Computational Approaches in Preclinical Studies on Drug Discovery and Development

Because undesirable pharmacokinetics and toxicity are significant reasons for the failure of drug development in the costly late stage, it has been widely recognized that drug ADMET properties should be considered as early as possible to reduce failure rates in the clinical phase of drug discovery. Concurrently, drug recalls have become increasingly common in recent years, prompting pharmaceutical companies to increase attention toward the safety evaluation of preclinical drugs. In vitro and in vivo drug evaluation techniques are currently more mature in preclinical applications, but these technologies are costly. In recent years, with the rapid development of computer science, in silico technology has been widely used to evaluate the relevant properties of drugs in the preclinical stage and has produced many software programs and in silico models, further promoting the study of ADMET in vitro. In this review, we first introduce the two ADMET prediction categories (molecular modeling and data modeling). Then, we perform a systematic classification and description of the databases and software commonly used for ADMET prediction. We focus on some widely studied ADMT properties as well as PBPK simulation, and we list some applications that are related to the prediction categories and web tools. Finally, we discuss challenges and limitations in the preclinical area and propose some suggestions and prospects for the future.

[1]  Xiaomei Zhuang,et al.  PBPK modeling and simulation in drug research and development , 2016, Acta pharmaceutica Sinica. B.

[2]  O. Fardel,et al.  In Silico Prediction for Intestinal Absorption and Brain Penetration of Chemical Pesticides in Humans , 2017, International journal of environmental research and public health.

[3]  Han van de Waterbeemd,et al.  Simulation models for drug disposition and drug interactions , 2004 .

[4]  A. Ziółkowska,et al.  Disposition of treosulfan and its active monoepoxide in a bone marrow, liver, lungs, brain, and muscle: Studies in a rat model with clinical relevance , 2017, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[5]  F. Główka,et al.  Ocular disposition of treosulfan and its active epoxy-transformers following intravenous administration in rabbits. , 2016, Drug metabolism and pharmacokinetics.

[6]  Sivanesan Dakshanamurthy,et al.  Drug Metabolism in Preclinical Drug Development: A Survey of the Discovery Process, Toxicology, and Computational Tools. , 2017, Current drug metabolism.

[7]  T. Monif,et al.  A Multi-centric Bioequivalence Trial in Ph+ Chronic Myeloid Leukemia Patients to Assess Bioequivalence and Safety Evaluation of Generic Imatinib Mesylate 400 mg Tablets , 2016, Cancer research and treatment : official journal of Korean Cancer Association.

[8]  P. Chalus,et al.  Characterising Drug Release from Immediate-Release Formulations of a Poorly Soluble Compound, Basmisanil, Through Absorption Modelling and Dissolution Testing , 2017, The AAPS Journal.

[9]  Lavanya Souda PadmaRao,et al.  Identification of Novel Antagonists for Rab38 Protein by Homology Modeling and Virtual Screening. , 2016, Combinatorial chemistry & high throughput screening.

[10]  Wolfgang Muster,et al.  Computational toxicology in drug development. , 2008, Drug discovery today.

[11]  H. Qiu,et al.  The pharmacokinetics of dexmedetomidine in patients with obstructive jaundice: A clinical trial , 2018, PloS one.

[12]  R. Greil,et al.  Assessment of Pharmacokinetic Interaction Between Capecitabine and Cetuximab in Metastatic Colorectal Cancer Patients. , 2016, Anticancer research.

[13]  David S. Wishart,et al.  DrugBank 5.0: a major update to the DrugBank database for 2018 , 2017, Nucleic Acids Res..

[14]  Ruifeng Liu,et al.  vNN Web Server for ADMET Predictions , 2017, Front. Pharmacol..

[15]  Y. Zhang,et al.  Prediction of the pharmacokinetics and tissue distribution of levofloxacin in humans based on an extrapolated PBPK model , 2015, European Journal of Drug Metabolism and Pharmacokinetics.

[16]  Dongyang Liu,et al.  Preliminary physiologically based pharmacokinetic modeling of renally cleared drugs in Chinese pregnant women , 2020, Biopharmaceutics & drug disposition.

[17]  Sarita Rajender Potlapally,et al.  Identification of New Lead Molecules Against UBE2NL Enzyme for Cancer Therapy , 2017, Applied Biochemistry and Biotechnology.

[18]  Malcolm Rowland,et al.  Physiologically based pharmacokinetics in Drug Development and Regulatory Science: A workshop report (Georgetown University, Washington, DC, May 29–30, 2002) , 2004, AAPS PharmSci.

[19]  Y. Pan,et al.  Pharmacokinetic and pharmacodynamic integration and modeling of acetylkitasamycin in swine for Clostridium perfringens , 2017, Journal of veterinary pharmacology and therapeutics.

[20]  Jingpu Zhang,et al.  In silico ADME and Toxicity Prediction of Ceftazidime and Its Impurities , 2019, Front. Pharmacol..

[21]  H. J. Olguín,et al.  Pharmacokinetics of sildenafil in children with pulmonary arterial hypertension , 2017, World Journal of Pediatrics.

[22]  I. Haq,et al.  Carboxylate derivatives of tributyltin (IV) complexes as anticancer and antileishmanial agents , 2017, DARU Journal of Pharmaceutical Sciences.

[23]  François Bouzom,et al.  Physiologically based pharmacokinetic (PBPK) modelling tools: how to fit with our needs? , 2012, Biopharmaceutics & drug disposition.

[24]  N. Yamaotsu,et al.  Precise prediction of activators for the human constitutive androstane receptor using structure-based three-dimensional quantitative structure-activity relationship methods. , 2017, Drug metabolism and pharmacokinetics.

[25]  David S. Wishart,et al.  DrugBank: a knowledgebase for drugs, drug actions and drug targets , 2007, Nucleic Acids Res..

[26]  Gordon C K Roberts,et al.  Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition. , 2004, Journal of medicinal chemistry.

[27]  A. Balupuri,et al.  Enzyme Kinetics and Molecular Docking Studies on Cytochrome 2B6, 2C19, 2E1, and 3A4 Activities by Sauchinone , 2018, Molecules.

[28]  Chao Shen,et al.  ADMET Evaluation in Drug Discovery. 19. Reliable Prediction of Human Cytochrome P450 Inhibition Using Artificial Intelligence Approaches , 2019, J. Chem. Inf. Model..

[29]  A. Vermeulen,et al.  PBPK and its Virtual Populations: the Impact of Physiology on Pediatric Pharmacokinetic Predictions of Tramadol , 2018, The AAPS Journal.

[30]  Evan Bolton,et al.  PubChem 2019 update: improved access to chemical data , 2018, Nucleic Acids Res..

[31]  Eric J Martin,et al.  Physiologically Based Pharmacokinetic Modeling in Lead Optimization. 1. Evaluation and Adaptation of GastroPlus To Predict Bioavailability of Medchem Series. , 2018, Molecular pharmaceutics.

[32]  Y. Dong,et al.  Toxicity assessment of the extractables from multi‐layer coextrusion poly ethylene bags exposed to pH=5 solution containing 4% benzyl alcohol and 0.1 M sodium acetate , 2018, Regulatory toxicology and pharmacology : RTP.

