Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.

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Roach SL, Higuchi RI, Hudson AR, Vassar A, Grant VH, Lamer R, Hooper C, Rungta D, Syka PM, Mais DE, Marschke KB, Zhi L

Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1658-62. doi: 10.1016/j.bmcl.2011.01.106. Epub 2011 Jan 27.

PubMed ID
21349714 [ View in PubMed
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Abstract

Continuing studies on tetrahydroquinoline glucocorticoid receptor anti-inflammatory agents lead to the identification of several tetrahydroquinolin-3-yl carbamates that exhibited steroid-like activity in in vitro transrepression assays with reduced transactivation of phosphoenol pyruvate carboxykinase (PEPCK), a key enzyme in the gluconeogenesis pathway.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PrednisoloneGlucocorticoid receptorEC 50 (nM)5.3N/AN/ADetails
PrednisoloneGlucocorticoid receptorKi (nM)5.3N/AN/ADetails
PrednisoloneGlucocorticoid receptorIC 50 (nM)4.1N/AN/ADetails
PrednisoloneGlucocorticoid receptorIC 50 (nM)23N/AN/ADetails
PrednisoloneGlucocorticoid receptorEC 50 (nM)26N/AN/ADetails