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Discovery of small molecule human FPR1 receptor antagonists |
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| Authors: | Unitt John Fagura Malbinder Phillips Tim King Sarah Perry Matthew Morley Andrew MacDonald Cathy Weaver Richard Christie Jadeen Barber Simon Mohammed Rukhsana Paul Melanie Cook Andrew Baxter Andrew |
| Institution: | a AstraZeneca R&D Charnwood, Bioscience, Bakewell Road, Loughborough LE11 5RH, UK b DMPK, Bakewell Road, Loughborough LE11 5RH, UK c Chemistry Departments, Bakewell Road, Loughborough LE11 5RH, UK |
| Abstract: | The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target. |
| Keywords: | FPR1 antagonist Hit-to-lead Small molecule |
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