Novel lead for potent inhibitors of breast cancer resistance protein (BCRP).

Article Details

Citation

Pick A, Muller H, Wiese M

Novel lead for potent inhibitors of breast cancer resistance protein (BCRP).

Bioorg Med Chem Lett. 2010 Jan 1;20(1):180-3. doi: 10.1016/j.bmcl.2009.11.004. Epub 2009 Nov 10.

PubMed ID
19932960 [ View in PubMed
]
Abstract

From our modulator library an interesting inhibitor of breast cancer resistance protein (BCRP) was identified. Due to its high inhibitory potency, this compound may serve as a promising novel lead for the design of new and potent modulators. This adds a new structural class to the few known highly active BCRP inhibitors.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ElacridarATP-binding cassette sub-family G member 2IC 50 (nM)430N/AN/ADetails
ElacridarATP-binding cassette sub-family G member 2IC 50 (nM)400N/AN/ADetails
GefitinibATP-binding cassette sub-family G member 2IC 50 (nM)1260N/AN/ADetails
GefitinibATP-binding cassette sub-family G member 2IC 50 (nM)1100N/AN/ADetails
ImatinibATP-binding cassette sub-family G member 2IC 50 (nM)3380N/AN/ADetails
ImatinibATP-binding cassette sub-family G member 2IC 50 (nM)4070N/AN/ADetails