | Matrix metalloproteinase-3 (MMP3) | SL-1 | STMY1 | Stromelysin 1 | Transin-1
Type:
Enzyme
Mol. Mass.:
53973.13
Organism:
Homo sapiens (Human)
Description:
P08254
Residue:
477
Sequence:
MKSLPILLLLCVAVCSAYPLDGAARGEDTSMNLVQKYLENYYDLKKDVKQFVRRKDSGPVVKKIREMQKFLGLEVTGKLDSDTLEVMRKPRCGVPDVGHFRTFPGIPKWRKTHLTYRIVNYTPDLPKDAVDSAVEKALKVWEEVTPLTFSRLYEGEADIMISFAVREHGDFYPFDGPGNVLAHAYAPGPGINGDAHFDDDEQWTKDTTGTNLFLVAAHEIGHSLGLFHSANTEALMYPLYHSLTDLTRFRLSQDDINGIQSLYGPPPDSPETPLVPTEPVPPEPGTPANCDPALSFDAVSTLRGEILIFKDRHFWRKSLRKLEPELHLISSFWPSLPSGVDAAYEVTSKDLVFIFKGNQFWAIRGNEVRAGYPRGIHTLGFPPTVRKIDAAISDKEKNKTYFFVEDKYWRFDEKRNSMEPGFPKQIAEDFPGIDSKIDAVFEEFGFFYFFTGSSQLEFDPNAKKVTHTLKSNSWLNC
Inhibitor
Name:
BDBM26567
Synonyms:
(3R,4R)-3-N-hydroxy-4-N-(4-{[2-(propan-2-yl)-1-benzofuran-3-yl]methyl}benzene)oxane-3,4-dicarboxamide | 2-isopropylbenzofuran, 28
Type:
Small organic molecule
Emp. Form.:
C25H28N2O5
Mol. Mass.:
436.5002
SMILES:
CC(C)c1oc2ccccc2c1Cc1ccc(cc1)C(=O)N[C@@H]1CCOC[C@@H]1C(=O)NO |r|
Substrate
Name:
MMP Substrate Peptide
Synonyms:
n/a
Type:
Fluorogenic Peptide
Mol. Mass.:
2468.31
Organism:
n/a
Description:
MCA, (7-methoxycoumarin-4-yl)acetyl. Dpa, N-3-(2,4-dinitrophenyl)-L-2,3-diaminopropionyl.
Residue:
23
Sequence:
MCAPRLEGLYLEDPAALAARGNH