[33]  K. Yelekçi,et al.  Identification of potential isoform-selective histone deacetylase inhibitors for cancer therapy: a combined approach of structure-based virtual screening, ADMET prediction and molecular dynamics simulation assay , 2018, Journal of biomolecular structure & dynamics.

[34]  Ravi Rawat,et al.  High-throughput virtual screening approach involving pharmacophore mapping, ADME filtering, molecular docking and MM-GBSA to identify new dual target inhibitors of PfDHODH and PfCytbc1 complex to combat drug resistant malaria , 2020, Journal of biomolecular structure & dynamics.

[35]  L Zhang,et al.  Applications of Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulation During Regulatory Review , 2011, Clinical pharmacology and therapeutics.

[36]  Prabha Garg,et al.  Classification of Breast Cancer Resistant Protein (BCRP) Inhibitors and Non-Inhibitors Using Machine Learning Approaches. , 2015, Combinatorial chemistry & high throughput screening.

[37]  Joseph A Morrone,et al.  Binding Specificity Determines the Cytochrome P450 3A4 Mediated Enantioselective Metabolism of Metconazole. , 2018, The journal of physical chemistry. B.

[38]  C. Sinha,et al.  Spectroscopic characterization, antimicrobial activity, DFT computation and docking studies of sulfonamide Schiff bases , 2017 .

[39]  M. Ceresia,et al.  Pharmacokinetics of intravenous gentamicin in healthy young‐adult compared to aged alpacas , 2018, Journal of veterinary pharmacology and therapeutics.

[40]  T. Eissing,et al.  Physiologically Based Pharmacokinetic Modeling of Renally Cleared Drugs in Pregnant Women , 2017, Clinical Pharmacokinetics.

[41]  Miriam J. Johnson,et al.  In silico (computed) modelling of doses and dosing regimens associated with morphine levels above international legal driving limits , 2018, Palliative medicine.

[42]  Junfeng Liu,et al.  Pharmacokinetics of tilmicosin in healthy pigs and in pigs experimentally infected with Haemophilus parasuis , 2017, Journal of veterinary science.

[43]  Xin He,et al.  Rapid screening the potential mechanism-based inhibitors of CYP3A4 from Tripterygium wilfordi based on computer approaches combined with in vitro bioassay. , 2017, Bioorganic & medicinal chemistry.

[44]  M. Pangalos,et al.  Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework , 2014, Nature Reviews Drug Discovery.

[45]  E. Chow,et al.  Using Physiologically Based Pharmacokinetic (PBPK) Modeling to Evaluate the Impact of Pharmaceutical Excipients on Oral Drug Absorption: Sensitivity Analyses , 2016, The AAPS Journal.

[46]  H. Jacob,et al.  Molecular modeling in the age of clinical genomics, the enterprise of the next generation , 2017, Journal of Molecular Modeling.

[47]  Beow Chin Yiap,et al.  Cytochrome P450 2C9‐natural antiarthritic interactions: Evaluation of inhibition magnitude and prediction from in vitro data , 2018, Biopharmaceutics & drug disposition.

[48]  Geert R Verheyen,et al.  Evaluation of existing (Q)SAR models for skin and eye irritation and corrosion to use for REACH registration. , 2017, Toxicology letters.

[49]  A. Akinmoladun,et al.  Xeronine structure and function: computational comparative mastery of its mystery , 2017, In Silico Pharmacology.

[50]  C. George Priya Doss,et al.  Computational approaches and resources in single amino acid substitutions analysis toward clinical research. , 2014, Advances in protein chemistry and structural biology.

[51]  Leon Aarons,et al.  Forecasting oral absorption across biopharmaceutics classification system classes with physiologically based pharmacokinetic models , 2016, The Journal of pharmacy and pharmacology.

[52]  Y Z Chen,et al.  Recent progresses in the exploration of machine learning methods as in-silico ADME prediction tools. , 2015, Advanced drug delivery reviews.

[53]  S. Singh,et al.  Identification of Dual negative allosteric modulators of Group I mGluR family: A shape based screening, ADME Prediction, Induced Fit Docking and Molecular Dynamics approach against Neurodegenerative Diseases. , 2019, Current topics in medicinal chemistry.

[54]  Wendy A. Warr,et al.  ChEMBL. An interview with John Overington, team leader, chemogenomics at the European Bioinformatics Institute Outstation of the European Molecular Biology Laboratory (EMBL-EBI) , 2009, J. Comput. Aided Mol. Des..

[55]  Sally R. Ellingson,et al.  Ensemble-based docking: From hit discovery to metabolism and toxicity predictions. , 2016, Bioorganic & medicinal chemistry.

[56]  Li Fu,et al.  Systematic Modeling of logD7.4 Based on Ensemble Machine Learning, Group Contribution and Matched Molecular Pair Analysis. , 2019, Journal of chemical information and modeling.

[57]  N. Badjatia,et al.  Lacosamide Pharmacokinetics in a Critically Ill Patient Receiving Continuous Venovenous Hemofiltration , 2018, Pharmacotherapy.

[58]  A. Tripathi,et al.  N1-benzenesulfonyl-2-pyrazoline hybrids in neurological disorders: Syntheses, biological screening and computational studies , 2018, EXCLI journal.

[59]  Hea‐Young Cho,et al.  Gender differences in pharmacokinetics and tissue distribution of 3 perfluoroalkyl and polyfluoroalkyl substances in rats. , 2016, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[60]  Yurie Watanabe,et al.  Investigation of substrate recognition for cytochrome P450 1A2 mediated by water molecules using docking and molecular dynamics simulations. , 2017, Journal of molecular graphics & modelling.

[61]  Andreas Bender,et al.  Computational Prediction of Metabolism: Sites, Products, SAR, P450 Enzyme Dynamics, and Mechanisms , 2012, J. Chem. Inf. Model..

[62]  Tingjun Hou,et al.  ADMET Evaluation in Drug Discovery. 11. PharmacoKinetics Knowledge Base (PKKB): A Comprehensive Database of Pharmacokinetic and Toxic Properties for Drugs , 2012, J. Chem. Inf. Model..

[63]  Richard J. Povinelli,et al.  An ensemble model of QSAR tools for regulatory risk assessment , 2016, Journal of Cheminformatics.

[64]  N. Zhang,et al.  The PK–PD Relationship and Resistance Development of Danofloxacin against Mycoplasma gallisepticum in An In Vivo Infection Model , 2017, Front. Microbiol..

[65]  P. Naidoo,et al.  Population pharmacokinetic modeling of glibenclamide in poorly controlled South African type 2 diabetic subjects , 2016, Clinical pharmacology : advances and applications.

[66]  Cristiana Stefan,et al.  Predicting Escitalopram Exposure to Breastfeeding Infants: Integrating Analytical and In Silico Techniques , 2018, Clinical Pharmacokinetics.

[67]  Philippe Vayer,et al.  Toward in silico structure-based ADMET prediction in drug discovery. , 2012, Drug discovery today.

