DNA Encoded Chemical Library at HitGen: Principle, Practice and Application #Chemspace #HitGen #DEL

Chemspace & HitGen held the Webinar 'DNA-Encoded Chemical Library at HitGen: Principle, Practice and Application', which took place on 15th of October, 2020.

DNA-encoded chemical library (DECL) is an innovative drug discovery technology rapidly gaining widespread interest in the pharmaceutical industry in recent years. It combines the power of molecular biology, combinatorial chemistry, high-throughput screening, and advanced informatics to create vast number of novel molecules for hit identification and lead generation. As one of the major leading companies in this area, HitGen has established an industry-leading platform for early-stage drug discovery research centered on DECLs.

This webinar covers the principle, practice and application of DNA-encoded library technology with proven successes in the selection of various target classes. The webinar finally concludes with the presentation of HitGen’s commercially available off-the-shelf DNA-encoded chemical library for self-service screening.

#Chemspace #HitGen #DEL

0:00 General info about webinar rules
0:59 Chemspace introduction by CEO Yurii Moroz.
4:28 Speaker’s introduction: Dr. Guansai Liu, Senior Director of Chemistry of HitGen.
6:11 Here we go!
6:57 Disclaimer
7:17 Outline of the presentation:
8:44 Budget on R&D and the cost to launch drugs
10:02 Opportunities from human Genome
11:24 Chemical Space
12:25 Major approaches to small molecule Drug Discovery
13:23 Invention and advance of DNA-encoded library
14:44 DNA-encoded library technology as a powerful tool
15:44 Basic construct of a DEL compound
17:33 DEL construction via "Split-and-Pool"
19:59 Hit identification process by DEL affinity selection
23:01 Reported active compounds generated from DELs
24:53 DNA-encoded chemical library design strategies at HitGen
28:51 On-DNA chemistry toolbox
30:16 Examples of on-DNA chemistry development
31:42 Examples of introducing key scaffolds into DECLs
33:35 From aqueous reaction systems to pure organic systems
34:29 DEL products at HitGen (more 500 Bn Cmpds)
37:51 Topological shape analysis of HitGen small molecular DEL compounds
38:45 Analysis of molecular shape diversity from exemplified small molecular DELs
39:54 DEL screening statistics at HitGen
41:35 Identification of transferase inhibitors
43:03 Identification of selective ROCK2 inhibitors
44:11 Identification of IL-17A/IL-17R blockers
45:43 Identification of RNA Helicase inhibitors
47:31 Novel GPCR inhibitor discovery
48:12 Identification of protein degraders
49:58 Hit expansion by DELT
51:07 Identification of novel EGFR T790M covalent inhibitors
51:54 HitGen overview
52:37 Development history
53:18 Integrated Drug Discovery Platform at HitGen
53:41 HitGen’s pipelines
53:58 Flexible business model creating value for partners
54:26 Custom DEL products provided by HitGen
55:03 DEL-related Service and Products
55:30 OpenDEL® as off-the-shelf products for self-service screening
58:40 Q&A session