-
1
-
-
0022017322
-
3H]CGP-12177 and its use to determine the rate constants of unlabeled -adrenergic antagonists
-
DOI 10.1073/pnas.82.3.925
-
Affolter H, Hertel C, Jaeggi K, Portenier M, and Staehelin M (1985) (-)-S-[3H]CGP-12177 and its use to determine the rate constants of unlabeled beta-adrenergic antagonists. Proc Natl Acad Sci USA 82:925-929. (Pubitemid 15142790)
-
(1985)
Proceedings of the National Academy of Sciences of the United States of America
, vol.82
, Issue.3
, pp. 925-929
-
-
Affolter, H.1
Hertel, C.2
Jaeggi, K.3
-
2
-
-
45549108603
-
2-adrenergic receptor structure
-
DOI 10.1038/nchembio.97, PII NCHEMBIO97
-
Audet M and Bouvier M (2008) Insights into signaling from the beta2-adrenergic receptor structure. Nat Chem Biol 4:397-403. (Pubitemid 351860553)
-
(2008)
Nature Chemical Biology
, vol.4
, Issue.7
, pp. 397-403
-
-
Audet, M.1
Bouvier, M.2
-
3
-
-
0031942688
-
PH-Metric logP 10. Determination of liposomal membrane-water partition coefficients of ionizable drugs
-
DOI 10.1023/A:1011954332221
-
Avdeef A, Box KJ, Comer JE, Hibbert C, and Tam KY (1998) pH-metric logP 10. Determination of liposomal membrane-water partition coefficients of ionizable drugs. Pharm Res 15:209-215. (Pubitemid 28144231)
-
(1998)
Pharmaceutical Research
, vol.15
, Issue.2
, pp. 209-215
-
-
Avdeef, A.1
Box, K.J.2
Comer, J.E.A.3
Hibbert, C.4
Tam, K.Y.5
-
4
-
-
77952054496
-
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist
-
Baur F, Beattie D, Beer D, Bentley D, Bradley M, Bruce I, Charlton SJ, Cuenoud B, Ernst R, and Fairhurst RA et al. (2010) The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist. J Med Chem 53:3675-3684.
-
(2010)
J Med Chem
, vol.53
, pp. 3675-3684
-
-
Baur, F.1
Beattie, D.2
Beer, D.3
Bentley, D.4
Bradley, M.5
Bruce, I.6
Charlton, S.J.7
Cuenoud, B.8
Ernst, R.9
Fairhurst, R.A.10
-
5
-
-
33847659232
-
Miniaturized receptor binding assays: Complications arising from ligand depletion
-
DOI 10.1177/1087057106297788
-
Carter CM, Leighton-Davies JR, and Charlton SJ (2007) Miniaturized receptor binding assays: complications arising from ligand depletion. J Biomol Screen 12:255-266. (Pubitemid 46364429)
-
(2007)
Journal of Biomolecular Screening
, vol.12
, Issue.2
, pp. 255-266
-
-
Carter, C.M.S.1
Leighton-Davies, J.R.2
Charlton, S.J.3
-
6
-
-
30044436650
-
Lipid membrane-induced optimization for ligand-receptor docking: Recent tools and insights for the "membrane catalysis" model
-
DOI 10.1007/s00249-005-0007-9
-
Castanho MA and Fernandes MX (2006) Lipid membrane-induced optimization for ligand-receptor docking: recent tools and insights for the "membrane catalysis" model. Eur Biophys J 35:92-103. (Pubitemid 43045700)
-
(2006)
European Biophysics Journal
, vol.35
, Issue.2
, pp. 92-103
-
-
Castanho, M.A.R.B.1
Fernandes, M.X.2
-
7
-
-
0015861774
-
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
-
Cheng Y and Prusoff WH (1973) Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
-
(1973)
Biochem Pharmacol
, vol.22
, pp. 3099-3108
-
-
Cheng, Y.1
Prusoff, W.H.2
-
8
-
-
72449144245
-
Drug efficiency indices for improvement of molecular docking scoring functions
-
García-Sosa AT, Hetényi C, and Maran U (2010) Drug efficiency indices for improvement of molecular docking scoring functions. J Comput Chem 31:174-184.
