-
1
-
-
0034002261
-
Role of the development scientist in compound lead selection and optimization
-
A key milestone that illuminates the contributions that development experience can make to discovery, to improve candidate readiness for development
-
Venkatesh S., Lipper R.A. Role of the development scientist in compound lead selection and optimization. J. Pharm. Sci. 89:2000;145-154 A key milestone that illuminates the contributions that development experience can make to discovery, to improve candidate readiness for development.
-
(2000)
J. Pharm. Sci.
, vol.89
, pp. 145-154
-
-
Venkatesh, S.1
Lipper, R.A.2
-
2
-
-
0036372804
-
High-throughput screening - brain versus brawn
-
An excellent article on issues and challenges facing today's drug discovery
-
Smith D.A. High-throughput screening - brain versus brawn. Ernst Schering Research Foundation Workshop. 37:2002;203-212 An excellent article on issues and challenges facing today's drug discovery.
-
(2002)
Ernst Schering Research Foundation Workshop
, vol.37
, pp. 203-212
-
-
Smith, D.A.1
-
3
-
-
0035150465
-
High throughput physicochemical profiling for drug discovery
-
Review of current high-throughput profiling assays for physicochemical properties
-
Kerns E.H. High throughput physicochemical profiling for drug discovery. J. Pharm. Sci. 90:2001;1838-1858 Review of current high-throughput profiling assays for physicochemical properties.
-
(2001)
J. Pharm. Sci.
, vol.90
, pp. 1838-1858
-
-
Kerns, E.H.1
-
4
-
-
0002041834
-
Multivariate pharmaceutical profiling for drug discovery
-
Kerns E.H., Di L. Multivariate pharmaceutical profiling for drug discovery. Curr. Topics Med. Chem. 2:2002;87-98.
-
(2002)
Curr. Topics Med. Chem.
, vol.2
, pp. 87-98
-
-
Kerns, E.H.1
Di, L.2
-
5
-
-
0035523337
-
Metabolism profiling and cytochrome P450 inhibition & induction in drug discovery
-
A thorough summary of current strategies in pharmacokinetics, toxicokinetics, drug metabolism, and drug-drug interaction for profiling drug discovery candidates
-
Yan Z., Caldwell G.W. Metabolism profiling and cytochrome P450 inhibition & induction in drug discovery. Curr. Topics Med. Chem. 1:2001;403-425 A thorough summary of current strategies in pharmacokinetics, toxicokinetics, drug metabolism, and drug-drug interaction for profiling drug discovery candidates.
-
(2001)
Curr. Topics Med. Chem.
, vol.1
, pp. 403-425
-
-
Yan, Z.1
Caldwell, G.W.2
-
6
-
-
0035415865
-
Screening of drug candidates for their drug-drug interaction potential
-
Key insights on the motivation, procedures and application of drug-drug interaction monitoring in drug discovery
-
Rodrigues A.D., Lin J.H. Screening of drug candidates for their drug-drug interaction potential. Curr. Opin. Chem. Biol. 5:2001;396-401 Key insights on the motivation, procedures and application of drug-drug interaction monitoring in drug discovery.
-
(2001)
Curr. Opin. Chem. Biol.
, vol.5
, pp. 396-401
-
-
Rodrigues, A.D.1
Lin, J.H.2
-
7
-
-
0035953319
-
Property-based design: Optimization of drug absorption and pharmacokinetics
-
The authors introduce the concept of property-based design and provide a broad-ranging discussions on designing drugs with optimal drug-like properties
-
van de Waterbeemd H., Smith D.A., Beaumont K., Walker D.K. Property-based design: optimization of drug absorption and pharmacokinetics. J. Med. Chem. 44:2001;1313-1333 The authors introduce the concept of property-based design and provide a broad-ranging discussions on designing drugs with optimal drug-like properties.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 1313-1333
-
-
Van de Waterbeemd, H.1
Smith, D.A.2
Beaumont, K.3
Walker, D.K.4
-
8
-
-
0037061628
-
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening
-
McGovern S.L., Caselli E., Grigorieff N., Shoichet B.K. A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening. J. Med. Chem. 45:2002;1712-1722.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 1712-1722
-
-
McGovern, S.L.1
Caselli, E.2
Grigorieff, N.3
Shoichet, B.K.4
-
9
-
-
0034461768
-
Drug-like properties and the causes of poor solubility and poor permeability
-
Outstanding article on the correlation of lead-generation strategies (HTS and rational design) with their effects on the solubility and permeability of discovery candidates
-
Lipinski C.A. Drug-like properties and the causes of poor solubility and poor permeability. J. Pharm. Tox. Methods. 44:2000;235-249 Outstanding article on the correlation of lead-generation strategies (HTS and rational design) with their effects on the solubility and permeability of discovery candidates.
