Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.

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van Oeveren A, Pio BA, Tegley CM, Higuchi RI, Wu M, Jones TK, Marschke KB, Negro-Vilar A, Zhi L

Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1523-6. Epub 2007 Jan 13.

PubMed ID
17257838 [ View in PubMed
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Abstract

A series of alkylamino-2-quinolinone compounds (3) was discovered as androgen receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to androgen receptor and potent receptor modulating activities in the cotransfection assays.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
BicalutamideAndrogen receptorKi (nM)1517.437Details
BicalutamideAndrogen receptorIC 50 (nM)1627.437Details
StanoloneAndrogen receptorKi (nM)0.27.437Details
StanoloneAndrogen receptorEC 50 (nM)5.17.437Details