High throughput P450 inhibition screens in early drug discovery (Q36294100)

13 August 2017

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title

High throughput P450 inhibition screens in early drug discovery (English)

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13 August 2017

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Gregor Zlokarnik

1

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PubMed ID

16243264

13 August 2017

Peter D J Grootenhuis

series ordinal

2

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PubMed ID

16243264

13 August 2017

John B Watson

series ordinal

3

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13 August 2017

1 November 2005

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13 August 2017

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13 August 2017

10

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13 August 2017

1443-1450

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13 August 2017

21

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The role of absorption, distribution, metabolism, excretion and toxicity in drug discovery

13 August 2017

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Metabolic screening in vitro: metabolic stability, CYP inhibition and induction

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Improvement of "hit-to-lead" optimization by integration of in vitro HTS experimental models for early determination of pharmacokinetic properties

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

The conduct of in vitro and in vivo drug-drug interaction studies: a Pharmaceutical Research and Manufacturers of America (PhRMA) perspective.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Cimetidine-drug interactions

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Clinical pharmacokinetics of mibefradil

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Development of a generalized, quantitative physicochemical model of CYP3A4 inhibition for use in early drug discovery

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Steric factors in the inhibitory interaction of imidazoles with microsomal enzymes

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Mechanism-based inactivation of human cytochrome P450 1A2 by furafylline: detection of a 1:1 adduct to protein and evidence for the formation of a novel imidazomethide intermediate

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Inhibition and induction of cytochrome P450 and the clinical implications

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Examination of 209 drugs for inhibition of cytochrome P450 2C8

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Summary of information on human CYP enzymes: human P450 metabolism data

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Introductory remarks on human CYPs

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Challenges and solutions to ultra-high-throughput screening assay miniaturization: submicroliter fluid handling

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Miniaturized HTS technologies - uHTS.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Mainstreaming microfluidics: diffusing microfluidics technology in the marketplace

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Current application of mass spectrometry to combinatorial chemistry

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Recent advances in use of LC/MS/MS for quantitative high-throughput bioanalytical support of drug discovery

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Optimization of a higher throughput microsomal stability screening assay for profiling drug discovery candidates.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

High-throughput screening for stability and inhibitory activity of compounds toward cytochrome P450-mediated metabolism

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Cytochrome P450 inhibition using recombinant proteins and mass spectrometry/multiple reaction monitoring technology in a cassette incubation

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Measurement of liver microsomal cytochrome p450 (CYP2D6) activity using [O-methyl-14C]dextromethorphan

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Fully automated analysis of activities catalysed by the major human liver cytochrome P450 (CYP) enzymes: assessment of human CYP inhibition potential

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

The potential for CYP2D6 inhibition screening using a novel scintillation proximity assay-based approach

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

In vitro assessment of human cytochrome P450.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Fluorometric high-throughput screening for inhibitors of cytochrome P450

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Design and synthesis of a new fluorescent probe for cytochrome P450 3A4 (CYP 3A4)

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Highly miniaturized formats for in vitro drug metabolism assays using vivid fluorescent substrates and recombinant human cytochrome P450 enzymes

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

In vitro drug interactions of cytochrome p450: an evaluation of fluorogenic to conventional substrates

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

In silico methods for predicting ligand binding determinants of cytochromes P450.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Cytochrome p450 in silico: an integrative modeling approach.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Generation and validation of rapid computational filters for cyp2d6 and cyp3a4.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

A neural network based virtual screening of cytochrome P450 3A4 inhibitors.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Greater than the sum of its parts: combining models for useful ADMET prediction

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Kohonen maps for prediction of binding to human cytochrome P450 3A4.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Crystal structures of human cytochrome P450 3A4 bound to metyrapone and progesterone

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

The structure of human microsomal cytochrome P450 3A4 determined by X-ray crystallography to 2.05-A resolution

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Crystal structure of human cytochrome P450 2C9 with bound warfarin

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Prediction of binding modes for ligands in the cytochromes P450 and other heme-containing proteins.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

CYP3A4 drug interactions: correlation of 10 in vitro probe substrates

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

In vitro and in vivo drug interactions involving human CYP3A.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Assessment of drug-drug interactions: concepts and approaches

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Microsomal protein concentration modifies the apparent inhibitory potency of CYP3A inhibitors

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Activation of CYP3A4: evidence for the simultaneous binding of two substrates in a cytochrome P450 active site.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

CO binding kinetics of human cytochrome P450 3A4. Specific interaction of substrates with kinetically distinguishable conformers.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Clinically significant drug interactions with cyclosporin. An update

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Prediction of pharmacokinetic properties using experimental approaches during early drug discovery

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Database analyses for the prediction of in vivo drug-drug interactions from in vitro data

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

In vitro approaches to predicting drug interactions in vivo.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Drug Metabolism and Drug Interactions: Application and Clinical Value of In Vitro Models

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs.

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

Predictive ADMET studies, the challenges and the opportunities

1 reference

https://api.crossref.org/works/10.1016%2FS1359-6446%2805%2903580-4

7 January 2021

10.1016/S1359-6446(05)03580-4

Identifiers

DOI

1 reference

13 August 2017

1 reference

PubMed ID

16243264