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.
Our selection of compounds is from a large virtual library of over 60 billion molecules. The production and distribution of these compounds are managed by our partner Reaxense.
The library features a range of promising modulators, each detailed with 38 ADME-Tox and 32 physicochemical and drug-likeness parameters. Plus, each compound is presented with its ideal docking poses, affinity scores, and activity scores, ensuring a thorough insight.
We utilise our cutting-edge, exclusive workflow to develop focused libraries for enzymes.
Fig. 1. The sreening workflow of Receptor.AI
It includes in-depth molecular simulations of both the catalytic and allosteric binding pockets, with ensemble virtual screening focusing on their conformational flexibility. For modulators, the process includes considering the structural shifts due to reaction intermediates to boost activity and selectivity.
Our library is unique due to several crucial aspects:
partner
Reaxense
upacc
P25098
UPID:
ARBK1_HUMAN
Alternative names:
G-protein coupled receptor kinase 2
Alternative UPACC:
P25098; B0ZBE1; Q13837; Q6GTT3
Background:
Beta-adrenergic receptor kinase 1, also known as G-protein coupled receptor kinase 2, plays a pivotal role in the regulation of beta-adrenergic and related receptors. By specifically phosphorylating the agonist-occupied form of these receptors, it induces desensitization, thereby modulating receptor sensitivity. This kinase is a key regulator of LPAR1 signaling, influencing receptor signaling through competition with RALA for LPAR1 binding. It also facilitates the Hedgehog signaling pathway by aiding the trafficking and activation of smoothened (SMO) in the cilium.
Therapeutic significance:
Understanding the role of Beta-adrenergic receptor kinase 1 could open doors to potential therapeutic strategies. Its involvement in critical signaling pathways and receptor regulation highlights its potential as a target for therapeutic intervention in diseases where these pathways are dysregulated.