Drug intelligence / Profile preview

EDO-1-119

Development stage
Preclinical
Lead developer
Georgetown University
Modality
Small Molecules
01

Overview

EDO-1-119 is a novel small molecule 4-aminopyrimidine derivative developed as a potential BRCA1-mimetic drug for the treatment of breast cancer. Discovered by researchers at Georgetown University, EDO-1-119 was identified through virtual screening of a computational model of the BRCA1:ER-1 (estrogen receptor 1) protein complex. It acts as an antagonist of Estrogen Receptor alpha (ER-α), mimicking the tumor suppressor activity of BRCA1 by inhibiting estrogen-stimulated ER-α transcriptional activity and cell proliferation. In vitro assays demonstrate that EDO-1-119 is a potent inhibitor of ER-α activity with an IC50 of 1.3 µM, representing a significant improvement in potency compared to its parent compound A9.

Other names
EDO 1-119EDO1-119EDO-1-119
02

Targets

ESR1 (ERα)

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