David E. Clarke
Amgen
3 Papers
14 Citations
David E. Clarke is an academic researcher from Amgen. The author has contributed to research in topics: Receptor & Nucleophile. The author has an hindex of 3, co-authored 3 publications. Previous affiliations of David E. Clarke include New Mexico State University.
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Papers
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Kaustav Biswas,Aiwen Li,Jian J. Chen,Derin C. D'amico,Christopher H. Fotsch,Nianhe Han,Jason Brooks Human,Qingyian Liu,Mark H. Norman,Bobby Riahi,Chester Chenguang Yuan,Hideo Suzuki,David A. Mareska,James Zhan,David E. Clarke,Andras Toro,Robert D. Groneberg,Burgess Laurence E,Dianna Lester-Zeiner,Gloria Biddlecome,Barton H. Manning,Leyla Arik,Hong Dong,Ming Huang,Augustus Kamassah,Richard Loeloff,Hong Sun,Feng-Yin Hsieh,Gondi N. Kumar,Gordon Ng,Randall W. Hungate,Benny C. Askew,Eileen Johnson +32 more
TL;DR: The most potent analog at the human receptor, compound 38, was also active in a rabbit B1 receptor cellular assay and displayed in vivo activity in two rabbit models, a pharmacodynamic model with a blood pressure readout and an efficacy model of inflammatory pain.
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Identification of a Nonpeptidic and Conformationally Restricted Bradykinin B1 Receptor Antagonist with Anti-Inflammatory Activity
Derin C. D'amico,Toshi Aya,Jason Brooks Human,Christopher H. Fotsch,Jian J. Chen,Kaustav Biswas,Bobby Riahi,Mark H. Norman,Christopher A. Willoughby,Randall W. Hungate,Paul J. Reider,Gloria Biddlecome,Dianna Lester-Zeiner,Carlo van Staden,Eileen Johnson,Augustus Kamassah,Leyla Arik,Judy Wang,Vellarkad N. Viswanadhan,Robert D. Groneberg,James Zhan,Hideo Suzuki,Andras Toro,David A. Mareska,David E. Clarke,Darren Martin Harvey,Burgess Laurence E,Laird Ellen,Benny C. Askew,Gordon Ng +29 more
TL;DR: The discovery of chroman 28, a potent and selective antagonist of human, nonhuman primate, rat, and rabbit bradykinin B1 receptors, is reported and a novel method to calculate entropy is introduced and ascribed approximately 30% of the gained affinity to decreased conformational entropy.
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Origins of Regioselectivity in the Reactions of α-Lactams with Nucleophiles. Two Distinct Acid-Catalyzed Pathways Involving O- and N-Protonation
TL;DR: The mechanism thus developed is very useful for understanding the changes in rates and product distributions in the reactions of sterically stabilized alpha-lactams with nucleophiles and can be extrapolated to other alpha-Lactams so that a more coherent picture of alpha- lactam reactivity can be developed.
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