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Review

Assay Operations for SAR Support

Benoit Beck  1 , Yun-Fei Chen, Walthere Dere, Viswanath Devanarayan, Brian J. Eastwood, Mark W. Farmen, Stephen J. Iturria, Phillip W. Iversen  1 , Steven D. Kahl, Roger A. Moore, Barry D. Sawyer, Jeffrey Weidner
Sarine Markossian  1 , Abigail Grossman  1 , Hannah Baskir  1 , Michelle Arkin  2 , Douglas Auld  3 , Christopher Austin  4 , Jonathan Baell  5 , Kyle Brimacombe  1 , Thomas D.Y. Chung  6 , Nathan P. Coussens  7 , Jayme L. Dahlin  8 , Viswanath Devanarayan  9 , Timothy L. Foley  10 , Marcie Glicksman  11 , Kirill Gorshkov  12 , Stefan Grotegut  13 , Matthew D. Hall  1 , Samuel Hoare  14 , James Inglese  1 , Philip W. Iversen  15 , Madhu Lal-Nag  16 , Zhuyin Li  12 , Jason R. Manro  13 , James McGee  17 , Allison Norvil  13 , Mackenzie Pearson  13 , Terry Riss  18 , Peter Saradjian  19 , G. Sitta Sittampalam  20 , Michael A. Tarselli  21 , O. Joseph Trask Jr.  22 , Jeffrey R. Weidner  23 , Mary Jo Wildey  24 , Kelli Wilson  1 , Menghang Xia  1 , Xin Xu  1
, editors.
In: Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004.
[updated ].
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Review

Assay Operations for SAR Support

Benoit Beck et al.
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Excerpt

Most biological assays measure potency of compounds as an activity coefficient, frequently known as molar concentration of inhibitor at 50% response (IC50) or an agonist concentration at 50% biological activity (EC50). Since biological response responses are non-linear and generally sigmoidal in shape, appropriate curve fitting is important. In addition, the variability in measured IC50/EC50 should be monitored to ensure reliable and robust data analysis of the assay curves to support expensive SAR operations in drug discovery. This chapter addresses in detail significant concepts in curve-fitting techniques and statistical concepts and tools required SAR support.

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References

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