Use of libraries to access new chemical space: applications to CRTH2.

The generation of novel CRTH2 ligands in heavily congested chemical space, by de novo design of libraries is disclosed. Novel (1719) compounds across seven libraries were synthesised. More than 100 of these compounds showed binding potency <3μM against CRTH2, with the most potent being 247nM. These libraries produced novel series and demonstrated that this approach is a viable one.