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Compound class: Synthetic organic
Comment: JNJ-10311795 is a chymase inhibitor with cathepsin G cross-reactivity. The isomer in CID 656932 is contained in PDB X-ray crystal structures . It is suggested to have potential clinical utility in pulmonary inflammatory diseases such as asthma and COPD.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. de Garavilla L, Greco MN, Sukumar N, Chen ZW, Pineda AO, Mathews FS, Di Cera E, Giardino EC, Wells GI, Haertlein BJ et al.. (2005)
A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.
J Biol Chem, 280 (18): 18001-7. [PMID:15741158]
2. Greco MN, Hawkins MJ, Powell ET, Almond Jr HR, de Garavilla L, Hall J, Minor LK, Wang Y, Corcoran TW, Di Cera E et al.. (2007)
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
J Med Chem, 50 (8): 1727-30. [PMID:17361995]