-
(2000)
J. Pharm. Tox. Methods
, vol.44
, pp. 235-249
-
-
Lipinski, C.A.1
-
10
-
-
0002510887
-
Avoiding investment in doomed drugs
-
Lipinski C.A. Avoiding investment in doomed drugs. Curr. Drug Disc. April:2001;17-19.
-
(2001)
Curr. Drug Disc.
, vol.APRIL
, pp. 17-19
-
-
Lipinski, C.A.1
-
11
-
-
0031024171
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
Landmark article on solubility, its effects on drug discovery research, and the highly effective 'rule of 5' for drug-like properties
-
Lipinski C.A., Lombardo F., Dominy B.W., Feeney P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Delivery Rev. 46:2001;3-26 Landmark article on solubility, its effects on drug discovery research, and the highly effective 'rule of 5' for drug-like properties.
-
(2001)
Adv. Drug Delivery Rev.
, vol.46
, pp. 3-26
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
12
-
-
0034655372
-
A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates
-
Bevan C.D., Lloyd R.S. A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates. Anal. Chem. 72:2000;1781-1787.
-
(2000)
Anal. Chem.
, vol.72
, pp. 1781-1787
-
-
Bevan, C.D.1
Lloyd, R.S.2
-
13
-
-
0035468033
-
Physicochemical profiling (solubility, permeability and charge state)
-
A detailed treatise on the fundamentals of key physicochemical properties, how these properties affect drug interaction with biological systems, and drug absorption
-
Avdeef A. Physicochemical profiling (solubility, permeability and charge state). Curr. Topics Med. Chem. 1:2001;277-351 A detailed treatise on the fundamentals of key physicochemical properties, how these properties affect drug interaction with biological systems, and drug absorption.
-
(2001)
Curr. Topics Med. Chem.
, vol.1
, pp. 277-351
-
-
Avdeef, A.1
-
14
-
-
0035069173
-
Comparison of chromatographic and spectroscopic methods used to rank compounds for aqueous solubility
-
Pan L., Ho Q., Tsutsui K., Takahashi L. Comparison of chromatographic and spectroscopic methods used to rank compounds for aqueous solubility. J. Pharm. Sci. 90:2001;521-529.
-
(2001)
J. Pharm. Sci.
, vol.90
, pp. 521-529
-
-
Pan, L.1
Ho, Q.2
Tsutsui, K.3
Takahashi, L.4
-
15
-
-
0036828814
-
Evaluation of method for high throughput solubility determination using a multi-wavelength UV plate reader
-
Chen T.M., Shen H., Zhu C. Evaluation of method for high throughput solubility determination using a multi-wavelength UV plate reader. Comb. Chem. High Throughput Screen. 5:2002;575-581.
-
(2002)
Comb. Chem. High Throughput Screen
, vol.5
, pp. 575-581
-
-
Chen, T.M.1
Shen, H.2
Zhu, C.3
-
16
-
-
0035286778
-
Caco-2 monolayers in experimental and theoretical predictions of drug transport
-
Artursson P., Palm K., Luthman K. Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adv. Drug Deliv. Rev. 46:2001;27-43.
-
(2001)
Adv. Drug Deliv. Rev.
, vol.46
, pp. 27-43
-
-
Artursson, P.1
Palm, K.2
Luthman, K.3
-
17
-
-
0032949615
-
MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening
-
Irvine J.D., Takahashi L., Lockhart K., Cheong J., Tolan J.W., Selick H.E., Grove J.R. MDCK (Madin-Darby canine kidney) cells: a tool for membrane permeability screening. J. Pharm. Sci. 88:1999;28-33.
