Principles and Processes of Early Drug Discovery
The early drug discovery process involves target identification and validation, hit discovery through confirming active compounds, assay development for testing effects, and employs various screening strategies such as high-throughput, virtual, phenotypic, and target-based screening to identify promising drug candidates.
Drug discovery is a long process that flows from target validation to clinical development, passing through the hit-to-lead stage. The early stages of drug development usually involve screening for active compounds.
Principles of Early Drug Discovery
- 1.
Target identification and validation
- This step involves identifying a target function and its role in the disease. It also involves learning how the drug can provide a therapeutic benefit at an acceptable safety level.
- 2.
Hit discovery process
- A drug discovery hit is a compound with promising activity against the target. This step requires confirming findings with additional testing.
- 3.
Assay development
- This step involves the creation of test systems used to evaluate the effects of the chemical compounds in an organism or organic sample.
What Screening Strategies Are Used in Drug Discovery?
An essential part of the drug discovery process, screening involves testing compounds to develop as drugs. The combination of screening strategies depends on the goal of the drug discovery and the resources available.
Different types of screening strategies include:
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High-throughput screening: Uses automatic equipment to rapidly test large numbers of compounds against a specific target to help identify compounds with the potential to bind to the target and modulate the pathway in a desirable way.
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Virtual screening: Uses computer modeling to predict the affinity of compounds for binding to a specific target. This helps identify compounds that are likely active with the target of interest, narrowing potential combinations to the most promising candidates.
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Phenotypic screening: Tests compounds for their ability to produce a specific phenotype of a cell or organism, helping to identify compounds with the potential to modulate specific targets.
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Target-based screening: Involves testing compounds for their ability to modulate a specific target. This can be achieved by using several types of biological assays.
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Natural product screening: Tests naturally occurring products for their potential activity against a specific target or pathway. This can be used to identify compounds with the potential for development into new drugs.
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How are small molecule drugs developed?
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