[68]  Feixiong Cheng,et al.  In silico ADMET prediction: recent advances, current challenges and future trends. , 2013, Current topics in medicinal chemistry.

[69]  G. Camenisch,et al.  In vitro studies and in silico predictions of fluconazole and CYP2C9 genetic polymorphism impact on siponimod metabolism and pharmacokinetics , 2017, European Journal of Clinical Pharmacology.

[70]  Sean Watford,et al.  ToxRefDB version 2.0: Improved utility for predictive and retrospective toxicology analyses. , 2019, Reproductive toxicology.

[71]  Suxia Zhang,et al.  The pharmacokinetics of moxidectin following intravenous and topical administration to swine. , 2018, Journal of veterinary pharmacology and therapeutics.

[72]  S. Modi Computational approaches to the understanding of ADMET properties and problems. , 2003, Drug discovery today.

[73]  N. Galante,et al.  OriginalClinicalScienceçGeneral Longitudinal Pharmacokinetics of Tacrolimus in Elderly Compared With Younger Recipients in the First 6 Months After Renal Transplantation , 2017 .

[74]  J. Crison,et al.  Mathematical Model-Based Accelerated Development of Extended-release Metformin Hydrochloride Tablet Formulation , 2015, AAPS PharmSciTech.

[75]  Danishuddin,et al.  Descriptors and their selection methods in QSAR analysis: paradigm for drug design. , 2016, Drug discovery today.

[76]  Corwin Hansch,et al.  The physicochemical approach to drug design and discovery (QSAR) , 1981 .

[77]  Hongbin Yang,et al.  Corrigendum: In Silico Prediction of Chemical Toxicity for Drug Design Using Machine Learning Methods and Structural Alerts , 2018, Front. Chem..

[78]  B. Keevil,et al.  Bioavailability of Oral Hydrocortisone Corrected for Binding Proteins and Measured by LC-MS/MS Using Serum Cortisol and Salivary Cortisone , 2018, Journal of bioequivalence & bioavailability.

[79]  R. Wu,et al.  Break‐through bleeding in relation to pharmacokinetics of Factor VIII in paediatric patients with severe haemophilia A , 2018, Haemophilia : the official journal of the World Federation of Hemophilia.

[80]  Jie Li,et al.  admetSAR 2.0: web‐service for prediction and optimization of chemical ADMET properties , 2018, Bioinform..

[81]  Douglas E. V. Pires,et al.  pkCSM: Predicting Small-Molecule Pharmacokinetic and Toxicity Properties Using Graph-Based Signatures , 2015, Journal of medicinal chemistry.

[82]  Walter Schmitt,et al.  Whole body physiologically-based pharmacokinetic models: their use in clinical drug development , 2008, Expert opinion on drug metabolism & toxicology.

[83]  A. Rostami-Hodjegan,et al.  Physiologically Based Pharmacokinetics Joined With In Vitro–In Vivo Extrapolation of ADME: A Marriage Under the Arch of Systems Pharmacology , 2012, Clinical pharmacology and therapeutics.

[84]  Hui Gong,et al.  CEBS: a comprehensive annotated database of toxicological data , 2016, Nucleic Acids Res..

[85]  George Papadatos,et al.  The ChEMBL database in 2017 , 2016, Nucleic Acids Res..

[86]  Thomas C. Wiegers,et al.  The Comparative Toxicogenomics Database: update 2019 , 2018, Nucleic Acids Res..

[87]  Stefano Moro,et al.  Pharmaceutical Perspectives of Nonlinear QSAR Strategies , 2010, J. Chem. Inf. Model..

[88]  Kairui Feng,et al.  The Simcyp® Population-based ADME Simulator , 2009 .

[89]  Chaoying Hu,et al.  Single- and Multiple-Dose Pharmacokinetics, Safety and Tolerability of Lurasidone in Healthy Chinese Subjects , 2017, Clinical Drug Investigation.

[90]  V. Masand,et al.  Design of novel amyloid β aggregation inhibitors using QSAR, pharmacophore modeling, molecular docking and ADME prediction , 2018, In Silico Pharmacology.

[91]  Abhijit Mitra,et al.  Prediction of Anti-Alzheimer's Activity of Flavonoids Targeting Acetylcholinesterase in silico. , 2017, Phytochemical analysis : PCA.

[92]  N. Parrott,et al.  Effects of Cytochrome P450 3A4 Inhibitors—Ketoconazole and Erythromycin—on Bitopertin Pharmacokinetics and Comparison with Physiologically Based Modelling Predictions , 2016, Clinical Pharmacokinetics.

[93]  Pamela J Spencer,et al.  Evaluation of TOPKAT, Toxtree, and Derek Nexus in Silico Models for Ocular Irritation and Development of a Knowledge-Based Framework To Improve the Prediction of Severe Irritation. , 2016, Chemical research in toxicology.

[94]  Hongbin Yang,et al.  ADMETopt: A Web Server for ADMET Optimization in Drug Design via Scaffold Hopping , 2018, J. Chem. Inf. Model..

[95]  Gary W Caldwell,et al.  ADME optimization and toxicity assessment in early- and late-phase drug discovery. , 2009, Current topics in medicinal chemistry.

[96]  Olivier Michielin,et al.  SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules , 2017, Scientific Reports.

[97]  Weiliang Zhu,et al.  New technologies in computer-aided drug design: Toward target identification and new chemical entity discovery , 2006, Drug Discovery Today: Technologies.

[98]  Walter Schmitt,et al.  Physiology-based pharmacokinetic modeling: ready to be used. , 2004, Drug discovery today. Technologies.

[99]  Humayun Kabir,et al.  Comparative Studies on Some Metrics for External Validation of QSPR Models , 2012, J. Chem. Inf. Model..

[100]  G. Patlewicz,et al.  An evaluation of the implementation of the Cramer classification scheme in the Toxtree software , 2008, SAR and QSAR in environmental research.

[101]  Divya Shaji Molecular docking studies of human MCT8 protein with soy isoflavones in Allan-Herndon-Dudley syndrome (AHDS) , 2018, Journal of pharmaceutical analysis.

[102]  I. Jung,et al.  Recent advances in physiologically based pharmacokinetic and pharmacodynamic models for anticancer nanomedicines , 2020, Archives of Pharmacal Research.

[103]  M. Nosrati,et al.  Frangulosid as a novel hepatitis B virus DNA polymerase inhibitor: a virtual screening study , 2018, In Silico Pharmacology.

[104]  Jie Shen,et al.  admetSAR: A Comprehensive Source and Free Tool for Assessment of Chemical ADMET Properties , 2012, J. Chem. Inf. Model..

[105]  H. Derendorf,et al.  Dermal pharmacokinetics of pyrazinamide determined by microdialysis sampling in rats. , 2017, International journal of antimicrobial agents.

[106]  L. Geerts,et al.  CON4EI: Evaluation of QSAR models for hazard identification and labelling of eye irritating chemicals. , 2017, Toxicology in vitro : an international journal published in association with BIBRA.

[107]  J. J. Espinosa-Aguirre,et al.  Inhibition of human and rat CYP1A1 enzyme by grapefruit juice compounds. , 2016, Toxicology letters.

