2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.

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Henke BR, Drewry DH, Jones SA, Stewart EL, Weaver SL, Wiethe RW

2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1939-42.

PubMed ID

11459665 [ View in PubMed

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Abstract

We have prepared a novel series of 2-amino-4,6-diarylpyridines that function as ligands of estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). These compounds bind to both ERalpha and ERbeta with a modest selectivity for the alpha subtype. The most potent of these analogues, compound 19, has a K(i)=20nM at ERalpha. These molecules represent a novel template for designing potentially useful ligands for the estrogen receptor.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor alpha	Ki (nM)	2.2	N/A	N/A	Details
Estradiol	Estrogen receptor beta	Ki (nM)	3.5	N/A	N/A	Details
Raloxifene	Estrogen receptor alpha	Ki (nM)	0.22	N/A	N/A	Details
Raloxifene	Estrogen receptor beta	Ki (nM)	10	N/A	N/A	Details