-
(2010)
J Comput Chem
, vol.31
, pp. 174-184
-
-
García-Sosa, A.T.1
Hetényi, C.2
Maran, U.3
-
9
-
-
0029841642
-
Sustained activation of a G protein-coupled receptor via "anchored" agonist binding. Molecular localization of the salmeterol exosite within the 2-adrenergic receptor
-
Green SA, Spasoff AP, Coleman RA, Johnson M, and Liggett SB (1996) Sustained activation of a G protein-coupled receptor via "anchored" agonist binding. Molecular localization of the salmeterol exosite within the 2-adrenergic receptor. J Biol Chem 271:24029-24035.
-
(1996)
J Biol Chem
, vol.271
, pp. 24029-24035
-
-
Green, S.A.1
Spasoff, A.P.2
Coleman, R.A.3
Johnson, M.4
Liggett, S.B.5
-
10
-
-
84857254248
-
Crystal structure of a lipid G proteincoupled receptor
-
Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, and Schuerer SC et al. (2012) Crystal structure of a lipid G proteincoupled receptor. Science 335:851-855.
-
(2012)
Science
, vol.335
, pp. 851-855
-
-
Hanson, M.A.1
Roth, C.B.2
Jo, E.3
Griffith, M.T.4
Scott, F.L.5
Reinhart, G.6
Desale, H.7
Clemons, B.8
Cahalan, S.M.9
Schuerer, S.C.10
-
11
-
-
0024559362
-
Interaction of 1,4 dihydropyridine calcium channel antagonists with biological membranes: Lipid bilayer partitioning could occur before drug binding to receptors
-
DOI 10.1016/0022-2828(89)90861-4
-
Herbette LG, Vant Erve YM, and Rhodes DG (1989) Interaction of 1, 4 dihydropyridine calcium channel antagonists with biological membranes: lipid bilayer partitioning could occur before drug binding to receptors. J Mol Cell Cardiol 21:187-201. (Pubitemid 19111208)
-
(1989)
Journal of Molecular and Cellular Cardiology
, vol.21
, Issue.2
, pp. 187-201
-
-
Herbette, L.G.1
Vant Erve, Y.M.H.2
Rhodes, D.G.3
-
12
-
-
84887212404
-
A ligand channel through the G protein coupled receptor opsin
-
Hildebrand PW, Scheerer P, Park JH, Choe HW, Piechnick R, Ernst OP, Hofmann KP, and Heck M (2009) A ligand channel through the G protein coupled receptor opsin. PLoS ONE 4:e4382.
-
(2009)
PLoS ONE
, vol.4
-
-
Hildebrand, P.W.1
Scheerer, P.2
Park, J.H.3
Choe, H.W.4
Piechnick, R.5
Ernst, O.P.6
Hofmann, K.P.7
Heck, M.8
-
13
-
-
0020004857
-
125iodo]cyanopindolol to guinea-pig left ventricle membranes
-
DOI 10.1007/BF00501172
-
Hoyer D, Engel G, and Berthold R (1982) Binding characteristics of (+)-, (+/-) - and (-)-[125iodo] cyanopindolol to guinea-pig left ventricle membranes. Naunyn Schmiedebergs Arch Pharmacol 318:319-329. (Pubitemid 12135730)
-
(1982)
Naunyn-Schmiedeberg's Archives of Pharmacology
, vol.318
, Issue.4
, pp. 319-329
-
-
Hoyer, D.1
Engel, G.2
Berthold, R.3
-
14
-
-
49849094738
-
Physiochemical drug properties associated with in vivo toxicological outcomes
-
Hughes JD, Blagg J, Price DA, Bailey S, Decrescenzo GA, Devraj RV, Ellsworth E, Fobian YM, Gibbs ME, and Gilles RW et al. (2008) Physiochemical drug properties associated with in vivo toxicological outcomes. Bioorg Med Chem Lett 18:4872-4875.
