I read following reviews…

Many pharmaceutical industry is facing low productivity of NME.
It is need to focus on right target for drug discovery to improve the productivity.
I think this review is nicely ordered in recent drug discovery process.
There are some example about target engagement.

Pfizer, many of drug discovery project dropped because of ‘lack of efficacy’.
They suggested ‘three pillars’ for evaluate drug-targets.
(1)sufficient exposure of ligands at the site of action; (2) proof of target engagement; (3) expression of functional pharmacological activity.
AstraZeneca also identified “five R’s”.
Right target, Right patient, Right tissue, Right safety and Right commercial potential.

Many approaches described in this review.

And I’m interested in CETSA also interested in Celgene’s BTK inh. approach.
That approach stands for cellar thermal shift assay.
If ligand bind to target, it shifts thermal stability. Fig 16 shows concept.
SPR is also measure ligand binding but we often get false positive, non specific binder.
CETSA seems to measure ligand binding directory using cells.
I’ll check papers later….

I think, to overcome low productivity of NME, I have to do my best not only as a medchem but also teammate.
Don’t be silos.


Published by iwatobipen

I'm medicinal chemist in mid size of pharmaceutical company. I love chemoinfo, cording, organic synthesis, my family.

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