High affinity retinoic acid receptor antagonists: analogs of AGN 193109.

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Johnson AT, Wang L, Gillett SJ, Chandraratna RA

High affinity retinoic acid receptor antagonists: analogs of AGN 193109.

Bioorg Med Chem Lett. 1999 Feb 22;9(4):573-6.

PubMed ID

10098666 [ View in PubMed

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Abstract

A series of high affinity retinoic acid receptor (RAR) antagonists were prepared based upon the known antagonist AGN 193109 (2). Introduction of various phenyl groups revealed a preference for substitution at the para-position relative to the meta-site. Antagonists with the highest affinities for the RARs possessed hydrophobic groups, however, the presence of polar functionality was also well tolerated.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tretinoin	Retinoic acid receptor alpha	Kd (nM)	15	N/A	N/A	Details
Tretinoin	Retinoic acid receptor beta	Kd (nM)	13	N/A	N/A	Details
Tretinoin	Retinoic acid receptor gamma	Kd (nM)	18	N/A	N/A	Details