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5-hydroxy-2-(4-hydroxyphenyl)-1-benzofuran-7-carbonitrile

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
01

Overview

5-hydroxy-2-(4-hydroxyphenyl)-1-benzofuran-7-carbonitrile is a synthetic small molecule belonging to the class of organic compounds known as 2-arylbenzofuran flavonoids[2]. It has been studied primarily as a potent and selective ligand for estrogen receptors, with high affinity for estrogen receptor beta (ERβ) and moderate affinity for estrogen receptor alpha (ERα)[4]. In binding assays, it demonstrated an IC50 of approximately 46 nM for ERα and an IC50/EC50 in the low nanomolar range (about 2 nM) for ERβ[4]. The compound is not currently approved or marketed as a pharmaceutical drug but has been investigated in preclinical research settings.

Other names
5-hydroxy-2-(4-hydroxyphenyl)-1-benzofuran-7-carbonitrilePubChem CID 656952
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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