Fully integrated service

The Target:

The target for this program is a pseudokinase. The client was looking for an antagonist of the receptor.

Compound Design:

Medicinal chemistry design was driven by the client with input from SYNthesis. Scaffolds were chosen to present substituents in similar locations to those of the competitor’s clinical candidate. SYNthesis were responsible for the collection of the SAR data obtained.

Key Achievements:

• Active compounds have been generated in three distinct chemical series.
• Compounds discovered within the program possess activity levels similar to those of the competitor’s clinical candidate and a preclinical candidate was nominated. 
• A few patent applications have been submitted and SYNthesis medicinal chemists are co-authors.
• The client managed to secure an IP license deal worth of $200 million with a big pharma using this research program.

The Chemistry:

Initially SYNthesis managed the sourcing and purchase of a 100 member library form multiple suppliers. These compounds were chosen after optimization using Cresset software. The compounds were screened on the target using a US-based CRO through a relationship that SYNthesis had already established or internally at the client’s facility. 

Information from this initial screen as well as from a patent review in the area was then used to design new compounds. Compounds within this series are heteroalkyl compounds most containing 1 or 2 chiral centres. Synthesized compounds were delivered in 10 mg – 1 g quantities at greater than 95% purity  

SYNthesis maintains the compound library for this program and manages the aliquoting and delivery of compounds to the biology CRO.