All Stories

  1. The rule of five should not impede anti-parasitic drug development

    Article • International Journal for Parasitology Drugs and Drug Resistance, August 2017, Elsevier

    Dr Christopher A Lipinski

  2. Rule of five in 2015 and beyond: Target and ligand structural limitations, ligand chemistry structure and drug discovery project decisions

    Article • Advanced Drug Delivery Reviews, June 2016, Elsevier

    Dr Christopher A Lipinski

  3. Badapple: promiscuity patterns from noisy evidence

    Article • Journal of Cheminformatics, May 2016, Springer Science + Business Media

    Dr Christopher A Lipinski

  4. simple proxies for enthalpy and entropy

    Article • Pharmaceutical Research, August 2015, Springer Science + Business Media

    Dr Sean Ekins, Dr Christopher A Lipinski

  5. small molecules active against Ebola

    Article • F1000Research, February 2015, Faculty of 1000, Ltd.

    Dr Sean Ekins, Dr Christopher A Lipinski

  6. Associated challenges with the divergent expansions of public and commercial sources of molecules

    Article • Journal of Medicinal Chemistry, December 2014, American Chemical Society (ACS)

    Dr Antony John Williams, Dr Sean Ekins, Dr Christopher Southan, Dr Nadia Litterman, Dr Christopher A Lipinski

  7. Modeling the decisions of a medicinal chemist

    Article • Journal of Chemical Information and Modeling, October 2014, American Chemical Society (ACS)

    Dr Sean Ekins, Dr Nadia Litterman, Dr Christopher A Lipinski

  8. A Perspective on the Evolution of Collaborative Drug Discovery and Future Challenges

    Article • April 2014, Wiley

    Dr Christopher A Lipinski

  9. My Perspective on Time, Managers—and Scientific Fun

    Article • January 2013, Elsevier

    Dr Christopher A Lipinski

  10. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

    Article • Advanced Drug Delivery Reviews, December 2012, Elsevier

    Dr Christopher A Lipinski

  11. Phenotypic and In Vivo Screening: Lead Discovery and Drug Repurposing

    Article • April 2012, Royal Society of Chemistry

    Dr Christopher A Lipinski

  12. PhenotypicIn VivoScreening to Identify New, Unpredicted Indications for Existing Drugs and Drug Candidates

    Article • April 2012, Wiley

    Dr Christopher A Lipinski

  13. MLR-1023 Is a Potent and Selective Allosteric Activator of Lyn Kinase In Vitro That Improves Glucose Tolerance In Vivo

    Article • Journal of Pharmacology and Experimental Therapeutics, April 2012, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Christopher A Lipinski

  14. The Lyn Kinase Activator MLR-1023 Is a Novel Insulin Receptor Potentiator that Elicits a Rapid-Onset and Durable Improvement in Glucose Homeostasis in Animal Models of Type 2 Diabetes

    Article • Journal of Pharmacology and Experimental Therapeutics, March 2012, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Dr Christopher A Lipinski

  15. Drug repurposing

    Article • Drug Discovery Today Therapeutic Strategies, December 2011, Elsevier

    Dr Christopher A Lipinski

  16. Analysis and hit filtering of a very large library of compounds screened against Mycobacterium tuberculosis

    Article • Molecular BioSystems, January 2010, Royal Society of Chemistry

    Dr Sean Ekins, Dr Christopher A Lipinski

  17. Erratum: A crowdsourcing evaluation of the NIH chemical probes

    Article • August 2009, Nature

    Dr Christopher A Lipinski

  18. A crowdsourcing evaluation of the NIH chemical probes

    Article • July 2009, Nature

    Dr Christopher A Lipinski

  19. Beautiful Biology But Bad Chemistry: Recognizing Chemistry Problems Earlier Rather Than Later

    Article • Antiviral Research, May 2009, Elsevier

    Dr Christopher A Lipinski

  20. Overview of Hit to Lead: The Medicinal Chemist's Role from HTS Retest to Lead Optimization Hand Off

    Article • January 2009, Springer Science + Business Media

    Dr Christopher A Lipinski

  21. Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824

    Article • Bioorganic & Medicinal Chemistry Letters, April 2008, Elsevier

    Dr Christopher A Lipinski

  22. Compound Properties and Drug Quality

    Article • January 2008, Elsevier

    Dr Christopher A Lipinski

  23. CHRISTOPHER LIPINSKI

    Article • Chemical & Engineering News, November 2007, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  24. Drug Solubility in Water and Dimethylsulfoxide

    Article • October 2007, Wiley

    Dr Christopher A Lipinski

  25. The anti-intellectual effects of intellectual property

    Article • Current Opinion in Chemical Biology, August 2006, Elsevier

    Dr Christopher A Lipinski

  26. High Throughput Sonication: Evaluation for Compound Solubilization

    Article • Combinatorial Chemistry & High Throughput Screening, September 2005, Bentham Science Publishers

    Dr Christopher A Lipinski

  27. Capter 11 Filtering in Drug Discovery

    Article • January 2005, Elsevier

    Dr Christopher A Lipinski

  28. Chemical Tools for Indications Discovery

    Article • January 2005, Elsevier

    Dr Christopher A Lipinski

  29. Navigating chemical space for biology and medicine

    Article • December 2004, Nature

    Dr Christopher A Lipinski

  30. Lead- and drug-like compounds: the rule-of-five revolution

    Article • Drug Discovery Today Technologies, December 2004, Elsevier

    Dr Christopher A Lipinski

  31. Solubility in the Design of Combinatorial Libraries

    Article • December 2003, Wiley

    Dr Christopher A Lipinski

  32. COMPOUND PROPERTIES AND DRUG QUALITY

    Article • January 2003, Elsevier

    Dr Christopher A Lipinski

  33. Chris Lipinski discusses life and chemistry after the Rule of Five

    Article • Drug Discovery Today, January 2003, Elsevier

    Dr Christopher A Lipinski

  34. Single-Mode Compound Retrieval for QSAR, QSPR Data Sets, and Batch Mode Exact Structure Searching

    Article • Journal of Pharmaceutical Sciences, December 2002, Elsevier

    Dr Christopher A Lipinski

  35. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings1PII of original article: S0169-409X(96)00423-1. The article was originally published in Advanced Drug Delivery Reviews 23 (1997...