[108]  Propofol target-controlled infusion modeling in rabbits: Pharmacokinetic and pharmacodynamic analysis , 2016, Journal of Huazhong University of Science and Technology [Medical Sciences].

[109]  A. Seal,et al.  Identification of a less toxic vinca alkaloid derivative for use as a chemotherapeutic agent, based on in silico structural insights and metabolic interactions with CYP3A4 and CYP3A5 , 2018, Journal of Molecular Modeling.

[110]  P. Bharatam,et al.  Mechanistic insights into the bioactivation of phenacetin to reactive metabolites: A DFT study , 2013 .

[111]  Taisheng Li,et al.  Steady-state pharmacokinetics of tenofovir disoproxil fumarate in human immunodeficiency virus-infected Chinese patients , 2017, Expert review of clinical pharmacology.

[112]  N. H. Nagoor,et al.  In vitro inhibitory mechanisms and molecular docking of 1'-S-1'-acetoxychavicol acetate on human cytochrome P450 enzymes. , 2017, Phytomedicine : international journal of phytotherapy and phytopharmacology.

[113]  Z. Kerem,et al.  In silico and in vitro inhibition of cytochrome P450 3A by synthetic stilbenoids. , 2017, Food chemistry.

[114]  Ren Jun,et al.  In silico approaches and tools for the prediction of drug metabolism and fate: A review , 2019, Comput. Biol. Medicine.

[115]  M. Jamei,et al.  Biopharmaceutic IVIVE-Mechanistic Modeling of Single- and Two-Phase In Vitro Experiments to Obtain Drug-Specific Parameters for Incorporation Into PBPK Models. , 2019, Journal of pharmaceutical sciences.

[116]  Q. Shan,et al.  Pharmacokinetics of enrofloxacin after oral, intramuscular and bath administration in crucian carp (Carassius auratus gibelio). , 2018, Journal of veterinary pharmacology and therapeutics.

[117]  E. Benfenati,et al.  A combination of 3D-QSAR, docking, local-binding energy (LBE) and GRID study of the species differences in the carcinogenicity of benzene derivatives chemicals. , 2008, Journal of molecular graphics & modelling.

[118]  G. Kearns,et al.  Obese Children Require Lower Doses of Pantoprazole Than Nonobese Peers to Achieve Equal Systemic Drug Exposures , 2018, The Journal of pediatrics.

[119]  Ajay Kumar,et al.  Molecular docking studies of 3-bromopyruvate and its derivatives to metabolic regulatory enzymes: Implication in designing of novel anticancer therapeutic strategies , 2017, PloS one.

[120]  Yun Tang,et al.  Network pharmacological mechanisms of Vernonia anthelmintica (L.) in the treatment of vitiligo: Isorhamnetin induction of melanogenesis via up-regulation of melanin-biosynthetic genes , 2017, BMC Systems Biology.

[121]  Hui Zhang,et al.  Applications of Machine Learning Methods in Drug Toxicity Prediction. , 2018, Current topics in medicinal chemistry.

[122]  Hao Sun,et al.  Structure‐based Drug Metabolism Predictions for Drug Design , 2010, Chemical biology & drug design.

[123]  H. van de Waterbeemd,et al.  ADMET in silico modelling: towards prediction paradise? , 2003, Nature reviews. Drug discovery.

[124]  Yeong Shik Kim,et al.  Biaryl scaffold-focused virtual screening for anti-aggregatory and neuroprotective effects in Alzheimer’s disease , 2018, BMC Neuroscience.

[125]  Alexandre Jacob,et al.  In silico platform for xenobiotics ADME-T pharmacological properties modeling and prediction. Part II: The body in a Hilbertian space. , 2009, Drug discovery today.

[126]  S. Hamadi,et al.  Saliva versus Plasma Therapeutic Drug Monitoring of Pregabalin in Jordanian Patients , 2018, Drug Research.

[127]  Zengrui Wu,et al.  Interactions of omeprazole-based analogues with cytochrome P450 2C19: a computational study. , 2016, Molecular bioSystems.

[128]  Emilio Benfenati,et al.  Performance of In Silico Models for Mutagenicity Prediction of Food Contact Materials , 2018, Toxicological sciences : an official journal of the Society of Toxicology.

[129]  Bhupinder Singh,et al.  Exploring and validating physicochemical properties of mangiferin through GastroPlus® software , 2017, Future science OA.

[130]  Santosh Putta,et al.  Shapes of things: computer modeling of molecular shape in drug discovery. , 2007, Current topics in medicinal chemistry.

[131]  Y. Hamada,et al.  Population pharmacokinetics of arbekacin in different infectious disease settings and evaluation of dosing regimens. , 2016, Journal of Infection and Chemotherapy.

[132]  A. Braeuning,et al.  Evaluation and improvement of QSAR predictions of skin sensitization for pesticides , 2018, SAR and QSAR in environmental research.

[133]  Dong-Sheng Cao,et al.  ADMETlab: a platform for systematic ADMET evaluation based on a comprehensively collected ADMET database , 2018, Journal of Cheminformatics.

[134]  Jianfeng Pei,et al.  Deep Learning Based Regression and Multiclass Models for Acute Oral Toxicity Prediction with Automatic Chemical Feature Extraction , 2017, J. Chem. Inf. Model..

[135]  Guixia Liu,et al.  Computational Investigation of Ligand Binding to the Peripheral Site in CYP3A4: Conformational Dynamics and Inhibitor Discovery , 2017, J. Chem. Inf. Model..

[136]  Saeed Alqahtani,et al.  In silico ADME-Tox modeling: progress and prospects , 2017, Expert opinion on drug metabolism & toxicology.

[137]  Dong-Sheng Cao,et al.  Structural Analysis and Identification of Colloidal Aggregators in Drug Discovery , 2019, J. Chem. Inf. Model..

[138]  F. Khan,et al.  3D-QSAR, Docking, ADME/Tox studies on Flavone analogs reveal anticancer activity through Tankyrase inhibition , 2019, Scientific Reports.

[139]  M V Patil,et al.  Evaluation of pharmacokinetic and pharmacodynamic parameters following single dose of sitagliptin in healthy Indian males , 2018, European Journal of Clinical Pharmacology.

[140]  Bowen Jp,et al.  A Perspective on Quantum Mechanics Calculations in ADMET Predictions , 2013 .

[141]  C. Andrade,et al.  In silico prediction of drug metabolism by P450. , 2014, Current drug metabolism.

[142]  Sarah Whalley,et al.  Predictions of Metabolic Drug-Drug Interactions Using Physiologically Based Modelling , 2010, Clinical pharmacokinetics.

[143]  M. Soliman,et al.  Allosteric inhibition induces an open WPD-loop: a new avenue towards glioblastoma therapy , 2018, RSC advances.

[144]  Stephani Joy Y Macalino,et al.  Role of computer-aided drug design in modern drug discovery , 2015, Archives of Pharmacal Research.

[145]  T. Teorell STUDIES ON THE DIFFUSION EFFECT UPON IONIC DISTRIBUTION , 1937, The Journal of general physiology.

