Tag Archive: BIA 10-2474

Apr
20

Final report of CSST on BIA 10-2474 tragedy

I took the report released yesterday by ANSM on BIA 10-2474 and Google translated the whole doc.. Its not perfect but here goes. All the usual caveats apply – that its far from a perfect job but should provide the key points. Would be great to get an official translation at some point. I find …

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Apr
19

Another tragedy – BIA 10-2474 – yes its toxic after 600hrs of committee deliberations

Wow what an anticlimax.. Months after the tragic death in January of a clinical trial volunteer, the medical experts (CSST) in France have declared BIA 10-2474, the experimental drug administered was the problem. It has to to be read to be believed. I bet you could have picked anyone off the street and presented with …

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Apr
13

BIA 10-2474 saga continues – who knew what and when – and nobody comes out a winner

Apologies, recovering from some bug and my head is a bit fuzzier than usual so I hope this all makes sense. A day that started surreal and just kept going. Straight out of the gate this morning I had an email from a journalist Damien Mascret from Le Figaro. I had never been in contact …

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Jan
21

Lets do it all again updating predictions for the ‘real’ BIA 10-2474

After todays unmasking of the ‘real’ BIA 10-2474 I ran it through some of the online tools used earlier and now I have found software issues – that darn pyridine 1 -oxide is not liked by some of the websites probably because they use the same SMILES to structure software plugin? SwissTarget Prediction identifies FAAH1 …

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Jan
21

is the structure of BIA 10-2474 actually BIA 10-2474

Well the protocol released by Bial for the clinical trial lists a molecule 3-(1-(cyclohexyl(methyl)carbamoyl)-1H-imidazol-4-yl)pyridine 1-oxide that when run through online software to convert it looks nothing like the one used previously and posted on wikipedia etc. I used 2 websites to convert name to structure Opsin and Openmolecules.org This looks like a puzzle that could …

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Jan
21

Differences between similar FAAH inhibitors and their in silico target predictions

**UPDATE As of 21st Jan 2016 please note the actual structure of BIA 10-2474 changed to this. The continuing follow up to the clinical trial disaster. Chris Southan yesterday suggested I try CID 57880883 as the comparator to CID 54576693 (JNJ-42165279).  These have IC50 75 nM vs 350 nM, respectively according to Jannsen’s WO2011139951. Yesterday …

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Jan
20

BIA 10-2474 is not that similar to synthetic cannabinoids and comparison to another FAAH compound

**UPDATE As of 21st Jan 2016 please note the actual structure of BIA 10-2474 changed to this. Lauren commented on an earlier post about synthetic cannabinoid toxicities and stroke potential. I took the structure of BIA 10-2474 and looked at the similarity to  a virtual library of synthetic cannabinoids which Matthew Krasowski and I had …

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Jan
20

Where will BIA 10-2474 lead us?

**UPDATE As of 21st Jan 2016 please note the actual structure of BIA 10-2474 changed to this. My “Armchair science” / speculative contributions on this blog for the clinical trial disaster with BIA 10-2474 got a bit of notice over the past few days at Forbes and C&E News. There have also been discussions with …

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Jan
19

Using more online software to make predictions for BIA 10-2474

**UPDATE As of 21st Jan 2016 please note the actual structure of BIA 10-2474 changed to this.   To continue the theme of the last few posts on the BIA 10-2474 compound in which I have used over 2000 Bayesian models and an App as well as another groups target prediction tool. To take this …

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Jan
18

BIA 10-2474 – more predictions

**UPDATE As of 21st Jan 2016 please note the actual structure of BIA 10-2474 changed to this.   I thought it perhaps worth trying other computational approaches with BIA 10-2474. First up is the similarity ensemble analysis (SEA)  from the Shoichet lab. This also makes use of ChEMBL (version 16 data). This seems to agree …

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