5-Functionalized indazoles as glucocorticoid receptor agonists.

Article Details

Citation
Copy to clipboard

Bai M, Carr G, Deorazio RJ, Friedrich TD, Dobritsa S, Fitzpatrick K, Guzzo PR, Kitchen DB, Lynch MA, Peace D, Sajad M, Usyatinsky A, Wolf MA

5-Functionalized indazoles as glucocorticoid receptor agonists.

Bioorg Med Chem Lett. 2010 May 15;20(10):3017-20. doi: 10.1016/j.bmcl.2010.04.012. Epub 2010 Apr 11.

PubMed ID
20427184 [ View in PubMed
]
Abstract

An indazole based series of glucocorticoid receptor agonists is reported. The SAR exploration of this scaffold yielded compounds with nanomolar affinity for the glucocorticoid receptor with indications of selectivity for the preferred transrepression mechanism; in vivo efficacy was observed in the mouse LPS induced TNFalpha model for compound 28.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PrednisoloneGlucocorticoid receptorIC 50 (nM)7N/AN/ADetails
PrednisoloneGlucocorticoid receptorEC 50 (nM)3N/AN/ADetails
PrednisoloneGlucocorticoid receptorEC 50 (nM)55N/AN/ADetails