-
1
-
-
33751547539
-
How Many Drug Targets are There?
-
Overington, J. P.; Al-Lazikani, B.; Hopkins, A. L. How Many Drug Targets are There? Nat. Rev. Drug Discovery 2006, 5, 993-996 10.1038/nrd2199
-
(2006)
Nat. Rev. Drug Discovery
, vol.5
, pp. 993-996
-
-
Overington, J.P.1
Al-Lazikani, B.2
Hopkins, A.L.3
-
2
-
-
80053615320
-
The Significance of G Protein-Coupled Receptor Crystallography for Drug Discovery
-
Salon, J. A.; Lodowski, D. T.; Palczewski, K. The Significance of G Protein-Coupled Receptor Crystallography for Drug Discovery Pharmacol. Rev. 2011, 63, 901-937 10.1124/pr.110.003350
-
(2011)
Pharmacol. Rev.
, vol.63
, pp. 901-937
-
-
Salon, J.A.1
Lodowski, D.T.2
Palczewski, K.3
-
3
-
-
78650122737
-
A Graphical Journey of Innovative Organic Architectures That Have Improved Our Lives
-
McGrath, N. A.; Brichacek, M.; Njardarson, J. T. A Graphical Journey of Innovative Organic Architectures That Have Improved Our Lives J. Chem. Educ. 2010, 87, 1348-1349 10.1021/ed1003806
-
(2010)
J. Chem. Educ.
, vol.87
, pp. 1348-1349
-
-
McGrath, N.A.1
Brichacek, M.2
Njardarson, J.T.3
-
4
-
-
79960176452
-
Progress in Structure Based Drug Design for G Protein-Coupled Receptors
-
Congreve, M.; Langmead, C. J.; Mason, J. S.; Marshall, F. H. Progress in Structure Based Drug Design for G Protein-Coupled Receptors J. Med. Chem. 2011, 54, 4283-4311 10.1021/jm200371q
-
(2011)
J. Med. Chem.
, vol.54
, pp. 4283-4311
-
-
Congreve, M.1
Langmead, C.J.2
Mason, J.S.3
Marshall, F.H.4
-
5
-
-
84890503612
-
The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors
-
Alexander, S. P. H.; Benson, H. E.; Faccenda, E.; Pawson, A. J.; Sharman, J. L.; Spedding, M.; Peters, J. A.; Harmar, A. J. The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors Br. J. Pharmacol. 2013, 170, 1459-1581 10.1111/bph.12445
-
(2013)
Br. J. Pharmacol.
, vol.170
, pp. 1459-1581
-
-
Alexander, S.P.H.1
Benson, H.E.2
Faccenda, E.3
Pawson, A.J.4
Sharman, J.L.5
Spedding, M.6
Peters, J.A.7
Harmar, A.J.8
-
6
-
-
84958216883
-
Binding and Activity of Opioid Ligands at the Cloned Human Delta, Mu, and Kappa Receptors
-
CRC Press: Boca Raton
-
Kemal, P. Binding and Activity of Opioid Ligands at the Cloned Human Delta, Mu, and Kappa Receptors. In The Delta Receptor; CRC Press: Boca Raton, 2003.
-
(2003)
The Delta Receptor
-
-
Kemal, P.1
-
7
-
-
0028006303
-
Pharmacological Characterization of the Cloned kappa-, delta-, and mu-opioid Receptors
-
Raynor, K.; Kong, H.; Chen, Y.; Yasuda, K.; Yu, L.; Bell, G. I.; Reisine, T. Pharmacological Characterization of the Cloned kappa-, delta-, and mu-opioid Receptors Mol. Pharmacol. 1994, 45, 330-334
-
(1994)
Mol. Pharmacol.
, vol.45
, pp. 330-334
-
-
Raynor, K.1
Kong, H.2
Chen, Y.3
Yasuda, K.4
Yu, L.5
Bell, G.I.6
Reisine, T.7
-
8
-
-
0028900341
-
Structure-Activity Relationships of Synthetic and Semisynthetic Opioid Agonists and Antagonists
-
Fuerst, S.; Hosztafi, S.; Friedmann, T. Structure-Activity Relationships of Synthetic and Semisynthetic Opioid Agonists and Antagonists Curr. Med. Chem. 1995, 1, 423
-
(1995)
Curr. Med. Chem.
, vol.1
, pp. 423
-
-
Fuerst, S.1
Hosztafi, S.2
Friedmann, T.3
-
9
-
-
0141692266
-
Analgesic Potency of Normorphine in Patients with Postoperative Pain
-
Lasagna, L.; De Kornfeld, T. J. Analgesic Potency of Normorphine in Patients with Postoperative Pain J. Pharmacol. Exp. Ther. 1958, 124, 260-263
-
(1958)
J. Pharmacol. Exp. Ther.
, vol.124
, pp. 260-263
-
-
Lasagna, L.1
De Kornfeld, T.J.2
-
10
-
-
0000801464
-
Nonpeptide Agonists for Peptide Receptors: Lessons from Ligands
-
James, A. B. Academic Press: New York, Chapter 28
-
Sugg, E. E., Nonpeptide Agonists for Peptide Receptors: Lessons from Ligands. In Annual Reports in Medicinal Chemistry; James, A. B., Ed.; Academic Press: New York, 1997; Vol. 32, Chapter 28, pp 277-283.
