Enabling Ear­ly Drug Dis­cov­ery: Inte­grat­ed Screen­ing Capa­bil­i­ties and a BRD4/CRBN PRO­TAC Case Study

Enam­ine is a glob­al provider of inte­grat­ed drug dis­cov­ery solu­tions sup­port­ing ear­ly-stage research through access to com­pound libraries and exper­i­men­tal screen­ing capa­bil­i­ties. Its plat­form enables effi­cient pro­gres­sion of dis­cov­ery projects by inte­grat­ing assay devel­op­ment, high-through­put screen­ing work­flows, and bio­phys­i­cal and cell-based char­ac­ter­i­za­tion methods.

Tar­get­ed pro­tein degra­da­tion has emerged as a pow­er­ful approach in can­cer drug dis­cov­ery, enabling mod­u­la­tion of pre­vi­ous­ly undrug­gable tar­gets through induced pro­tein degra­da­tion mechanisms.

Using a BRD4/CRBN PRO­TAC case study, we will present a step­wise screen­ing approach for iden­ti­fy­ing ini­tial degrad­er can­di­dates. The work­flow includes pri­ma­ry screen­ing, fol­lowed by bio­phys­i­cal char­ac­ter­i­za­tion and cell-based assess­ment of tar­get engage­ment and degra­da­tion effects. Par­tic­u­lar empha­sis will be placed on assay selec­tion strat­e­gy, data triag­ing, and pro­gres­sion cri­te­ria applied dur­ing hit identification.

The exam­ple illus­trates how com­ple­men­tary exper­i­men­tal read­outs are inte­grat­ed to sup­port eval­u­a­tion of ear­ly PRO­TAC can­di­dates and guide pro­gres­sion with­in ear­ly-stage dis­cov­ery programs.