Synonyms: L-454,560 [1] | L-454560 | MK0359
Compound class:
Synthetic organic
Comment: MK-0359 is a potent and selective, oral PDE4 inhibitor that has a competitive and reversible mode of interaction. MK-0359 is identified as L-454,560 [1] by citation in [2]. MK-0359 inhibits both the apo- (Mg2+ free) and holoenzyme ((Mg2+-bound) states of PDE4 [1].
Ligand Activity Visualisation ChartsThese 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. ✖ |
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Immunopharmacology Comments |
MK-0359 is a PDE4 inhibitor that is being evaluated for clinical anti-inflammatory efficacy. It blocks LPS-induced TNF-α formation in whole blood assays with a potency similar to that exhibited by roflumilast, and is superior to cilomilast [1]. |
Immunopharmacology Disease | |||
Disease | X-Refs | Comment | References |
Rheumatoid arthritis |
Disease Ontology:
DOID:7148 OMIM: 180300 |
Completed Phase 2 clinical evaluation in RA- see NCT00482417 | |
Chronic obstructive pulmonary disease |
Disease Ontology:
DOID:3083 |
Completed Phase 2 clinical evaluation in COPD- see NCT00482235 | |
Asthma |
Disease Ontology:
DOID:2841 OMIM: 600807 |
Completed Phase 2 clinical evaluation in asthma- see NCT00482898 |