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24 Aug

Deciding Which Commercially Available Analogues to Buy Within the Thienopyrimidine Series

Published by JimCronshaw

Subject 

Request for Help

Analogues of the amino thienopyrimidine lead compound are needed to assess structure-activity relationship's (SAR's) of the compound. To acheive this, both novel synthetic compounds and commercially available compounds must be obtained and submitted for biological screening. The novel synthetic compounds are being synthesised in the Todd lab at the University of Sydney. The commercially available compounds were identified by performing a similarity search on eMolecules using a similarity (Tanimoto) co-efficient of 0.55.

31 Jul

Pharmacokinetics

Published by pylioja

Subject 

Results

Previously, we found that we had no efficacy for the compounds tested in our  in vivo plasmodium berghei study. Until now we haven't had our pharmacokinetic to figure out why this was. We had previously found that OSM-S-5 (PMY 10-6/TCMDC-123812) is rapidly metabolised in mouse plasma, but that it is stable in human plasma.

Consultation Outcome

Published by pylioja on 26 July 2012 - 6:59am

Subject 

Results

Firstly, thanks for coming to the online meeting. I found it worked quite well (minor glitches aside) but it would be great to hear your thoughts. We'll post the recording up in the near-ish future. The OpenWetWare wiki will soon be updated to reflect the outcomes of the meeting, along with SMILES. Of course if anyone is keen and beats me to it, then even better.

24 Jul

A quick compound update

Published by pylioja

Subject 

Results

Tomorrow we will be having an open chat with anyone who wants to pitch in about which compounds we should be making for the next round of testing. We've been talking about this for a while (phase 1, phase 2) and this the final call before we split some of the compounds into seperate jobs that teams can take on. In the mean time, I've made a few of the compounds we mentioned and I'm most of the way to a couple of others.

15 Jul

Shop Till You Hit - Part II, no Giveaways after all ?

Published by cdsouthan

Subject 

External News

This is a follow up to the post from May  
http://www.thesynapticleap.org/node/404
Unfortunately the vendors survery conducted on behalf of OSDD malaria, despite some helpfull publicity, came up with only two replies.
I have expounded on the possible reasons for failiure in this blog post
http://cdsouthan.blogspot.se/2012/07/shop-till-you-hit-part-ii.html

13 Jul

New ChEMBL malaria data access service

Published by cdsouthan

Subject 

External News

These announcments today refer to a new acess service for data on malaria-related compounds, assays and targets. This involves ChEMBL MMV and EBI.   Sounds good and I will take a look in due course
http://chembl.blogspot.se/2012/07/chembl-delivers-new-malaria-data.html?...
http://www.ebi.ac.uk/Information/News/press-releases/press-release-13072...

Desired Compounds Consultation Phase 2

Published by MatTodd on 28 June 2012 - 1:23pm

Subject 

Request for Help

The evaluation of the arylpyrroles has gone well, in that we've identified promising new antimalarial compounds. Besides their high potency, they exhibit high levels of activity in a late-stage gametocyte assay which is very exciting.

21 Jun

June 2012 update on two potential drug candidates from the Todd group

Published by JimCronshaw

Jim Cronshaw from the Todd group at the University of Sydney here again. It’s been quite some time since I made an update on my research on The Synaptic Leap. This post is intended to give an overview of what problems have been hounding me over the intervening two months.

Desired Compounds Consultation

Published by pylioja on 8 June 2012 - 4:32am

Subject 

Request for Help

We're looking to identify a new set of compounds for the next round of optimisation. This is happening in addition to sourcing of commercially available analogues that will fill a bit more of the SAR space but aren't necessarily exactly what we want.

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