-
(1999)
J. Pharm. Sci.
, vol.88
, pp. 28-33
-
-
Irvine, J.D.1
Takahashi, L.2
Lockhart, K.3
Cheong, J.4
Tolan, J.W.5
Selick, H.E.6
Grove, J.R.7
-
18
-
-
0034896546
-
Evaluation of BBMEC model for screening the CNS permeability of drugs
-
Otis K.W., Avery M.L., Broward-Partin S.M., Hansen D.K., Behlow H.W. Jr., Scott D.O., Thompson T.N. Evaluation of BBMEC model for screening the CNS permeability of drugs. J. Pharm. Tox. Methods. 45:2001;71-77.
-
(2001)
J. Pharm. Tox. Methods
, vol.45
, pp. 71-77
-
-
Otis, K.W.1
Avery, M.L.2
Broward-Partin, S.M.3
Hansen, D.K.4
Behlow H.W., Jr.5
Scott, D.O.6
Thompson, T.N.7
-
19
-
-
0032568397
-
Physicochemical high throughput screening: Parallel artificial membrane permeation assay in the description of passive absorption processes
-
Kansy M., Senner F., Gubernator K. Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. J. Med. Chem. 41:1998;1007-1010.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 1007-1010
-
-
Kansy, M.1
Senner, F.2
Gubernator, K.3
-
20
-
-
0035866672
-
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes
-
Wohnsland F., Faller B. High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. J. Med. Chem. 44:2001;923-930.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 923-930
-
-
Wohnsland, F.1
Faller, B.2
-
21
-
-
0037173513
-
Prediction of total passive permeation using bio-mimetic artificial membrane permeability and paracellular pathway model
-
Sugano K., Takata N., Machida M., Saitoh K. Prediction of total passive permeation using bio-mimetic artificial membrane permeability and paracellular pathway model. J. Pharm. Sci. Tech. Japan. 62:2002;241.
-
(2002)
J. Pharm. Sci. Tech. Japan
, vol.62
, pp. 241
-
-
Sugano, K.1
Takata, N.2
Machida, M.3
Saitoh, K.4
-
22
-
-
0036238280
-
A comparative study of artificial permeability assay for high throughput profiling of drug absorption potential
-
Zhu C., Jiang L., Chen T.M., Hwang K.K. A comparative study of artificial permeability assay for high throughput profiling of drug absorption potential. Eur. J. Med. Chem. 37:2002;399-407.
-
(2002)
Eur. J. Med. Chem.
, vol.37
, pp. 399-407
-
-
Zhu, C.1
Jiang, L.2
Chen, T.M.3
Hwang, K.K.4
-
23
-
-
84962359573
-
High throughput artificial membrane permeability assay for blood-brain barrier
-
in press
-
Di L, Kerns EH, Fan K, McConnell OJ, Carter G: High throughput artificial membrane permeability assay for blood-brain barrier. Eur J Med Chem 2003, in press.
-
(2003)
Eur J Med Chem
-
-
Di, L.1
Kerns, E.H.2
Fan, K.3
McConnell, O.J.4
Carter, G.5
-
24
-
-
0035478419
-
The drug efflux-metabolism alliance: Biochemical aspects
-
Benet L.Z., Cummins C.L. The drug efflux-metabolism alliance: biochemical aspects. Adv. Drug Deliv. Rev. 50(Suppl 1):2001;S3-11.
-
(2001)
Adv. Drug Deliv. Rev.
, vol.50
, Issue.SUPPL. 1
, pp. 3-11
-
-
Benet, L.Z.1
Cummins, C.L.2
-
25
-
-
0034763005
-
Rational use of in vitro P-glycoprotein assays in drug discovery
-
Polli J.W., Wring S.A., Humphreys J.E., Huang L., Morgan J.B., Webster L.O., Serabjit-Singh C.S. Rational use of in vitro P-glycoprotein assays in drug discovery. J. Pharm. Exp. Ther. 299:2001;620-628.