-
(2008)
Bioorg Med Chem Lett
, vol.18
, pp. 4872-4875
-
-
Hughes, J.D.1
Blagg, J.2
Price, D.A.3
Bailey, S.4
Decrescenzo, G.A.5
Devraj, R.V.6
Ellsworth, E.7
Fobian, Y.M.8
Gibbs, M.E.9
Gilles, R.W.10
-
15
-
-
77952921531
-
A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor
-
Hurst DP, Grossfield A, Lynch DL, Feller S, Romo TD, Gawrisch K, Pitman MC, and Reggio PH (2010) A lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptor. J Biol Chem 285:17954-17964.
-
(2010)
J Biol Chem
, vol.285
, pp. 17954-17964
-
-
Hurst, D.P.1
Grossfield, A.2
Lynch, D.L.3
Feller, S.4
Romo, T.D.5
Gawrisch, K.6
Pitman, M.C.7
Reggio, P.H.8
-
16
-
-
53149123260
-
A method for rapidly predicting drug tissue distribution using surfactant vesicle electrokinetic chromatography
-
Jiang Z, Reilly J, and Everatt B (2008) A method for rapidly predicting drug tissue distribution using surfactant vesicle electrokinetic chromatography. Electrophoresis 29:3674-3684.
-
(2008)
Electrophoresis
, vol.29
, pp. 3674-3684
-
-
Jiang, Z.1
Reilly, J.2
Everatt, B.3
-
17
-
-
0037683435
-
Pharmaceutical profiling method for lipophilicity and integrity using liquid chromatography-mass spectrometry
-
DOI 10.1016/S1570-0232(03)00250-2
-
Kerns EH, Di L, Petusky S, Kleintop T, Huryn D, McConnell O, and Carter G (2003) Pharmaceutical profiling method for lipophilicity and integrity using liquid chromatography-mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci 791:381-388. (Pubitemid 36638771)
-
(2003)
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
, vol.791
, Issue.1-2
, pp. 381-388
-
-
Kerns, E.H.1
Di, L.2
Petusky, S.3
Kleintop, T.4
Huryn, D.5
McConnell, O.6
Carter, G.7
-
18
-
-
35748934487
-
The influence of drug-like concepts on decision-making in medicinal chemistry
-
DOI 10.1038/nrd2445, PII NRD2445
-
Leeson PD and Springthorpe B (2007) The influence of drug-like concepts on decisionmaking in medicinal chemistry. Nat Rev Drug Discov 6:881-890. (Pubitemid 350042396)
-
(2007)
Nature Reviews Drug Discovery
, vol.6
, Issue.11
, pp. 881-890
-
-
Leeson, P.D.1
Springthorpe, B.2
-
19
-
-
0035289779
-
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
-
DOI 10.1016/S0169-409X(00)00129-0, PII S0169409X00001290
-
Lipinski CA, Lombardo F, Dominy BW, and Feeney PJ (2001) Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 46:3-26. (Pubitemid 33653411)
-
(2000)
Advanced Drug Delivery Reviews
, vol.46
, Issue.1-3
, pp. 3-26
-
-
Lipinski, C.A.1
Lombardo, F.2
Dominy, B.W.3
Feeney, P.J.4
-
20
-
-
0025854810
-
Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes
-
Mason RP, Rhodes DG, and Herbette LG (1991) Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes. J Med Chem 34:869-877.
