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Literature DB >> 16022186

Application of pharmaceutical profiling assays for optimization of drug-like properties.

Abstract

Pharmaceutical profiling assays provide an early assessment of drug-like properties, such as solubility, permeability, metabolism, stability and drug-drug interactions. This information can be used to alert project teams to potential property issues, predict and diagnose in vivo assay results, guide structure-property relationships, provide insight into structure modification, and help drug discovery teams to make informed decisions. Successful drugs can be developed when biological activities of interest and pharmaceutical properties are optimized in parallel.

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Year: 2005 PMID： 16022186

Source DB: PubMed Journal: Curr Opin Drug Discov Devel ISSN： 1367-6733

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Cited

13 in total

1. A bifunctional dimethylsulfoxide substitute enhances the aqueous solubility of small organic molecules.

Authors: Melissa M Sprachman; Peter Wipf
Journal: Assay Drug Dev Technol Date: 2011-12-22 Impact factor: 1.738

2. Importance of hydrogen-bonding sites in the chiral recognition mechanism between racemic D3 terbium(III) complexes and amino acids.

Authors: Ahmed Moussa; Christine Pham; Shruthi Bommireddy; Gilles Muller
Journal: Chirality Date: 2009-05 Impact factor: 2.437

3. Effect of the Plasticizer DEHP in Blood Collection Bags on Human Plasma Fraction Unbound Determination for Alpha-1-Acid Glycoprotein (AAG) Binding Drugs.

Authors: Nicholas Ingram; Christopher Dishinger; Jennifer Wood; J Matthew Hutzler; Sherri Smith; Michael Huskin
Journal: AAPS J Date: 2018-11-16 Impact factor: 4.009

Review 4. Probing the links between in vitro potency, ADMET and physicochemical parameters.

Authors: M Paul Gleeson; Anne Hersey; Dino Montanari; John Overington
Journal: Nat Rev Drug Discov Date: 2011-03 Impact factor: 84.694

5. Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling.

Authors: Mark E McDonnell; Matthew D Vera; Benjamin E Blass; Jeffrey C Pelletier; Richard C King; Carmen Fernandez-Metzler; Garry R Smith; Jay Wrobel; Suzie Chen; Brian A Wall; Allen B Reitz
Journal: Bioorg Med Chem Date: 2012-07-21 Impact factor: 3.641

6. Design, synthesis, and biological evaluation of N-alkylated deoxynojirimycin (DNJ) derivatives for the treatment of dengue virus infection.

Authors: Wenquan Yu; Tina Gill; Lijuan Wang; Yanming Du; Hong Ye; Xiaowang Qu; Ju-Tao Guo; Andrea Cuconati; Kang Zhao; Timothy M Block; Xiaodong Xu; Jinhong Chang
Journal: J Med Chem Date: 2012-06-29 Impact factor: 7.446

Application of pharmaceutical profiling assays for optimization of drug-like properties.

1. A bifunctional dimethylsulfoxide substitute enhances the aqueous solubility of small organic molecules.

2. Importance of hydrogen-bonding sites in the chiral recognition mechanism between racemic D3 terbium(III) complexes and amino acids.

3. Effect of the Plasticizer DEHP in Blood Collection Bags on Human Plasma Fraction Unbound Determination for Alpha-1-Acid Glycoprotein (AAG) Binding Drugs.

Review 4. Probing the links between in vitro potency, ADMET and physicochemical parameters.

5. Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling.

6. Design, synthesis, and biological evaluation of N-alkylated deoxynojirimycin (DNJ) derivatives for the treatment of dengue virus infection.

Review 7. Paradigm shift in toxicity testing and modeling.

8. Dipeptide Prodrugs of the Glutamate Modulator Riluzole.

Review 9. Luminescent chiral lanthanide(III) complexes as potential molecular probes.

10. Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries.