Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.

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Marshall DR, Rodriguez G, Thomson DS, Nelson R, Capolina A

Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):315-9. Epub 2006 Oct 25.

PubMed ID
17118655 [ View in PubMed
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Abstract

Alpha-methyltryptamine sulfonamides were identified as human glucocorticoid receptor (hGR) ligands in an ultra high throughput screening (UHTS) campaign. Described will be the hit-to-lead activities, including parallel and single point analog synthesis to map the scaffold. Ligands were identified that exhibited 30 nM binding to hGR. The SAR and selectivity of these compounds will be discussed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DexamethasoneGlucocorticoid receptorIC 50 (nM)3.4N/AN/ADetails