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Synonyms: compound 183 [WO2007138072A2]
Compound class: Synthetic organic
Comment: This compound was developed by Galapagos as a MAPKAPK5 inhibitor, in the search for a novel anti-inflammatory mechanism that would be applicable to the treatment of rheumatoid arthritis (RA). The discovery pathway is detailed in the pdf entitled 'Discovery of inhibitors of MAPKAPK5, a novel target for rheumatoid arthritis', which is available online here. The chemical structure is claimed in Galapagos patent WO2007138072A2, as compound 183 . This compound (compound D) is likely to be a relation of the Galapagos clinical candidate GLPG0259, which failed in Phase 2 clinical trial in patients with methotrexate-refractory RA .
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. Andrews M.
Discovery of inhibitors of MAPKAPK5, a novel target for rheumatoid arthritis.
Accessed on 15/03/2018. Modified on 15/03/2018. www.rsc.org, https://www.google.co.uk/url?sa=t&rct=j&q=&esrc=s&source=web&cd=7&cad=rja&uact=8&ved=0ahUKEwiEjPvHy-7ZAhUGKewKHf2vBYAQFghJMAY&url=http%3A%2F%2Fwww.rsc.org%2Fimages%2FMartinAndrews_tcm18-195242.pdf&usg=AOvVaw38oSSfFTUgOzaYq791YK8Q
2. Andrews MJI, Edwards P, Chambers MS, Schmidt W, Clase JA, Bar G, Hirst KL, Macleod A. (2007)
Triazolopyrazine compounds useful for the treatment of degenerative & inflammatory diseases.
Patent number: WO2007138072A2. Assignee: Galapagos N.V.. Priority date: 31/05/2006. Publication date: 06/12/2007.
3. Westhovens R, Keyser FD, Rekalov D, Nasonov EL, Beetens J, Van der Aa A, Wigerinck P, Namour F, Vanhoutte F, Durez P. (2013)
Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: a phase II, randomised, double-blind, placebo-controlled, multicentre trial.
Ann. Rheum. Dis., 72 (5): 741-4. [PMID:23161899]