Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

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Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, Zhu Y, Stouch TR, Bassolino-Klimas D, Parker R, Harrity T, Stoffel R, Taylor DS, Lavoie TB, Kish K, Jacobson BL, Sheriff S, Adam LP, Ewing WR, Robl JA

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. Epub 2006 Dec 21.

PubMed ID
17502136 [ View in PubMed
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Abstract

Herein we report the first disclosure of biphenyl azoles that are nanomolar binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
8-anilinonaphthalene-1-sulfonic acidFatty acid-binding protein, adipocyteKi (nM)1000N/AN/ADetails
8-anilinonaphthalene-1-sulfonic acidFatty acid-binding protein, adipocyteKd (nM)150N/AN/ADetails
Palmitic AcidFatty acid-binding protein, adipocyteKi (nM)336N/AN/ADetails
Palmitic AcidFatty acid-binding protein, epidermalKi (nM)802N/AN/ADetails