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Enable Innovative Drug Discover with DEL, FBDD and SBDD

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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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For more details on how we can advance your innovative drug discovery projects

Sites: HitGen Inc.

Building C2, NO.8, Huigu 1st East Road
Tianfu International Bio-Town,
Shuangliu District, Chengdu City,
Sichuan Province,P.R. China

Tel : +86-28-8519-7385

HitGen Pharmaceuticals Inc.(US Subsidiary)

Tel : +1-(508)-840-9646

Vernalis (R&D) Limited (UK Subsidiary)

Granta Park,Great Abington
Cambridge,CB21 6GB
United Kingdom

Tel : +44(0)1223-895555

Contact: Business Inquiry : bd@hitgen.com; Investor Relations : investors@hitgen.com; Media : media@hitgen.com; Career and Jobs : human.resources@hitgen.com

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