OpenSourceMalaria:Story so far: Difference between revisions

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===Summary===

The first series to be tried was based on an [http://openwetware.org/wiki/OpenSourceMalaria:GSK_Arylpyrrole_Series arylpyrrole] that was one of the most attractive hits in the [https://www.ebi.ac.uk/chemblntd/#tcams_dataset original GSK dataset]. Ultimately this series was parked because the ester, which was metabolically unstable, could not be replaced with another functional group. A related set of compounds, the "Near Neighbours" displayed high potency but were found to be too insoluble. Series 2, the triazoloureas, appeared promising but there was a suggestion another team were working on this series, so it was parked. Series 3, the aminothienopyrimidines, are under current investigation, though the analogs examined to date have been inactive and also suffer from low solubility.

The first series to be tried was based on an [http://openwetware.org/wiki/OpenSourceMalaria:GSK_Arylpyrrole_Series arylpyrrole] that was one of the most attractive hits in the [https://www.ebi.ac.uk/chemblntd/#tcams_dataset original GSK dataset]. Ultimately this series was parked because the ester, which was metabolically unstable, could not be replaced with another functional group. A related set of compounds, the "Near Neighbours" displayed high potency but were found to be too insoluble. Series 2, the triazoloureas, appeared promising but there was a suggestion another team were working on this series, so it was parked. Series 3, the aminothienopyrimidines, are under current investigation, though the analogs examined to date have been inactive and also suffer from low solubility. It is likely that the project will shortly (end 2013) move to [[OpenSourceMalaria:Triazolopyrazine (TP) Series| Series 4]].

Compounds evaluated to date (assigned OSM codes): [http://malaria.ourexperiment.org/osm_procedures/group/Compound%20List picture list], [https://github.com/OpenSourceMalaria/OSM_compounds .sdf], [http://bit.ly/OSDDcompounds old spreadsheet]

@@ Line 21: / Line 21: @@
 ===Summary===
-The first series to be tried was based on an [http://openwetware.org/wiki/OpenSourceMalaria:GSK_Arylpyrrole_Series arylpyrrole] that was one of the most attractive hits in the [https://www.ebi.ac.uk/chemblntd/#tcams_dataset original GSK dataset]. Ultimately this series was parked because the ester, which was metabolically unstable, could not be replaced with another functional group. A related set of compounds, the "Near Neighbours" displayed high potency but were found to be too insoluble. Series 2, the triazoloureas, appeared promising but there was a suggestion another team were working on this series, so it was parked. Series 3, the aminothienopyrimidines, are under current investigation, though the analogs examined to date have been inactive and also suffer from low solubility.
+The first series to be tried was based on an [http://openwetware.org/wiki/OpenSourceMalaria:GSK_Arylpyrrole_Series arylpyrrole] that was one of the most attractive hits in the [https://www.ebi.ac.uk/chemblntd/#tcams_dataset original GSK dataset]. Ultimately this series was parked because the ester, which was metabolically unstable, could not be replaced with another functional group. A related set of compounds, the "Near Neighbours" displayed high potency but were found to be too insoluble. Series 2, the triazoloureas, appeared promising but there was a suggestion another team were working on this series, so it was parked. Series 3, the aminothienopyrimidines, are under current investigation, though the analogs examined to date have been inactive and also suffer from low solubility. It is likely that the project will shortly (end 2013) move to [[OpenSourceMalaria:Triazolopyrazine (TP) Series| Series 4]].
 Compounds evaluated to date (assigned OSM codes): [http://malaria.ourexperiment.org/osm_procedures/group/Compound%20List picture list], [https://github.com/OpenSourceMalaria/OSM_compounds .sdf], [http://bit.ly/OSDDcompounds old spreadsheet]