-
(2001)
J. Pharm. Exp. Ther.
, vol.299
, pp. 620-628
-
-
Polli, J.W.1
Wring, S.A.2
Humphreys, J.E.3
Huang, L.4
Morgan, J.B.5
Webster, L.O.6
Serabjit-Singh, C.S.7
-
26
-
-
0037171818
-
A computational ensemble pharmacophore model for identifying substrates of P-glycoprotein
-
Penzotti J.E., Lamb M.L., Evensen E., Grootenhuis D.J. A computational ensemble pharmacophore model for identifying substrates of P-glycoprotein. J. Med. Chem. 45:2002;1737-1740.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 1737-1740
-
-
Penzotti, J.E.1
Lamb, M.L.2
Evensen, E.3
Grootenhuis, D.J.4
-
28
-
-
13244293644
-
High throughput measurement of Log D and pKa
-
Edited by van de Waterbeemd H, Lennernas H, Artursson P. Weinheim: Wiley-VCH; in press
-
Comer JEA: High throughput measurement of Log D and pKa. In Drug Bioavailability. Estimation of Solubility, Permeability and Absorption. Edited by van de Waterbeemd H, Lennernas H, Artursson P. Weinheim: Wiley-VCH; in press.
-
Drug Bioavailability. Estimation of Solubility, Permeability and Absorption
-
-
Comer, J.E.A.1
-
29
-
-
0034493887
-
An increased throughput method for the determination of partition coefficients
-
Hitzel L., Watt A.P., Locker K.L. An increased throughput method for the determination of partition coefficients. Pharm. Res. 17:2000;1389-1395.
-
(2000)
Pharm. Res.
, vol.17
, pp. 1389-1395
-
-
Hitzel, L.1
Watt, A.P.2
Locker, K.L.3
-
30
-
-
0036804586
-
Relative hydrophobicity and lipophilicity of β-blockers and related compounds as measured by aqueous two-phase partitioning, octanol-buffer partitioning, and HPLC
-
Gulyaeva N., Zaslavsky A., Lechner P., Chlenov M., Chait A., Zaslavsky B. Relative hydrophobicity and lipophilicity of β-blockers and related compounds as measured by aqueous two-phase partitioning, octanol-buffer partitioning, and HPLC. Eur. J. Pharm. Sci. 17:2002;81-93.
-
(2002)
Eur. J. Pharm. Sci.
, vol.17
, pp. 81-93
-
-
Gulyaeva, N.1
Zaslavsky, A.2
Lechner, P.3
Chlenov, M.4
Chait, A.5
Zaslavsky, B.6
-
31
-
-
0035913059
-
ElogD(oct): A tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds
-
Lombardo F., Shalaeva M.Y., Tupper K.A., Gao F. ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. J. Med. Chem. 44:2001;2490-2497.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2490-2497
-
-
Lombardo, F.1
Shalaeva, M.Y.2
Tupper, K.A.3
Gao, F.4
-
32
-
-
0034929926
-
Rapid method for the estimation of octanol/water partition coefficient (log P(oct)) from gradient RP-HPLC retention and a hydrogen bond acidity term (Σα2H)
-
Valko K., Du C.M., Bevan C., Reynolds D.P., Abraham M.H. Rapid method for the estimation of octanol/water partition coefficient (log P(oct)) from gradient RP-HPLC retention and a hydrogen bond acidity term (Σα2H). Curr. Med. Chem. 8:2001;1137-1146.
-
(2001)
Curr. Med. Chem.
, vol.8
, pp. 1137-1146
-
-
Valko, K.1
Du, C.M.2
Bevan, C.3
Reynolds, D.P.4
Abraham, M.H.5
-
34
-
-
0033384221
-
Prediction of distribution coefficients from structure. Comparison of calculated and experimental data for various drugs
-
Tsantili-Kakoulidou A, Panderi I, Piperaki S, Csizmadia F, Darvas F: Prediction of distribution coefficients from structure. Comparison of calculated and experimental data for various drugs. Eur J Drug Metab Pharmacokin 1999, 24:205-212. On World Wide Web URL: http://www.ahsystem.com/compudrug.html .