[146]  M. Govarthanan,et al.  Ligand-based pharmacophore filtering, atom based 3D-QSAR, virtual screening and ADME studies for the discovery of potential ck2 inhibitors , 2020 .

[147]  A. Beresford,et al.  The emerging importance of predictive ADME simulation in drug discovery. , 2002, Drug discovery today.

[148]  Tania Portolés,et al.  Identification of substances migrating from plastic baby bottles using a combination of low-resolution and high-resolution mass spectrometric analysers coupled to gas and liquid chromatography. , 2015, Journal of mass spectrometry : JMS.

[149]  T. Eissing,et al.  Development of a Whole-Body Physiologically Based Pharmacokinetic Approach to Assess the Pharmacokinetics of Drugs in Elderly Individuals , 2016, Clinical Pharmacokinetics.

[150]  David S. Wishart,et al.  DrugBank: a comprehensive resource for in silico drug discovery and exploration , 2005, Nucleic Acids Res..

[151]  N Parrott,et al.  Physiologically based pharmacokinetic modeling in drug discovery and development: A pharmaceutical industry perspective , 2015, Clinical pharmacology and therapeutics.

[152]  Pantelis Sopasakis,et al.  Collaborative development of predictive toxicology applications , 2010, J. Cheminformatics.

[153]  Tingjun Hou,et al.  ADME evaluation in drug discovery , 2002, Journal of molecular modeling.

[154]  Robert D Clark,et al.  Neighborhood behavior: a useful concept for validation of "molecular diversity" descriptors. , 1996, Journal of medicinal chemistry.

[155]  G. Ilia,et al.  The antiviral activity and cytotoxicity of 15 natural phenolic compounds with previously demonstrated antifungal activity , 2019, Journal of environmental science and health. Part. B, Pesticides, food contaminants, and agricultural wastes.

[156]  Suxia Zhang,et al.  Pharmacokinetic profile of Ceftiofur Hydrochloride Injection in lactating Holstein dairy cows , 2018, Journal of veterinary pharmacology and therapeutics.

[157]  Xin He,et al.  Human cytochrome P450 enzyme inhibition profile of three flavonoids isolated from Psoralea corylifolia: in silico predictions and experimental validation , 2018 .

[158]  M. Elaasser,et al.  New thiobarbituric acid scaffold‐based small molecules: Synthesis, cytotoxicity, 2D‐QSAR, pharmacophore modelling and in‐silico ADME screening , 2019, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[159]  V. Frecer,et al.  Diarylcyclopropane hydroxamic acid inhibitors of histone deacetylase 4 designed by combinatorial approach and QM/MM calculations. , 2018, Journal of molecular graphics & modelling.

[160]  D. Poirier,et al.  Structure-Based Design and Synthesis of New Estrane-Pyridine Derivatives as Cytochrome P450 (CYP) 1B1 Inhibitors. , 2017, ACS medicinal chemistry letters.

[161]  Chris Oostenbrink,et al.  Catalytic site prediction and virtual screening of cytochrome P450 2D6 substrates by consideration of water and rescoring in automated docking. , 2006, Journal of medicinal chemistry.

[162]  I. Piedade,et al.  In silico prediction of , 2014 .

[163]  Tingjun Hou,et al.  ADMET evaluation in drug discovery. 20. Prediction of breast cancer resistance protein inhibition through machine learning , 2020, Journal of Cheminformatics.

[164]  Y. Huang,et al.  Pharmacokinetic/Pharmacodynamic Modeling of Tulathromycin against Pasteurella multocida in a Porcine Tissue Cage Model , 2017, Front. Pharmacol..

[165]  Runling Wang,et al.  Synthesis, bioactivity, 3D-QSAR studies of novel dibenzofuran derivatives as PTP-MEG2 inhibitors , 2017, Oncotarget.

[166]  Suxia Zhang,et al.  Evaluation of pharmacokinetic properties of vitacoxib in fasted and fed horses , 2018, Journal of veterinary pharmacology and therapeutics.

[167]  Weihua Li,et al.  In Silico Prediction of Chemical Toxicity for Drug Design Using Machine Learning Methods and Structural Alerts , 2018, Front. Chem..

[168]  Stefan Willmann,et al.  A generic whole body physiologically based pharmacokinetic model for therapeutic proteins in PK-Sim , 2017, Journal of Pharmacokinetics and Pharmacodynamics.

[169]  M. Takač,et al.  Evaluation of phenylethylamine type entactogens and their metabolites relevant to ecotoxicology – a QSAR study , 2019, Acta pharmaceutica.

[170]  A. S. A. Majid,et al.  Designing the angiogenic inhibitor for brain tumor via disruption of VEGF and IL17A expression. , 2016, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[171]  Stewart B Kirton,et al.  In silico methods for predicting ligand binding determinants of cytochromes P450. , 2004, Current topics in medicinal chemistry.

[172]  M. Taroncher,et al.  In silico and in vitro prediction of the toxicological effects of individual and combined mycotoxins. , 2018, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[173]  B. Goh,et al.  Phenotyping of UGT1A1 Activity Using Raltegravir Predicts Pharmacokinetics and Toxicity of Irinotecan in FOLFIRI , 2016, PloS one.

[174]  G. Bifulco,et al.  Discovery of 3-hydroxy-3-pyrrolin-2-one-based mPGES-1 inhibitors using a multi-step virtual screening protocol. , 2018, MedChemComm.

[175]  Qingping Shi,et al.  Pharmacokinetic/Pharmacodynamic Analysis of Meropenem for the Treatment of Nosocomial Pneumonia in Intracerebral Hemorrhage Patients by Monte Carlo Simulation , 2017, The Annals of pharmacotherapy.

[176]  T. van Gelder,et al.  Highly variable absorption of clavulanic acid during the day: a population pharmacokinetic analysis , 2018, The Journal of antimicrobial chemotherapy.

[177]  Igor V. Tetko,et al.  Applicability Domains for Classification Problems: Benchmarking of Distance to Models for Ames Mutagenicity Set , 2010, J. Chem. Inf. Model..

[178]  Y. Tao,et al.  The Epidemiologic and Pharmacodynamic Cutoff Values of Tilmicosin against Haemophilus parasuis , 2016, Front. Microbiol..

[179]  John P. Overington ChEMBL. An interview with John Overington, team leader, chemogenomics at the European Bioinformatics Institute Outstation of the European Molecular Biology Laboratory (EMBL-EBI). Interview by Wendy A. Warr. , 2009, Journal of computer-aided molecular design.

[180]  Cheng Luo,et al.  In silico ADME/T modelling for rational drug design , 2015, Quarterly Reviews of Biophysics.

[181]  Christoph Helma,et al.  Lazy structure-activity relationships (lazar) for the prediction of rodent carcinogenicity and Salmonella mutagenicity , 2006, Molecular Diversity.

[182]  Ola Spjuth,et al.  A confidence predictor for logD using conformal regression and a support-vector machine , 2018, Journal of Cheminformatics.

[183]  E. Patterson,et al.  Intravenous Topiramate: Pharmacokinetics in Dogs with Naturally Occurring Epilepsy , 2016, Front. Vet. Sci..

