High affinity retinoic acid receptor antagonists: analogs of AGN 193109.
Article Details
- CitationCopy to clipboard
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]
- 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