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Lead development: validation and application of high throughput screening for determination of pharmacokinetic parameters for enzyme inhibitors.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 1996 May; Vol. 4 (5), pp. 639-43. - Publication Year :
- 1996
-
Abstract
- An approach utilizing robotics (automation) for the rapid and reliable determination of protease inhibitor concentration in rat plasma samples is described. The bioassay protocol using an immobilized peptide substrate allows high sample throughput, compatible with parallel synthesis/SAR development strategy.
- Subjects :
- Amino Acid Sequence
Animals
Chromatography, High Pressure Liquid methods
Dose-Response Relationship, Drug
Extracellular Matrix enzymology
Fluorescence
Humans
Hydrolysis
Metalloendopeptidases metabolism
Methanol chemistry
Molecular Sequence Data
Protease Inhibitors blood
Rats
Recombinant Proteins metabolism
Reproducibility of Results
Structure-Activity Relationship
Time Factors
Biological Assay methods
Metalloendopeptidases antagonists & inhibitors
Protease Inhibitors pharmacokinetics
Robotics methods
Subjects
Details
- Language :
- English
- ISSN :
- 0968-0896
- Volume :
- 4
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 8804527
- Full Text :
- https://doi.org/10.1016/0968-0896(96)00057-0