[184]  Adriano D Andricopulo,et al.  ADMET modeling approaches in drug discovery. , 2019, Drug discovery today.

[185]  J. Pedraz,et al.  Pharmacokinetics of Benznidazole in Healthy Volunteers and Implications in Future Clinical Trials , 2017, Antimicrobial Agents and Chemotherapy.

[186]  Kailas S. Khomane,et al.  Identification of leads for antiproliferative activity on MDA-MB-435 human breast cancer cells through pharmacophore and CYP1A1-mediated metabolism. , 2016, European journal of medicinal chemistry.

[187]  Min Li,et al.  Physiologically Based Pharmacokinetic (PBPK) Modeling of Pharmaceutical Nanoparticles , 2016, The AAPS Journal.

[188]  R. Davey,et al.  Phenotypic Prioritization of Diphyllin Derivatives That Block Filoviral Cell Entry by Vacuolar (H+)‐ATPase Inhibition , 2018, ChemMedChem.

[189]  T. Teorell Studies on the "Diffusion Effect" upon Ionic Distribution. Some Theoretical Considerations. , 1935, Proceedings of the National Academy of Sciences of the United States of America.

[190]  C. Simoneau,et al.  Identification and quantification of the migration of chemicals from plastic baby bottles used as substitutes for polycarbonate , 2011, Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment.

[191]  Alfonso Lampen,et al.  Use of in silico models for prioritization of heat-induced food contaminants in mutagenicity and carcinogenicity testing , 2017, Archives of Toxicology.

[192]  Z. Kerem,et al.  Inhibition of cytochrome P450 3A by acetoxylated analogues of resveratrol in in vitro and in silico models , 2016, Scientific Reports.

[193]  P. Pennell,et al.  Lamotrigine pharmacokinetics following oral and stable‐labeled intravenous administration in young and elderly adult epilepsy patients: Effect of age , 2018, Epilepsia.

[194]  Sheng Tian,et al.  ADME evaluation in drug discovery. 9. Prediction of oral bioavailability in humans based on molecular properties and structural fingerprints. , 2011, Molecular pharmaceutics.

[195]  Daxesh P. Patel,et al.  A multiparametric organ toxicity predictor for drug discovery , 2019, Toxicology mechanisms and methods.

[196]  H. Zhai,et al.  Investigations of FAK inhibitors: a combination of 3D-QSAR, docking, and molecular dynamics simulations studies , 2018, Journal of biomolecular structure & dynamics.

[197]  Min Xu,et al.  Preclinical pharmacokinetics of MHAA4549A, a human monoclonal antibody to influenza A virus, and the prediction of its efficacious clinical dose for the treatment of patients hospitalized with influenza A , 2016, mAbs.

[198]  B. Walther,et al.  Pharmacokinetic predictions in children by using the physiologically based pharmacokinetic modelling , 2008, Fundamental & clinical pharmacology.

[199]  José L Medina-Franco,et al.  Systematic characterization of structure-activity relationships and ADMET compliance: a case study. , 2013, Drug discovery today.

[200]  L. Blank,et al.  Model-based contextualization of in vitro toxicity data quantitatively predicts in vivo drug response in patients , 2016, Archives of Toxicology.

[201]  S. Singh,et al.  Shape and pharmacophore-based virtual screening to identify potential cytochrome P450 sterol 14α-demethylase inhibitors , 2013, Journal of receptor and signal transduction research.

[202]  T. Grabowski,et al.  Determination of cloxacillin residues in dairy cows after intramammary administration , 2017, Journal of veterinary pharmacology and therapeutics.

[203]  Jerzy Leszczynski,et al.  Recent Advances of Computational Modeling for Predicting Drug Metabolism: A Perspective. , 2017, Current drug metabolism.

[204]  John C Dearden,et al.  In silico prediction of ADMET properties: how far have we come? , 2007, Expert opinion on drug metabolism & toxicology.

[205]  Mikiko Nakamura,et al.  Physiologically Based Absorption Modeling to Explore the Impact of Food and Gastric pH Changes on the Pharmacokinetics of Alectinib , 2016, The AAPS Journal.

[206]  F. Yang,et al.  Pharmacokinetics of cefquinome in crucian carp (Carassius auratus gibelio) after oral, intramuscular, intraperitoneal, and bath administration , 2018, Journal of veterinary pharmacology and therapeutics.

[207]  Christel A. S. Bergström,et al.  Does the Intake of Ethanol Affect Oral Absorption of Poorly Soluble Drugs? , 2019, Journal of pharmaceutical sciences.

[208]  L. Görlitz,et al.  Development of Physiologically Based Organ Models to Evaluate the Pharmacokinetics of Drugs in the Testes and the Thyroid Gland , 2017, CPT: pharmacometrics & systems pharmacology.

[209]  M. Duarte,et al.  Fluconazole induces genotoxicity in cultured human peripheral blood mononuclear cells via immunomodulation of TNF-α, IL-6, and IL-10: new challenges for safe therapeutic regimens , 2019, Immunopharmacology and immunotoxicology.

[210]  Fen Yang,et al.  Prediction of a Therapeutic Dose for Buagafuran, a Potent Anxiolytic Agent by Physiologically Based Pharmacokinetic/Pharmacodynamic Modeling Starting from Pharmacokinetics in Rats and Human , 2017, Front. Pharmacol..

[211]  Dhaval B. Patel,et al.  Synthesis of novel quinoline‐thiosemicarbazide hybrids and evaluation of their biological activities, molecular docking, molecular dynamics, pharmacophore model studies, and ADME‐Tox properties , 2020 .

[212]  T Lavé,et al.  Challenges and opportunities with modelling and simulation in drug discovery and drug development , 2007, Xenobiotica; the fate of foreign compounds in biological systems.

[213]  Yongjun Hu,et al.  In Silico Prediction of the Absorption and Disposition of Cefadroxil in Humans using an Intestinal Permeability Method Scaled from Humanized PepT1 Mice , 2018, Drug Metabolism and Disposition.

[214]  R. Kaliszan,et al.  Blood-brain barrier permeability mechanisms in view of quantitative structure-activity relationships (QSAR). , 2015, Journal of pharmaceutical and biomedical analysis.

[215]  David W. Ritchie,et al.  Using Consensus-Shape Clustering To Identify Promiscuous Ligands and Protein Targets and To Choose the Right Query for Shape-Based Virtual Screening , 2011, J. Chem. Inf. Model..

[216]  Ivan Nestorov,et al.  Whole Body Pharmacokinetic Models , 2003, Clinical pharmacokinetics.

[217]  Cédric Merlot,et al.  Computational toxicology--a tool for early safety evaluation. , 2010, Drug discovery today.

[218]  Kairui Feng,et al.  The Simcyp population-based ADME simulator. , 2009, Expert opinion on drug metabolism & toxicology.

[219]  Hafiza Amna Younus,et al.  Sulfonyl hydrazones derived from 3-formylchromone as non-selective inhibitors of MAO-A and MAO-B: Synthesis, molecular modelling and in-silico ADME evaluation. , 2017, Bioorganic chemistry.

