Description

Hit-to-Lead - CRT Discoveries Laboratories Project

A hit-to-lead stage programme is ongoing to discover small molecule inhibitors of PAK4. This kinase is involved in invasion and migration, anchorage independent growth, cell survival under stress, and signalling via cMet in a range of tumour types including prostate, pancreatic and colorectal. Two chemical series of drug-like patentable small molecules with low nM biochemical IC50s and in vitro PD biomarker modulation are being investigated, with examples from one series showing selectivity for Group II over Group I PAKs. Medicinal chemistry is driven by the early input of structural biology, with a number of key compounds co-crystallised with the protein at high resolution. This programme also benefits from the expertise of academic collaborators in the field.

For more information please contact

Dr Anne Horgan

+44 (0) 20 3469 6300 .(JavaScript must be enabled to view this email address)