Welcome to HitGen
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HitGen Inc.

HitGen has established a drug discovery research platform for small molecules and nucleic acid drugs centered on the design, synthesis and screening of DNA encoded chemical libraries (DELs), fragment-based drug discovery (FBDD) and structure-based drug design (SBDD) technologies.

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HitGen Inc. (SSE: 688222.SH), is a drug discovery research company with headquarters in Chengdu, China, and subsidiaries in Cambridge, UK and Houston, USA. HitGen has established leading technology platforms to enable the discovery and optimization of small molecules and nucleic acid drugs. Our key technology platforms include world-leading DNA-encoded library technology (DEL), fragment-based drug discovery and structure-based drug design technologies (FBDD/SBDD), as well as the emerging technology platforms for synthetic therapeutic oligonucleotide technology (STO), and targeted protein degradation technology (TPD). Through our diverse and flexible business models, we have built up collaboration partnership with several hundred biopharmaceutical research organizations worldwide. HitGen has multiple programmes from early discovery to clinical trial stage.


For more information, please call +86-28-85197385, +1-508-840-9646 or visit www.hitgen.com.

For media inquiries: media@hitgen.com

For investor inquiries: investors@hitgen.com  

For business development: bd@hitgen.com  


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History and Honor

  • 2023
  • 2022
  • 2021
  • 2020
  • 2019
  • 2018
  • 2017
  • 2016
  • 2015
  • 2014
  • 2013
  • 2012

Publications

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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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