Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Article Details
- CitationCopy to clipboard
Biggadike K, Caivano M, Clackers M, Coe DM, Hardy GW, Humphreys D, Jones HT, House D, Miles-Williams A, Skone PA, Uings I, Weller V, McLay IM, Macdonald SJ
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4846-50. doi: 10.1016/j.bmcl.2009.06.020. Epub 2009 Jun 13.
- PubMed ID
- 19592247 [ View in PubMed]
- Abstract
Starting from a non-steroidal glucocorticoid agonist aryl pyrazole derivative, the NFkappaB agonist activity was optimised in an iterative process from pIC(50) 7.5 (for 7), to pIC(50) 10.1 (for 38E1). An explanation for the SAR observed based is presented along with a proposed docking of 38E1 into the active site of the glucocorticoid receptor.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Dexamethasone Glucocorticoid receptor IC 50 (nM) 1 N/A N/A Details Fluticasone furoate Glucocorticoid receptor IC 50 (nM) 0.0398 N/A N/A Details