[220]  Ann M Richard,et al.  Distributed structure-searchable toxicity (DSSTox) public database network: a proposal. , 2002, Mutation research.

[221]  Junmei Wang,et al.  Chapter 5 Recent Advances on in silico ADME Modeling , 2009 .

[222]  N. Savithramma,et al.  Isolation, characterization and in silico docking studies of synergistic estrogen receptor a anticancer polyphenols from Syzygium alternifolium (Wt.) Walp. , 2017, Journal of intercultural ethnopharmacology.

[223]  Antony J. Williams,et al.  The CompTox Chemistry Dashboard: a community data resource for environmental chemistry , 2017, Journal of Cheminformatics.

[224]  Jamshid Tabeshpour,et al.  Computer-aided Drug Design and Drug Pharmacokinetic Prediction: A Mini-review. , 2018, Current pharmaceutical design.

[225]  V. Ostafe,et al.  Computational Assessment of Pharmacokinetics and Biological Effects of Some Anabolic and Androgen Steroids , 2018, Pharmaceutical Research.

[226]  Yanli Wang,et al.  Structure-Based Virtual Screening for Drug Discovery: a Problem-Centric Review , 2012, The AAPS Journal.

[227]  Micha Rautenberg,et al.  lazar: a modular predictive toxicology framework , 2013, Front. Pharmacol..

[228]  Tahmeena Khan,et al.  Exploring the novel heterocyclic derivatives as lead molecules for design and development of potent anticancer agents. , 2018, Journal of molecular graphics & modelling.

[229]  Vinícius Gonçalves Maltarollo,et al.  Applying machine learning techniques for ADME-Tox prediction: a review , 2015, Expert opinion on drug metabolism & toxicology.

[230]  P. Bharatam,et al.  Shape-based virtual screening, docking, and molecular dynamics simulations to identify Mtb-ASADH inhibitors , 2015, Journal of biomolecular structure & dynamics.

[231]  C. Jacob,et al.  Cytoprotective and antioxidant properties of organic selenides for the myelin-forming cells, oligodendrocytes. , 2018, Bioorganic chemistry.

[232]  Roy J. Vaz,et al.  Amelioration of mechanism-based inactivation of CYP3A4 by a H-PGDS inhibitor. , 2018, Bioorganic & medicinal chemistry letters.

[233]  Huidong Yu,et al.  Recent developments of in silico predictions of oral bioavailability. , 2011, Combinatorial chemistry & high throughput screening.

[234]  W. Ding,et al.  Synthesis and Acaricidal Activities of Scopoletin Phenolic Ether Derivatives: QSAR, Molecular Docking Study and in Silico ADME Predictions , 2018, Molecules.

[235]  M. Ibarra,et al.  Integration of in vitro biorelevant dissolution and in silico PBPK model of carvedilol to predict bioequivalence of oral drug products , 2018, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[236]  Jing-Hung Wang,et al.  Utilizing native fluorescence imaging, modeling and simulation to examine pharmacokinetics and therapeutic regimen of a novel anticancer prodrug , 2016, BMC Cancer.

[237]  S. Singh,et al.  In vivo in silico pharmacokinetic simulation studies of carvedilol-loaded nanocapsules using GastroPlus. , 2016, Therapeutic delivery.

[238]  Keun Woo Lee,et al.  Pharmacophore modeling, virtual screening, molecular docking studies and density functional theory approaches to identify novel ketohexokinase (KHK) inhibitors , 2015, Biosyst..

[239]  S. Verma,et al.  Structure based comprehensive modelling, spatial fingerprints mapping and ADME screening of curcumin analogues as novel ALR2 inhibitors , 2017, PloS one.

[240]  S. Hosek,et al.  Short Communication: Bioequivalence of Tenofovir and Emtricitabine After Coencapsulation with the Proteus Ingestible Sensor. , 2018, AIDS research and human retroviruses.

[241]  A. Covaci,et al.  Investigation of the genotoxicity of substances migrating from polycarbonate replacement baby bottles to identify chemicals of high concern. , 2016, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[242]  Zhancheng Gao,et al.  Continuous hypoxia reduces the concentration of streptomycin in the blood , 2018, BMC Infectious Diseases.

[243]  Dan Li,et al.  ADMET Evaluation in Drug Discovery. 16. Predicting hERG Blockers by Combining Multiple Pharmacophores and Machine Learning Approaches. , 2016, Molecular pharmaceutics.

[244]  Shashank Jain,et al.  Transdermal iontophoretic delivery of tacrine hydrochloride: Correlation between in vitro permeation and in vivo performance in rats. , 2016, International journal of pharmaceutics.

[245]  B. Dasgupta,et al.  Plasma and brain pharmacokinetics of letrozole and drug interaction studies with temozolomide in NOD-scid gamma mice and sprague dawley rats , 2018, Cancer Chemotherapy and Pharmacology.

[246]  H. Soeorg,et al.  Pharmacokinetics of Penicillin G in Preterm and Term Neonates , 2018, Antimicrobial Agents and Chemotherapy.

[247]  Ruchi Malik,et al.  Pharmacophore modeling, 3D-QSAR, and in silico ADME prediction of N-pyridyl and pyrimidine benzamides as potent antiepileptic agents , 2017, Journal of receptor and signal transduction research.

[248]  M. D. de Groot,et al.  Designing better drugs: predicting cytochrome P450 metabolism. , 2006, Drug discovery today.

[249]  David S Wishart,et al.  Improving early drug discovery through ADME modelling: an overview. , 2007, Drugs in R&D.

[250]  M. Harmer The classification of breast cancer. , 1970, Indian journal of cancer.

[251]  I. Kola,et al.  Can the pharmaceutical industry reduce attrition rates? , 2004, Nature Reviews Drug Discovery.

[252]  Bi-kui Zhang,et al.  Bioequivalence of two quetiapine extended release tablets in Chinese healthy volunteers under fasting and fed conditions and effects of food on pharmacokinetic profiles , 2018, Drug design, development and therapy.

[253]  H. Chuman,et al.  Molecular dynamics and density functional studies on the metabolic selectivity of antipsychotic thioridazine by cytochrome P450 2D6: Connection with crystallographic and metabolic results. , 2015, Bioorganic & medicinal chemistry.

[254]  Hui Liu,et al.  Comparative analyses of structural features and scaffold diversity for purchasable compound libraries , 2017, Journal of Cheminformatics.

[255]  Jian Sun,et al.  Pharmacokinetic and pharmacodynamic modeling of sarafloxacin against avian pathogenic Escherichia coli in Muscovy ducks , 2016, BMC Veterinary Research.

[256]  R. Holt,et al.  Pharmacokinetics of glycerol phenylbutyrate in pediatric patients 2 months to 2 years of age with urea cycle disorders. , 2018, Molecular genetics and metabolism.

[257]  Diansong Zhou,et al.  COMPARISON OF METHODS FOR THE PREDICTION OF THE METABOLIC SITES FOR CYP3A4-MEDIATED METABOLIC REACTIONS , 2006, Drug Metabolism and Disposition.