-
(1999)
Eur J Drug Metab Pharmacokin
, vol.24
, pp. 205-212
-
-
Tsantili-Kakoulidou, A.1
Panderi, I.2
Piperaki, S.3
Csizmadia, F.4
Darvas, F.5
-
35
-
-
0034256965
-
On the recognition of mammalian microsomal cytochrome P450 substrates and their characteristics: Towards the prediction of human P450 substrate specificity and metabolism
-
Lewis D.F.V. On the recognition of mammalian microsomal cytochrome P450 substrates and their characteristics: towards the prediction of human P450 substrate specificity and metabolism. Biochem. Pharmacol. 60:2000;293-306.
-
(2000)
Biochem. Pharmacol.
, vol.60
, pp. 293-306
-
-
Lewis, D.F.V.1
-
36
-
-
85031154214
-
High throughput measurement of pKa values in a mixed-buffer linear pH gradient system
-
in press
-
Box K, Bevan C, Comer J, Hill A, Allen R, Reynolds D: High throughput measurement of pKa values in a mixed-buffer linear pH gradient system. Anal Chem, in press.
-
Anal Chem
-
-
Box, K.1
Bevan, C.2
Comer, J.3
Hill, A.4
Allen, R.5
Reynolds, D.6
-
37
-
-
0036017359
-
A rapid method for pKa determination of drugs using pressure-assisted capillary electrophoresis with photodiode array detection in drug discovery
-
Ishihama Y., Nakamura M., Miwa T., Kajima T., Asakawa N. A rapid method for pKa determination of drugs using pressure-assisted capillary electrophoresis with photodiode array detection in drug discovery. J. Pharm. Sci. 91:2002;933-942.
-
(2002)
J. Pharm. Sci.
, vol.91
, pp. 933-942
-
-
Ishihama, Y.1
Nakamura, M.2
Miwa, T.3
Kajima, T.4
Asakawa, N.5
-
38
-
-
85031161560
-
ACD/PhysChem: Product overview
-
Nov. Toronto
-
Jouravleva D: ACD/PhysChem: product overview. AAPS - ACD Users' Meeting 2002, Nov. Toronto http://www.acdlabs.com/publish/.
-
AAPS - ACD Users' Meeting 2002
-
-
Jouravleva, D.1
-
39
-
-
0035031472
-
In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery
-
The authors provided excellent comparisons and precautions for different high-throughput metabolic screening assays
-
Masimirembwa C.M., Thompson R., Andersson T.B. In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery. Comb. Chem. High Throughput Screen. 4:2001;245-263 The authors provided excellent comparisons and precautions for different high-throughput metabolic screening assays.
-
(2001)
Comb. Chem. High Throughput Screen
, vol.4
, pp. 245-263
-
-
Masimirembwa, C.M.1
Thompson, R.2
Andersson, T.B.3
-
40
-
-
0035313896
-
Screening for human ADME/Tox drug properties in drug discovery
-
Li A.P. Screening for human ADME/Tox drug properties in drug discovery. Drug Disc. Today. 6:2001;357-366.
-
(2001)
Drug Disc. Today
, vol.6
, pp. 357-366
-
-
Li, A.P.1
-
41
-
-
0036112196
-
Application of parallel liquid chromatography/mass spectrometry for high throughput microsomal stability screening of compound libraries
-
Xu R., Nemes C., Jenkins K.M., Rourick R.A., Kassel D.B., Liu C.Z.C. Application of parallel liquid chromatography/mass spectrometry for high throughput microsomal stability screening of compound libraries. J. Am. Soc. Mass. Spec. 13:2002;155-165.
-
(2002)
J. Am. Soc. Mass. Spec.
, vol.13
, pp. 155-165
-
-
Xu, R.1
Nemes, C.2
Jenkins, K.M.3
Rourick, R.A.4
Kassel, D.B.5
Liu, C.Z.C.6
-
42
-
-
0035298741
-
A high-capacity LC/MS system for the bioanalysis of samples generated from plate-based metabolic screening
-
An innovative approach for increasing sensitivity and selectivity in high-throughput assays by using LC/MS/MS and unique automation
-
Janiszewski J.S., Rogers K.J., Whalen K.M., Cole M.J., Liston T.E., Duchoslav E., Fouda H.G. A high-capacity LC/MS system for the bioanalysis of samples generated from plate-based metabolic screening. Anal. Chem. 73:2001;1495-1501 An innovative approach for increasing sensitivity and selectivity in high-throughput assays by using LC/MS/MS and unique automation.
