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- Design
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Drug discovery handbook
Published 2005Table of Contents: “…[et al.] -- Metal-enhanced fluorescence: application to high-throughput screening and drug discovery / Kadir Aslan .. [et al,] -- Methods for the design and analysis of replicate-experiment studies to establish assay reproducibility and the equivalence of two potency assays / Brian J. …”
An electronic book accessible through the World Wide Web; click to view
Electronic eBook -
8
Polypharmacology in drug discovery
Published 2012Table of Contents: “…Hopkins Part A: Polypharmacology - a safety concern in drug discovery. 1 The relevance of off-target polypharmacology Bruce D. Car 2 Screening for safety-relevant off-target activities Laszlo Urban, Steven Whitebread, Jacques Hamon, Dmitri Mikhailov and Kamal Azzaoui 2.1 Introduction. 2.2 General aspects. 2.3 Selection of off-targets. 2.4 In silico approaches to off-target profiling .2.5 Summary and conclusions. 3 Pharmacological promiscuity and molecular propertiesJens-Uwe Peters 3.1 Introduction: pharmacological promiscuity in the history of drug discovery. 3.2 Lipophilicity. 3.3 Molecular weight. 3.4 Ionisation state. 3.5 Other molecular descriptors and structural motifs. 3.6 Implications for drug discovery. 4 Kinases as antitargets in genotoxicity Stephan Kirchner 4.1 Protein Kinases and inhibitor-binding sites. 4.2 Cyclin-Dependent Kinases (CDKs) controlling unregulated cell proliferation. 4.3 Mitotic kinases as guardians protecting cells from aberrant chromosome segregation. 5 Activity at cardiovascular ion channels: a key issue for drug discoveryIan M. …”
An electronic book accessible through the World Wide Web; click to view
Electronic eBook -
9
Evaluation of enzyme inhibitors in drug discovery a guide for medicinal chemists and pharmacologists /
Published 2013Table of Contents: “…Assay Considerations for Compound Library Screening.4.1 Defining Inhibition Signal Robustness, and Hit Criteria.4.2 Measuring Initial Velocity.4.2.1 End-Point and Kinetic Readouts.4.2.2 Effects of Enzyme Concentration.4.3 Balanced Assay Conditions.4.3.1 Balancing Conditions for Multisubstrate Reactions.4.4 Order of Reagent Addition.4.5 Use of Natural Substrates and Enzymes.4.6 Coupled Enzyme Assays.4.7 Hit Validation and Progression.4.8 Summary.References.5. …”
An electronic book accessible through the World Wide Web; click to view
Electronic eBook