[258]  Stefan S De Buck,et al.  Physiologically based approaches towards the prediction of pharmacokinetics: in vitro–in vivo extrapolation , 2007, Expert opinion on drug metabolism & toxicology.

[259]  Dominique Tytgat,et al.  Physiologically based pharmacokinetics (PBPK) , 2009, Drug metabolism reviews.

[260]  Lina Ding,et al.  Flavokawain A inhibits Cytochrome P450 in in vitro metabolic and inhibitory investigations. , 2016, Journal of ethnopharmacology.

[261]  A. Lampen,et al.  In silico genotoxicity and carcinogenicity prediction for food-relevant secondary plant metabolites. , 2018, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association.

[262]  Awanish Kumar,et al.  Docking and ADMET prediction of few GSK-3 inhibitors divulges 6-bromoindirubin-3-oxime as a potential inhibitor. , 2016, Journal of molecular graphics & modelling.

[263]  J. Gao,et al.  Bioequivalence Comparison of Pediatric Dasatinib Formulations and Elucidation of Absorption Mechanisms Through Integrated PBPK Modeling. , 2019, Journal of pharmaceutical sciences.

[264]  S. Muresan,et al.  Chemical predictive modelling to improve compound quality , 2013, Nature Reviews Drug Discovery.

[265]  Hongshi Yu,et al.  ADME-Tox in drug discovery: integration of experimental and computational technologies. , 2003, Drug discovery today.

[266]  Yao Chen,et al.  Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening. , 2015, Bioorganic & medicinal chemistry letters.

[267]  Ulrike Schmidt,et al.  SuperToxic: a comprehensive database of toxic compounds , 2008, Nucleic Acids Res..

[268]  Xiaohui Fan,et al.  Why QSAR fails: an empirical evaluation using conventional computational approach. , 2011, Molecular pharmaceutics.

[269]  K. Saravanan,et al.  Design, 3D QSAR modeling and docking of TGF-β type I inhibitors to target cancer , 2018, Comput. Biol. Chem..

[270]  David S. Wishart,et al.  DrugBank 4.0: shedding new light on drug metabolism , 2013, Nucleic Acids Res..

[271]  Robert P. Sheridan,et al.  Similarity to Molecules in the Training Set Is a Good Discriminator for Prediction Accuracy in QSAR , 2004, J. Chem. Inf. Model..

[272]  B. Simões,et al.  Use of an Oral Busulfan Test Dose in Patients Undergoing Hematopoietic Stem Cell Transplantation Treated With or Without Fludarabine , 2016, Journal of clinical pharmacology.

[273]  Keli Han,et al.  Recent density functional theory model calculations of drug metabolism by cytochrome P450 , 2012 .

[274]  Helena Carla Castro,et al.  Assessment of predictivity of volatile organic compounds carcinogenicity and mutagenicity by freeware in silico models , 2017, Regulatory toxicology and pharmacology : RTP.

[275]  D. Muller,et al.  Pharmacokinetics of Escalating Doses of Oral Psilocybin in Healthy Adults , 2017, Clinical Pharmacokinetics.

[276]  Mahmud Tareq Hassan Khan,et al.  Predictions of the ADMET properties of candidate drug molecules utilizing different QSAR/QSPR modelling approaches. , 2010, Current drug metabolism.

[277]  J. Mullen,et al.  Clinical Bioavailability of the Novel BACE1 Inhibitor Lanabecestat (AZD3293): Assessment of Tablet Formulations Versus an Oral Solution and the Impact of Gastric pH on Pharmacokinetics , 2018, Clinical pharmacology in drug development.

[278]  Sarita Rajender Potlapally,et al.  Targeting the ubiquitin-conjugating enzyme E2D4 for cancer drug discovery–a structure-based approach , 2017, Journal of chemical biology.

[279]  M. Shahlaei,et al.  Exploring the interaction between epidermal growth factor receptor tyrosine kinase and some of the synthesized inhibitors using combination of in-silico and in-vitro cytotoxicity methods , 2018, Research in pharmaceutical sciences.

[280]  T. Arafat,et al.  Saliva versus Plasma Bioequivalence of Valsartan/Hydrochlorothiazide in Humans: Validation of Classes II and IV Drugs of the Salivary Excretion Classification System , 2017, Drug Research.

[281]  A. Wen,et al.  Pharmacokinetic study of single- and multiple-dosing with metolazone tablets in healthy Chinese population , 2017, BMC Pharmacology and Toxicology.

[282]  L. Chinn,et al.  In Vitro, in Silico, and in Vivo Assessments of Intestinal Precipitation and Its Impact on Bioavailability of a BCS Class 2 Basic Compound. , 2018, Molecular pharmaceutics.

[283]  Jie Shen,et al.  Comparison of Cramer classification between Toxtree, the OECD QSAR Toolbox and expert judgment. , 2015, Regulatory toxicology and pharmacology : RTP.

[284]  D. Poirier,et al.  Targeting cytochrome P450 (CYP) 1B1 with steroid derivatives. , 2016, Bioorganic & medicinal chemistry letters.

[285]  R. Guha The ups and downs of structure-activity landscapes. , 2011, Methods in molecular biology.

[286]  M. Shaik,et al.  Population pharmacokinetics of gliclazide in normal and diabetic rabbits , 2018, Biopharmaceutics & drug disposition.

[287]  Fumiyoshi Yamashita,et al.  In silico approaches for predicting ADME properties of drugs. , 2004, Drug metabolism and pharmacokinetics.

[288]  S. A. Mesbah-Namin,et al.  The effects of cinnamaldehyde and eugenol on human adipose-derived mesenchymal stem cells viability, growth and differentiation: a cheminformatics and in vitro study , 2016, Avicenna journal of phytomedicine.

[289]  Jing Lin,et al.  The role of absorption, distribution, metabolism, excretion and toxicity in drug discovery. , 2003, Current topics in medicinal chemistry.

[290]  Z. Zeng,et al.  Comparative pharmacokinetics of diaveridine in pigs and chickens following single intravenous and oral administration , 2017, Journal of veterinary pharmacology and therapeutics.

[291]  Junmei Wang,et al.  An insight into paracetamol and its metabolites using molecular docking and molecular dynamics simulation , 2018, Journal of Molecular Modeling.

[292]  A. Covaci,et al.  Development and application of a non-targeted extraction method for the analysis of migrating compounds from plastic baby bottles by GC-MS , 2014, Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment.

[293]  Philippe Manivet,et al.  In silico platform for xenobiotics ADME-T pharmacological properties modeling and prediction. Part I: Beyond the reduction of animal model use. , 2009, Drug discovery today.

[294]  Malcolm Rowland,et al.  Physiologically-based pharmacokinetics in drug development and regulatory science. , 2011, Annual review of pharmacology and toxicology.

[295]  W. Haefeli,et al.  A physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) model of the histone deacetylase (HDAC) inhibitor vorinostat for pediatric and adult patients and its application for dose specification , 2017, Cancer Chemotherapy and Pharmacology.

[296]  Martin Karplus,et al.  Catalysis and specificity in enzymes: a study of triosephosphate isomerase and comparison with methyl glyoxal synthase. , 2003, Advances in protein chemistry.