PT2385
Antagonist of EPAS1
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
There are multiple lines of convincing evidence to support meaningful HIF2α modulation by PT-2385 in cell-free, cellular, and in vivo assays. This includes nanomolar cell-free target inhibition, x-ray crystal structures, ITC, convincing SAR, and activity consistent with HIF2α engagement in multiple cellular and in vivo assays. I recommend including an inactive control analog in cellular assays, and in vivo assays if possible.
(last updated: 20 May 2021 )
SERP Ratings
(last updated: 4 Jun 2021 )
SERP Ratings
SERP Comments:
This is a promising HiF-2a antagonist with a high affinity to target, high cell potency, expected cellular effects (in vitro and in vivo), good in vivo PK and toxicology profiles, and very good selectivity properties.
(last updated: 4 Jun 2021 )