Explore the Potential with AI-Driven Innovation
This comprehensive focused library is produced on demand with state-of-the-art virtual screening and parameter assessment technology driven by Receptor.AI drug discovery platform. This approach outperforms traditional methods and provides higher-quality compounds with superior 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 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 use our state-of-the-art dedicated workflow for designing focused libraries for ion channels.
Fig. 1. The sreening workflow of Receptor.AI
It includes extensive molecular simulations of the channel in its native membrane environment in open, closed and inactivated forms and the ensemble virtual screening accounting for conformational mobility in each of these states. Tentative binding pockets are considered inside the pore, in the gating region and in the allosteric locations to cover the whole spectrum of possible mechanisms of action.
Our library distinguishes itself through several key aspects:
partner
Reaxense
upacc
Q9UK17
UPID:
KCND3_HUMAN
Alternative names:
Voltage-gated potassium channel subunit Kv4.3
Alternative UPACC:
Q9UK17; O60576; O60577; Q14D71; Q5T0M0; Q9UH85; Q9UH86; Q9UK16
Background:
Potassium voltage-gated channel subfamily D member 3, also known as Kv4.3, plays a crucial role in the electrical signaling in neurons and the heart. It forms the pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels, contributing to the I(To) current in the heart and I(Sa) current in neurons. Its modulation by interactions with other alpha subunits and regulatory subunits fine-tunes channel properties.
Therapeutic significance:
Kv4.3's involvement in Spinocerebellar ataxia 19 and Brugada syndrome 9 highlights its therapeutic significance. Understanding its role in these diseases could lead to targeted treatments for the cerebellar ataxic syndrome with cognitive impairment and the life-threatening tachyarrhythmia, respectively.