-
(2001)
Anal. Chem.
, vol.73
, pp. 1495-1501
-
-
Janiszewski, J.S.1
Rogers, K.J.2
Whalen, K.M.3
Cole, M.J.4
Liston, T.E.5
Duchoslav, E.6
Fouda, H.G.7
-
43
-
-
0033800945
-
Rapid assessment of drug metabolism in the drug discovery process
-
Bertrand M., Jackson P., Walther B. Rapid assessment of drug metabolism in the drug discovery process. Eur. J. Pharm. Sci. 11(Suppl 2):2000;S61-S72.
-
(2000)
Eur. J. Pharm. Sci.
, vol.11
, Issue.SUPPL. 2
-
-
Bertrand, M.1
Jackson, P.2
Walther, B.3
-
44
-
-
0037175444
-
Semi-automated determination of plasma stability of drug discovery compounds using liquid chromatography-tandem mass spectrometry
-
Wang G., Hsieh Y., Lau Y.Y., Cheng K.-C., Ng K., Korfmacher W.A., White R.E. Semi-automated determination of plasma stability of drug discovery compounds using liquid chromatography-tandem mass spectrometry. J. Chromatogr. B. 780:2002;451-457.
-
(2002)
J. Chromatogr. B
, vol.780
, pp. 451-457
-
-
Wang, G.1
Hsieh, Y.2
Lau, Y.Y.3
Cheng, K.-C.4
Ng, K.5
Korfmacher, W.A.6
White, R.E.7
-
45
-
-
0033694566
-
Fluorometric high-throughput screening for inhibitors of cytochrome P450
-
Miller V.P., Stresser D.M., Blanchard A.P., Turner S., Crespi C.L. Fluorometric high-throughput screening for inhibitors of cytochrome P450. Annals New York Academy Sci. 919:2000;26-32.
-
(2000)
Annals New York Academy Sci.
, vol.919
, pp. 26-32
-
-
Miller, V.P.1
Stresser, D.M.2
Blanchard, A.P.3
Turner, S.4
Crespi, C.L.5
-
46
-
-
0037212558
-
High-throughput inhibition screening of major human cytochrome P450 enzymes using an in vitro cocktail and liquid chromatography-tandem mass spectrometry
-
Testino S.A. Jr., Patonay G. High-throughput inhibition screening of major human cytochrome P450 enzymes using an in vitro cocktail and liquid chromatography-tandem mass spectrometry. J. Pharm. Biomed. Anal. 30:2003;1459-1467.
-
(2003)
J. Pharm. Biomed. Anal.
, vol.30
, pp. 1459-1467
-
-
Testino S.A., Jr.1
Patonay, G.2
-
47
-
-
0032970480
-
Fully automated analysis of activities catalysed by the major human liver cytochrome P450 (CYP) enzymes: Assessment of human CYP inhibition potential
-
Moody G.C., Griffin S.J., Mather A.N., McGinnity D.F., Riley R.J. Fully automated analysis of activities catalysed by the major human liver cytochrome P450 (CYP) enzymes: assessment of human CYP inhibition potential. Xenobiotica. 29:1999;53-75.
-
(1999)
Xenobiotica
, vol.29
, pp. 53-75
-
-
Moody, G.C.1
Griffin, S.J.2
Mather, A.N.3
McGinnity, D.F.4
Riley, R.J.5
-
49
-
-
0035039894
-
Inhibition of CYP3A4 in a rapid microtiter plate assay using recombinant enzyme and in human liver microsomes using conventional substrates
-
Nomeir A.A., Ruegg C., Shoemaker M., Favreau L.V., Palamanda J.R., Silber P., Lin C.C. Inhibition of CYP3A4 in a rapid microtiter plate assay using recombinant enzyme and in human liver microsomes using conventional substrates. Drug Metab. Disp. 29:2001;748-753.
-
(2001)
Drug Metab. Disp.
