Literature DB >> 23360135

Lipophilic efficiency: the most important efficiency metric in medicinal chemistry.

Kevin D Freeman-Cook, Robert L Hoffman, Ted W Johnson.   

Abstract

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Year:  2013        PMID： 23360135     DOI： 10.4155/fmc.12.208

Source DB:  PubMed          Journal:  Future Med Chem        ISSN： 1756-8919            Impact factor:   3.808


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  28 in total

Review 1.  The role of ligand efficiency metrics in drug discovery.

Authors:  Andrew L Hopkins; György M Keserü; Paul D Leeson; David C Rees; Charles H Reynolds
Journal:  Nat Rev Drug Discov       Date:  2014-02       Impact factor: 84.694

2.  Ligand efficiency metrics considered harmful.

Authors:  Peter W Kenny; Andrei Leitão; Carlos A Montanari
Journal:  J Comput Aided Mol Des       Date:  2014-06-05       Impact factor: 3.686

3.  Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.

Authors:  Michael A Brodney; Elizabeth M Beck; Christopher R Butler; Gabriela Barreiro; Eric F Johnson; David Riddell; Kevin Parris; Charles E Nolan; Ying Fan; Kevin Atchison; Cathleen Gonzales; Ashley E Robshaw; Shawn D Doran; Mark W Bundesmann; Leanne Buzon; Jason Dutra; Kevin Henegar; Erik LaChapelle; Xinjun Hou; Bruce N Rogers; Jayvardhan Pandit; Ricardo Lira; Luis Martinez-Alsina; Peter Mikochik; John C Murray; Kevin Ogilvie; Loren Price; Subas M Sakya; Aijia Yu; Yong Zhang; Brian T O'Neill
Journal:  J Med Chem       Date:  2015-04-01       Impact factor: 7.446

4.  Copper-Catalyzed Chan-Lam Cyclopropylation of Phenols and Azaheterocycles.

Authors:  Joseph Derosa; Miriam L O'Duill; Matthew Holcomb; Mark N Boulous; Ryan L Patman; Fen Wang; Michelle Tran-Dubé; Indrawan McAlpine; Keary M Engle
Journal:  J Org Chem       Date:  2018-03-13       Impact factor: 4.354

5.  Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.

Authors:  Sharan K Bagal; Peter J Bungay; Stephen M Denton; Karl R Gibson; Melanie S Glossop; Tanya L Hay; Mark I Kemp; Charlotte A L Lane; Mark L Lewis; Graham N Maw; William A Million; C Elizabeth Payne; Cedric Poinsard; David J Rawson; Blanda L Stammen; Edward B Stevens; Lisa R Thompson
Journal:  ACS Med Chem Lett       Date:  2015-04-29       Impact factor: 4.345

6.  Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity.

Authors:  Tyler S Beyett; Xinmin Gan; Shannon M Reilly; Andrew V Gomez; Louise Chang; John J G Tesmer; Alan R Saltiel; Hollis D Showalter
Journal:  Bioorg Med Chem       Date:  2018-09-20       Impact factor: 3.641

Review 7.  The essential roles of chemistry in high-throughput screening triage.

Authors:  Jayme L Dahlin; Michael A Walters
Journal:  Future Med Chem       Date:  2014-07       Impact factor: 3.808

8.  Discovery of Selective, Substrate-Competitive, and Passive Membrane Permeable Glycogen Synthase Kinase-3β Inhibitors: Synthesis, Biological Evaluation, and Molecular Modeling of New C-Glycosylflavones.

Authors:  Zhibin Liang; Qing X Li
Journal:  ACS Chem Neurosci       Date:  2018-02-13       Impact factor: 4.418

9.  Synthesis and anticonvulsant activity of phenoxyacetyl derivatives of amines, including aminoalkanols and amino acids.

Authors:  Katarzyna Pańczyk; Dorota Żelaszczyk; Paulina Koczurkiewicz; Karolina Słoczyńska; Elżbieta Pękala; Ewa Żesławska; Wojciech Nitek; Paweł Żmudzki; Henryk Marona; Anna Waszkielewicz
Journal:  Medchemcomm       Date:  2018-10-19       Impact factor: 3.597

10.  Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of aldehyde dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy.

Authors:  Brandt C Huddle; Edward Grimley; Mikhail Chtcherbinine; Cameron D Buchman; Cyrus Takahashi; Bikash Debnath; Stacy C McGonigal; Shuai Mao; Siwei Li; Jeremy Felton; Shu Pan; Bo Wen; Duxin Sun; Nouri Neamati; Ronald J Buckanovich; Thomas D Hurley; Scott D Larsen
Journal:  Eur J Med Chem       Date:  2020-12-03       Impact factor: 6.514
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