High Throughput Screening (HTS) is a drug discovery process that uses automation to quickly assay large numbers of compounds, often over 50,000 per day. The goal of HTS is to identify hits or leads that modify a biological target in the desired manner at low concentrations, and may represent new structures. HTS assays use various detection methods like spectroscopy, chromatography, and calorimetry to rapidly screen libraries of natural products, combinatorial compounds, and other drug-like molecules in order to discover novel bioactive agents.

1. HIGH THROUGHPUT SCREENING (HTS)
PRESENTED BY:
IQRAR AHMAD
(M.PHARM SECOND SEMESTER)
DEPARTMENT OF PHARMACEUTICAL CHEMISTRY
R.C PATEL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH,SHIRPUR
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2. HIGH THROUGHPUT SCREENING (HTS)
HTS is process by which large number of
compounds are rapidly tested for their
ability to modify the properties of a selected
biological target.
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3. INTRODUCTION
High Throughput Screening (HTS) is a
drug-discovery process widely used in the
pharmaceutical industry. It leverages
automation to quickly assay the biological
or biochemical activity of a large number
of drug-like compounds.
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4. It is a useful for discovering ligands for
receptors, enzymes, ion-channels or other
pharmacological targets, or pharmacologically
profiling a cellular or biochemical pathway of
interest.
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5. GOAL OF HTS
Goal is to identify ‘hits’ or ‘leads’
 - affect target in desired manner
 active at fairly low concenteration ( more likely to show
specificity)
 - new structure
 HTS = 50,000-100,000 compounds screened per day!!!
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6. DETECTION METHODS IN HTS:
• Spectroscopy
• Mass Spectrometry
• Chromatography
• Calorimetry
• X-ray diffraction
• Microscopy
• Radioactive methods 6

7. SPECTROSCOPY IN HTS:
• Fluorescence Spectroscopy
• Total internal reflection fluorescence (TIRF)
• Nuclear magnetic resonance (NMR)
• Absorption and luminescence sp.
• Fourier transformed infrared sp. (FTIR)
• Light scattering
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8. CHROMATOGRAPHY IN HTS:
• Gas chromatography (GC)
• Thin layer chromatography
• Liquid chromatography (HPLC)
• Ion Exchange chromatography
• Reverse phase chromatography
• Hydrophobic interaction chromatography
• Affinity chromatography 8

9. CALORIMETRY IN HTS:
• Isothermal titration Calorimetry (ITC)
• Differential scanning Calorimetry (DSC)
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10. ADVANTAGES OF HTS
 High sensitivity of assay (single molecule detection)
 High speed of assay (automation)
 Fast data processing of results
 Reproducibility
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11. DISADVANTAGES:
 High cost
 Low data quality
 Local contamination
 Need of relatively pure product
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12. USES OF HTS:
 To screen for all kind of novel biological active compounds
(libraries):
• Natural products
• Combinatorial Libraries (peptides, chemicals…)
• Biological libraries
 To screen Micro arrays such as:
• DNA chips
• RNA chips
• Protein chips 12

13. NEWER METHOD IN HTS:
 High-Throughput, Fluorescence-Based Screening
For screening, expressed proteins are labelled
either as fusions with green fluorescent protein (GFP)or
through translational incorporation of a fluorescent amino
acid derivative, BODIPY-FL-Lysine.
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14. REFRENCES:
1. “Medicnal chemistry” by ashutosh kar fifth revised and
expanded edition new age international publication,reprint
2011
2. Review On: High-Throughput Screening Is An Approach To
Drug Discovery by Ashok A. Hajare, Sachin S. American
Journal Of Pharmatech Research
3. Text book of Lead Generation Approaches In Drug
Discovery by Zoran Rankovic
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