Focused On-demand Library for G-protein coupled receptor 143

Focused On-demand Libraries - Reaxense Collaboration

Explore the Potential with AI-Driven Innovation

Our detailed focused library is generated on demand with advanced virtual screening and parameter assessment technology powered by the Receptor.AI drug discovery platform. This method surpasses traditional approaches, delivering compounds of better quality with enhanced 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 receptors.

Fig. 1. The sreening workflow of Receptor.AI

This includes comprehensive molecular simulations of the receptor in its native membrane environment, paired with ensemble virtual screening that factors in its conformational mobility. In cases involving dimeric or oligomeric receptors, the entire functional complex is modelled, pinpointing potential binding pockets on and between the subunits to capture the full range of mechanisms of action.

Our library is unique due to several crucial aspects:

Receptor.AI compiles all relevant data on the target protein, such as past experimental results, literature findings, known ligands, and structural data, thereby enhancing the likelihood of focusing on the most significant compounds.
By utilizing advanced molecular simulations, the platform is adept at locating potential binding sites, rendering the compounds in the focused library well-suited for unearthing allosteric inhibitors and binders for hidden pockets.
The platform is supported by more than 50 highly specialized AI models, all of which have been rigorously tested and validated in diverse drug discovery and research programs. Its design emphasizes efficiency, reliability, and accuracy, crucial for producing focused libraries.
Receptor.AI extends beyond just creating focused libraries; it offers a complete spectrum of services and solutions during the preclinical drug discovery phase, with a success-dependent pricing strategy that reduces risk and fosters shared success in the project.

partner

Reaxense

upacc

P51810

UPID:

GP143_HUMAN

Alternative names:

Ocular albinism type 1 protein

Alternative UPACC:

P51810; Q6NTI7

Background:

G-protein coupled receptor 143 (GPR143) plays a pivotal role in melanosome biogenesis, organization, and transport within melanocytic cells. It functions as a receptor for tyrosine, L-DOPA, and dopamine, facilitating crucial signaling pathways involved in cellular responses. The receptor's activity, mediated by G proteins, activates the phosphoinositide signaling pathway, highlighting its integral role in cellular communication and response mechanisms.

Therapeutic significance:

GPR143 is directly associated with Albinism ocular 1 and Nystagmus 6, congenital, X-linked, diseases characterized by visual impairments. Understanding the role of GPR143 could open doors to potential therapeutic strategies aimed at mitigating the symptoms of these ocular conditions, offering hope for improved quality of life for affected individuals.