Explore the Potential with AI-Driven Innovation
This extensive focused library is tailor-made using the latest virtual screening and parameter assessment technology, operated by the Receptor.AI drug discovery platform. This technique is more effective than traditional methods, offering compounds with improved activity, selectivity, and safety.
The compounds are cherry-picked from the vast virtual chemical space of over 60B molecules. The synthesis and delivery of compounds is facilitated by our partner Reaxense.
The library includes a list of the most promising modulators annotated with 38 ADME-Tox and 32 physicochemical and drug-likeness parameters. Also, each compound is presented with its optimal docking poses, affinity scores, and activity scores, providing a comprehensive overview.
We employ our advanced, specialised process to create targeted libraries for enzymes.
Fig. 1. The sreening workflow of Receptor.AI
The method includes detailed molecular simulations of the catalytic and allosteric binding pockets, along with ensemble virtual screening that considers their conformational flexibility. In the design of modulators, structural changes induced by reaction intermediates are taken into account to enhance activity and selectivity.
Our library is unique due to several crucial aspects:
partner
Reaxense
upacc
P16234
UPID:
PGFRA_HUMAN
Alternative names:
Alpha platelet-derived growth factor receptor; Alpha-type platelet-derived growth factor receptor; CD140 antigen-like family member A; CD140a antigen; Platelet-derived growth factor alpha receptor; Platelet-derived growth factor receptor 2
Alternative UPACC:
P16234; B2RE69; E9PBH0; Q6P4H5; Q96KZ7; Q9UD28
Background:
The Platelet-derived growth factor receptor alpha (PDGFRA) is a tyrosine-protein kinase playing a pivotal role in various cellular processes such as embryonic development, cell proliferation, survival, and chemotaxis. It acts as a cell-surface receptor for PDGFA, PDGFB, and PDGFC, influencing bone marrow-derived mesenchymal stem cells differentiation, skeleton development, and gastrointestinal tract mucosa lining development.
Therapeutic significance:
PDGFRA's mutations and constitutive activation are linked to Gastrointestinal stromal tumor (GIST) and GIST-plus syndrome, highlighting its critical role in disease pathogenesis. Understanding the role of PDGFRA could open doors to potential therapeutic strategies targeting these mutations to manage or treat GISTs.