, vol.29
, pp. 748-753
-
-
Nomeir, A.A.1
Ruegg, C.2
Shoemaker, M.3
Favreau, L.V.4
Palamanda, J.R.5
Silber, P.6
Lin, C.C.7
-
50
-
-
0033664783
-
Substrate-dependent modulation of CYP3A4 catalytic activity: Analysis of 27 test compounds with four fluorometric substrates
-
Stresser D.M., Blanchard A.P., Turner S.D., Erve J.C.L., Dandeneau A.A., Miller V.P., Crespi C.L. Substrate-dependent modulation of CYP3A4 catalytic activity: analysis of 27 test compounds with four fluorometric substrates. Drug Metab. Dispos. 28:2000;1440-1448.
-
(2000)
Drug Metab. Dispos.
, vol.28
, pp. 1440-1448
-
-
Stresser, D.M.1
Blanchard, A.P.2
Turner, S.D.3
Erve, J.C.L.4
Dandeneau, A.A.5
Miller, V.P.6
Crespi, C.L.7
-
51
-
-
0037204548
-
Computational methods for the prediction of ADME and toxicity
-
The entire issue (page 253-451) covers in silico methods for ADME/TOX predictions by a group of highly respected scientists
-
Clark D.E. Computational methods for the prediction of ADME and toxicity. Adv. Drug Deliv. Rev. 54:2002;253-254 The entire issue (page 253-451) covers in silico methods for ADME/TOX predictions by a group of highly respected scientists.
-
(2002)
Adv. Drug Deliv. Rev.
, vol.54
, pp. 253-254
-
-
Clark, D.E.1
-
52
-
-
0037413529
-
Structure-activity relationships of 1,2,4-benzotriazine 1,4-dioxides as hypoxia-selective analogues of tirapazamine
-
Hay M.P., Gamage S.A., Kovacs M.S., Pruijn F.B., Anderson R.F., Patterson A.V., Wilson W.R., Brown J.M., Denny W.A. Structure-activity relationships of 1,2,4-benzotriazine 1,4-dioxides as hypoxia-selective analogues of tirapazamine. J. Med. Chem. 46:2003;145-154.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 145-154
-
-
Hay, M.P.1
Gamage, S.A.2
Kovacs, M.S.3
Pruijn, F.B.4
Anderson, R.F.5
Patterson, A.V.6
Wilson, W.R.7
Brown, J.M.8
Denny, W.A.9
-
53
-
-
0037153202
-
Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-{2-[(3-substituted)-1-azetidinyl]ethyl}-2-piperidones. 1. Selective antagonists of the neurokinin-2 receptor
-
MacKenzie A.R., Marchington A.P., Middleton D.S., Newman S.D., Jones B.C. Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-{2-[(3-substituted)-1-azetidinyl]ethyl}-2-piperidones. 1. Selective antagonists of the neurokinin-2 receptor. J. Med. Chem. 45:2002;5365-5377.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 5365-5377
-
-
MacKenzie, A.R.1
Marchington, A.P.2
Middleton, D.S.3
Newman, S.D.4
Jones, B.C.5
-
54
-
-
0001620405
-
SAR and pH stability of cyano-substituted epothilones
-
Regueiro-Ren A., Leavitt K., Kim S., Höfle G., Kiffe M., Gougoutas J.Z., DiMarco J.D., Lee F.Y.F., Fairchild C.R., Long B.H., Vite G.D. SAR and pH stability of cyano-substituted epothilones. Org. Lett. 4:2002;3815-3818.
-
(2002)
Org. Lett.
, vol.4
, pp. 3815-3818
-
-
Regueiro-Ren, A.1
Leavitt, K.2
Kim, S.3
Höfle, G.4
Kiffe, M.5
Gougoutas, J.Z.6
DiMarco, J.D.7
Lee, F.Y.F.8
Fairchild, C.R.9
Long, B.H.10
Vite, G.D.11
-
55
-
-
0034608331
-
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors
-
Revesz L., Di Padova F.E., Buhl T., Feifel R., Gram H., Hiestand P., Manning U., Zimmerlin A.G. SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors. Bioorg. Med. Chem. Lett. 10:2000;1261-1264.
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 1261-1264
-
-
Revesz, L.1
Di Padova, F.E.2
Buhl, T.3
Feifel, R.4
Gram, H.5
Hiestand, P.6
Manning, U.7
Zimmerlin, A.G.8
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