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Enable Innovative Drug Discover with DEL, FBDD and SBDD

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  2. Case Studies

Case Studies

  • Novel BRD4 Degrader Discovery using DEL Technology
    DEL selection is an affinity-based approach to recognize compounds interacting with the target, including the compounds modulating target function(s) or simply binding to the protein. The architecture of a DNA Encoded Compound is very similar to proteolysis targeting chimeras (PROTAC) as shown in the following figure. Both DEL compound and PROTAC molecule require covalent linkage of two molecules with known attachment points that have minimal impact to the binding.
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  • Identification of Transferase NAA50 Inhibitors by DEL Selection
    The two isomers of the selected compound DEL951-34-888-1668 were synthesized and tested by SPR in the presence of CoA and AcCoA and biochemical assay. The chiral isomer 4a has been found as a very potent inhibitor with improved MW, Ligand Efficiency, and tPSA. The interaction of compound 4a and NAA50 has been further confirmed by co-crystal structure by Pfizer (pdb code: 6WFN).
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  • FBDD Case Studies
    We have pioneered the use of off-rate screening (ORS) to kinetically sample hit-to-lead chemical space, combining our expertise in cheminformatics, compound library synthesis and use of surface plasmon resonance (SPR), to enable screening of unpurified reaction products. This has been applied to the rapid generation of lead compounds from fragment hits without purification of compound libraries or the use of protein structure (Murray, J. B. et al., J. Med. Chem. 2014).
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