Todd J. Kohn
Eli Lilly and Company
26 Papers
202 Citations
Todd J. Kohn is an academic researcher from Eli Lilly and Company. The author has contributed to research in topics: Discovery and development of direct thrombin inhibitors & Chemistry. The author has an hindex of 9, co-authored 26 publications. Previous affiliations of Todd J. Kohn include Amgen.
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Papers
Dibasic benzo[b]thiophene derivatives as a novel class of active site-directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure-activity relationships, and binding orientation.
Daniel Jon Sall,Jolie Anne Bastian,Stephen L. Briggs,John A. Buben,Nickolay Y. Chirgadze,David K. Clawson,Michael L. Denney,Deborah D. Giera,Donetta S. Gifford-Moore,Richard Waltz Harper,Kenneth Lee Hauser,Valentine J. Klimkowski,Todd J. Kohn,Ho-Shen Lin,Jefferson Ray Mccowan,Alan David Palkowitz,Gerald F. Smith,K. Takeuchi,Kenneth Jeff Thrasher,Jennifer M. Tinsley,Barbara G. Utterback,Sau-Chi B. Yan,Minsheng Zhang +22 more
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Discovery and in Vivo Evaluation of Dual PI3Kβ/δ Inhibitors
Felix Gonzalez-Lopez de Turiso,Youngsook Shin,Matthew Frank Brown,Mario G. Cardozo,Yi Chen,David Fong,Xiaolin Hao,Xiao He,Kirk Henne,Yi-Ling Hu,Michael G. Johnson,Todd J. Kohn,Julia Winslow Lohman,Helen J. McBride,Lawrence R. McGee,Julio C. Medina,Daniela Metz,Kent Miner,Deanna Mohn,Vatee Pattaropong,Jennifer Seganish,Jillian L. Simard,Sharon Wannberg,Douglas A. Whittington,Gang Yu,Timothy D. Cushing +25 more
TL;DR: The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ dual inhibitor that displayed suitable physicochemical properties and pharmacokinetic profile for animal studies and was found to be efficacious in animal models of inflammation.
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Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.
Kumiko Takeuchi,Todd J. Kohn,Nicholas Allan Honigschmidt,Vincent Patrick Rocco,Patrick Gianpietro Spinazze,Daniel James Koch,David L. Nelson,D.Bradley Wainscott,Laura J Ahmad,Janice Shaw,Penny G. Threlkeld,David T. Wong +11 more
TL;DR: In vivo evaluation of this series of compounds demonstrated elevated extracellular serotonin levels from the basal and quick recovery of neuron firing that was presumably suppressed by the initial acute activation of 5-HT1A somatodendritic autoreceptors.
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Dibasic benzo[B]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[B]thiophenes.
Kumiko Takeuchi,Todd J. Kohn,Daniel Jon Sall,Michael L. Denney,Jefferson Ray Mccowan,Smith Gf,Donetta S. Gifford-Moore +6 more
TL;DR: A novel series of benzo[b]thiophene diamine thrombin inhibitors with a conformationally restricted C3-side chain 3 was investigated and resulted in the discovery of a potentThrombin inhibitor 27 that was over 750-fold more potent than the initial lead compound 1.
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Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Potency, efficacy, and pharmacokinetic properties of modified C-3 side chain derivatives.
Daniel Jon Sall,Dianna L. Bailey,Jolie Anne Bastian,John A. Buben,Nickolay Y. Chirgadze,Amy Clemens-Smith,Michael L. Denney,Matthew J. Fisher,Deborah D. Giera,Donetta S. Gifford-Moore,Richard Waltz Harper,Lea M. Johnson,Valentine J. Klimkowski,Todd J. Kohn,Ho-Shen Lin,Jefferson Ray Mccowan,Alan David Palkowitz,Michael Enrico Richett,Gerald F. Smith,David W. Snyder,Kumiko Takeuchi,John E. Toth,Minsheng Zhang +22 more
TL;DR: The more potent members of this series have been studied in an arterial/venous shunt (AV shunt) model of thrombosis and were found to be efficacious in reducing clot formation, but their efficacy is currently limited by their rapid and extensive distribution following administration.
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