Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Article Details
- CitationCopy to clipboard
Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Bioorg Med Chem Lett. 2005 Apr 15;15(8):2163-7.
- PubMed ID
- 15808489 [ View in PubMed]
- Abstract
A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Prednisolone Glucocorticoid receptor IC 50 (nM) 13.8 N/A N/A Details Prednisolone Glucocorticoid receptor EC 50 (nM) 4.5 N/A N/A Details Prednisolone Glucocorticoid receptor EC 50 (nM) 24 N/A N/A Details