Optimization in drug discovery : in vitro methods / edited by Zhengyin Yan, Gary W. Caldwell.

Includes bibliographical references and index.

pKa, solubility and lipophilicity: assessing physicochemical properties of lead compounds / Yushen Guo and Hong Shen -- Use of caco-2 cell monolayers to study drug absorption and metabolism / Ming Hu ... [et al.] -- Absorption screening using the PAMPA approach / Jeffrey A. Ruell and Alex Avdeef -- In situ single-pass perfused rat intestinal model for absorption and metabolism / Eun Ju Jeong ... [et al.] -- In vitro permeation study with bovine brain microvessel endothelial cells / Sung-Hack Lee ... [et al.] -- An enzymatic microplate assay for testing P-glycoprotein substrates and inhibitors / S. Orlowski, J. Nugier and Eric Ezan -- Evaluation of drug-transporter interactions using in vitro cell models / Yaming Su and Patrick J. Sinko -- Plasma protein-binding methods in drug discovery / Lucinda H. Cohen --

Isothermal titration calorimetry characterization of drug-binding energetics to blood proteins / Gary W. Caldwell and Zhengyin Yan -- Metabolic stability assessed by liver microsomes and hepatocytes / David C. Ackley, Kevin T. Rockich, and Timothy R. Baker -- In vitro drug metabolite profiling using hepatic S9 and human liver microsomes / Wu-Nan Wu and Linda A. McKown --

In vitro identification of UDP-glucuronosyltransferases involved in drug metabolism / Michael H. Court -- In vitro CYP induction in human hepatocytes / Daniel R. Mudra and Andrew Parkinson -- High-throughput screening of human cytochrome P450 inhibitors using fluorometric substrates: methodology for 25 enzyme/substrate pairs / David M. Stresser -- Evaluation of cytochrome P450 inhibition in human liver microsomes / Zhengyin Yan and Gary W. Caldwell -- Identification of CYP mechanism-based inhibitors / Amin A. Nomeir, Jairam Palamanda, and Leonard Favreau --

Detection of DNA adducts by 32P-postlabeling analysis / Naomi Suzuki, Padmaja M. Prabhu, and Shinya Shibutani -- Covalent DNA adduct formation mediated by cytochrome P450 / Marie Stiborová -- Application of in vitro comet assay for genotoxicity testing / Bojana Zegura and Metka Filipic -- Assessing DNA damage using a reporter gene system / Xuming Jia and Wei Xiao -- Improvement of the Ames test using human liver S9 preparation / Atsushi Hakura, Satoshi Suzuki, and Tetsuo Satoh -- Screening for chemical mutagens using the mouse lymphoma assay / Tao Chen and Martha M. Moore -- A high throughput binding assay for HERG / Keith Finlayson and John Sharkey -- In vitro drug metabolism: thiol conjugation / Wei Tang and Randy R. Miller -- In vitro screening assay of the reactivity of acyl glucuronides / Sébastien Bolze.