-
(1991)
J Med Chem
, vol.34
, pp. 869-877
-
-
Mason, R.P.1
Rhodes, D.G.2
Herbette, L.G.3
-
21
-
-
0022625444
-
Rates of membrane-associated reactions: Reduction of dimensionality revisited
-
DOI 10.1083/jcb.102.1.88
-
McCloskey MA and Poo MM (1986) Rates of membrane-associated reactions: reduction of dimensionality revisited. J Cell Biol 102:88-96. (Pubitemid 16155556)
-
(1986)
Journal of Cell Biology
, vol.102
, Issue.1
, pp. 88-96
-
-
McCloskey, M.A.1
Poo, M.-M.2
-
22
-
-
0021336303
-
The kinetics of competitive radioligand binding predicted by the law of mass action
-
Motulsky HJ and Mahan LC (1984). The kinetics of competitive radioligand binding predicted by the law of mass action. Mol Pharmacol 25:1-9. (Pubitemid 14223246)
-
(1984)
Molecular Pharmacology
, vol.25
, Issue.1
, pp. 1-9
-
-
Motulsky, H.J.1
Mahan, L.C.2
-
23
-
-
0021861363
-
Kinetics of binding of membrane-active drugs to receptor sites. Diffusion-limited rates for a membrane bilayer approach of 1,4-dihydropyridine calcium channel antagonists to their active site
-
Rhodes DG, Sarmiento JG, and Herbette LG (1985) Kinetics of binding of membraneactive drugs to receptor sites. Diffusion-limited rates for a membrane bilayer approach of 1, 4-dihydropyridine calcium channel antagonists to their active site. Mol Pharmacol 27:612-623. (Pubitemid 15010692)
-
(1985)
Molecular Pharmacology
, vol.27
, Issue.6
, pp. 612-623
-
-
Rhodes, D.G.1
Sarmiento, J.G.2
Herbette, L.G.3
-
25
-
-
69549098265
-
Exploring the mechanism of agonist efficacy: A relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor
-
Sykes DA, Dowling MR, and Charlton SJ (2009) Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor. Mol Pharmacol 76:543-551.
-
(2009)
Mol Pharmacol
, vol.76
, pp. 543-551
-
-
Sykes, D.A.1
Dowling, M.R.2
Charlton, S.J.3
-
26
-
-
84859059730
-
Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists
-
Sykes DA and Charlton SJ (2012) Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists. Br J Pharmacol 165:2672-2683.
-
(2012)
Br J Pharmacol
, vol.165
, pp. 2672-2683
-
-
Sykes, D.A.1
Charlton, S.J.2
-
27
-
-
69249205472
-
Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol
-
Szczuka A, Wennerberg M, Packeu A, and Vauquelin G (2009) Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol. Br J Pharmacol 158:183-194.
-
(2009)
Br J Pharmacol
, vol.158
, pp. 183-194
-
-
Szczuka, A.1
Wennerberg, M.2
Packeu, A.3
Vauquelin, G.4
-
28
-
-
0033818097
-
Rapid-gradient HPLC method for measuring drug interactions with immobilized artificial membrane: Comparison with other lipophilicity measures
-
Valko K, Du CM, Bevan CD, Reynolds DP, and Abraham MH (2000) Rapid-gradient HPLC method for measuring drug interactions with immobilized artificial membrane: comparison with other lipophilicity measures. J Pharm Sci 89:1085-1096.
-
(2000)
J Pharm Sci
, vol.89
, pp. 1085-1096
-
-
Valko, K.1
Du, C.M.2
Bevan, C.D.3
Reynolds, D.P.4
Abraham, M.H.5
-
29
-
-
77956805081
-
Rebinding: Or why drugs may act longer in vivo than expected from their in vitro target residence time
-
Vauquelin G (2010) Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time. Expert Opin Drug Discov 5:927-941.
-
(2010)
Expert Opin Drug Discov
, vol.5
, pp. 927-941
-
-
Vauquelin, G.1
-
30
-
-
69249210978
-
Ligands, their receptors and... Plasma membranes
-
Vauquelin G and Packeu A (2009) Ligands, their receptors and... plasma membranes. Mol Cell Endocrinol 311:1-10.
-
(2009)
Mol Cell Endocrinol
, vol.311
, pp. 1-10
-
-
Vauquelin, G.1
Packeu, A.2
-
31
-
-
77956309074
-
Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action
-
Vauquelin G and Charlton SJ (2010) Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action. Br J Pharmacol 161:488-508.
-
(2010)
Br J Pharmacol
, vol.161
, pp. 488-508
-
-
Vauquelin, G.1
Charlton, S.J.2
|