The Hit-to-lead phase is to filter several hit compounds that would condense into 2 or 3 Hit series that have the best potential to lead candidates. Once a hit series is confirmed to demonstrate acceptable SAR understanding, engagement of the hit molecule with the biological target can be confirmed. Hit series with true target engagement are then advanced down the screening cascade in the program. In addition, evaluation of in-vitro ADMET properties is important to determine suitable leads per the predefined criteria. Hit-to-lead projects typically run for 6 – 9 months. Rigorous early assessment of the available hits has a major impact on the time required for lead identification.
Aragen IDD has a track record of delivering lead series that can be quickly optimised to robust candidate drugs. IDD teams typically work on setting the cut-offs on the following parameters for the successful candidate to be declared a lead :
Aragen IDD has the requisite infrastructure and resources to conduct efficient and effective hit-to-lead studies and advance a good lead to be optimized further.