    Article • Advanced Drug Delivery Reviews, March 2001, Elsevier

    Dr Christopher A Lipinski

  36. Drug-like properties and the causes of poor solubility and poor permeability

    Article • Journal of Pharmacological and Toxicological Methods, July 2000, Elsevier

    Dr Christopher A Lipinski

  37. Quantitative Structure−Activity Relationships among Macrolide Antibacterial Agents:  In Vitro and in Vivo Potency against Pasteurella multocida

    Article • Journal of Medicinal Chemistry, April 1997, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  38. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

    Article • Advanced Drug Delivery Reviews, January 1997, Elsevier

    Dr Christopher A Lipinski

  39. Hydantoin bioisosteres. In vivo active spiro hydroxy acetic acid aldose reductase inhibitors

    Article • Journal of Medicinal Chemistry, June 1992, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  40. pKa, Log P and MedChem CLOGP Fragment Values of Acidic Heterocyclic Potential Bioisosteres

    Article • Quantitative Structure-Activity Relationships, January 1991, Wiley

    Dr Christopher A Lipinski

  41. Physical parameters for brian uptake: optimizing log P, log D and pKa of T H A

    Article • Bioorganic & Medicinal Chemistry Letters, January 1991, Elsevier

    Dr Christopher A Lipinski

  42. N‐chlorination of dilantin and sorbinil

    Article • Journal of Heterocyclic Chemistry, September 1990, Wiley

    Dr Christopher A Lipinski

  43. Acidic isostere design: Synthetic strategies and recent progress in understanding electronic properties and metabolic stability

    Article • Pesticide Science, January 1990, Wiley

    Dr Christopher A Lipinski

  44. Medicinal chemistry of aldose reductase inhibitors

    Article • Medicinal Research Reviews, April 1988, Wiley

    Dr Christopher A Lipinski

  45. Bioisosteric prototype design of biaryl imidazolyl and triazolyl competitive histamine H2-receptor antagonists

    Article • Journal of Medicinal Chemistry, November 1986, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  46. Chapter 27. Bioisosterism in Drug Design

    Article • January 1986, Elsevier

    Dr Christopher A Lipinski

  47. 2‐Amino‐ and 2‐guanidino‐4‐thiazolylpyrimidines

    Article • Journal of Heterocyclic Chemistry, November 1985, Wiley

    Dr Christopher A Lipinski

  48. Pseudosymmetry and bioisosterism in biaryl pyridyl competitive histamine H2-receptor antagonists

    Article • Journal of Medicinal Chemistry, November 1985, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  49. An improved preparation and use of 2-bromoacetoacetaldehyde in a new synthesis of 2-substituted-4-acetylimidazoles

    Article • The Journal of Organic Chemistry, February 1984, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  50. Chapter 17. Aldose Reductase Inhibitors as a New Approach to the Treatment of Diabetic Complications

    Article • January 1984, Elsevier

    Dr Christopher A Lipinski

  51. Bioisosteric design of conformationally restricted pyridyltriazole histamine H2-receptor antagonists

    Article • Journal of Medicinal Chemistry, January 1983, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  52. Chapter 10. Agents Affecting Gastrointestinal Functions

    Article • January 1977, Elsevier

    Dr Christopher A Lipinski

  53. Chapter 10. Agents Affecting Gastrointestinal Functions

    Article • January 1977, Elsevier

    Dr Christopher A Lipinski

  54. Total synthesis of terpenes. XIX. Synthesis of 8-methoxy-4a.beta., 10b.beta., 12a.alpha.-trimethyl-3,4,4a,4b.alpha.,5,6,10b,11,12,12a-decahydrochrysen-1(2H)-one, a key intermediate in the total synthesis of (+-)-shionone

    Article • The Journal of Organic Chemistry, April 1975, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  55. Chapter 10. Agents Affecting Gastrointestinal Functions

    Article • January 1975, Elsevier

    Dr Christopher A Lipinski

  56. Total synthesis of dl-shionone, a tetracyclic triterpene

    Article • Journal of the American Chemical Society, May 1974, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  57. Transmission of substituent effects in heterocycles. Rates of solvolysis of substituted 1-(2-thienyl)ethyl p-nitrobenzoates

    Article • The Journal of Organic Chemistry, August 1972, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  58. Correlation of the reactivity of thiophene derivatives

    Article • The Journal of Organic Chemistry, May 1970, American Chemical Society (ACS)

    Dr Christopher A Lipinski

  59. The utility of the coupling reaction between propargyl grignard reagent and allylic halides for the synthesis of acetylenes

    Article • Tetrahedron Letters, January 1970, Elsevier

    Dr Christopher A Lipinski

  60. ADMET Screen

    Article • Springer Science + Business Media

    Dr Christopher A Lipinski