-
(1997)
Annual Reports in Medicinal Chemistry
, vol.32
, pp. 277-283
-
-
Sugg, E.E.1
-
11
-
-
84866730292
-
Subtleties in GPCR Drug Discovery: a Medicinal Chemistry Perspective
-
Fujioka, M.; Omori, N. Subtleties in GPCR Drug Discovery: a Medicinal Chemistry Perspective Drug Discovery Today 2012, 17, 1133-1138 10.1016/j.drudis.2012.06.010
-
(2012)
Drug Discovery Today
, vol.17
, pp. 1133-1138
-
-
Fujioka, M.1
Omori, N.2
-
12
-
-
35348825010
-
Quinazolinone Derivatives as Orally Available Ghrelin Receptor Antagonists for the Treatment of Diabetes and Obesity
-
Rudolph, J.; Esler, W. P.; O'Connor, S.; Coish, P. D. G.; Wickens, P. L.; Brands, M.; Bierer, D. E.; Bloomquist, B. T.; Bondar, G.; Chen, L.; Chuang, C.-Y.; Claus, T. H.; Fathi, Z.; Fu, W.; Khire, U. R.; Kristie, J. A.; Liu, X.-G.; Lowe, D. B.; McClure, A. C.; Michels, M.; Ortiz, A. A.; Ramsden, P. D.; Schoenleber, R. W.; Shelekhin, T. E.; Vakalopoulos, A.; Tang, W.; Wang, L.; Yi, L.; Gardell, S. J.; Livingston, J. N.; Sweet, L. J.; Bullock, W. H. Quinazolinone Derivatives as Orally Available Ghrelin Receptor Antagonists for the Treatment of Diabetes and Obesity J. Med. Chem. 2007, 50, 5202-5216 10.1021/jm070071+
-
(2007)
J. Med. Chem.
, vol.50
, pp. 5202-5216
-
-
Rudolph, J.1
Esler, W.P.2
O'Connor, S.3
Coish, P.D.G.4
Wickens, P.L.5
Brands, M.6
Bierer, D.E.7
Bloomquist, B.T.8
Bondar, G.9
Chen, L.10
Chuang, C.-Y.11
Claus, T.H.12
Fathi, Z.13
Fu, W.14
Khire, U.R.15
Kristie, J.A.16
Liu, X.-G.17
Lowe, D.B.18
McClure, A.C.19
Michels, M.20
Ortiz, A.A.21
Ramsden, P.D.22
Schoenleber, R.W.23
Shelekhin, T.E.24
Vakalopoulos, A.25
Tang, W.26
Wang, L.27
Yi, L.28
Gardell, S.J.29
Livingston, J.N.30
Sweet, L.J.31
Bullock, W.H.32
more..
-
13
-
-
19944405095
-
The Synthesis of Substituted Bipiperidine Amide Compounds as CCR3 Ligands: Antagonists versus Agonists
-
Ting, P. C.; Umland, S. P.; Aslanian, R.; Cao, J.; Garlisi, C. G.; Huang, Y.; Jakway, J.; Liu, Z.; Shah, H.; Tian, F.; Wan, Y.; Shih, N.-Y. The Synthesis of Substituted Bipiperidine Amide Compounds as CCR3 Ligands: Antagonists versus Agonists Bioorg. Med. Chem. Lett. 2005, 15, 3020-3023 10.1016/j.bmcl.2005.04.054
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 3020-3023
-
-
Ting, P.C.1
Umland, S.P.2
Aslanian, R.3
Cao, J.4
Garlisi, C.G.5
Huang, Y.6
Jakway, J.7
Liu, Z.8
Shah, H.9
Tian, F.10
Wan, Y.11
Shih, N.-Y.12
-
14
-
-
26944475559
-
Metabotropic Glutamate II Receptor Agonists in Panic Disorder: a Double Blind Clinical Trial with LY354740
-
Bergink, V.; Westenberg, H. G. M. Metabotropic Glutamate II Receptor Agonists in Panic Disorder: a Double Blind Clinical Trial with LY354740 Int. Clin. Psychopharmal. 2005, 20, 291-293 10.1097/00004850-200511000-00001
-
(2005)
Int. Clin. Psychopharmal.
, vol.20
, pp. 291-293
-
-
Bergink, V.1
Westenberg, H.G.M.2
-
15
-
-
20844441772
-
Methyl Substitution of 2-Aminobicyclo[3.1.0]hexane 2,6-Dicarboxylate (LY354740) Determines Functional Activity at Metabotropic Glutamate Receptors: Identification of a Subtype Selective mGlu2 Receptor Agonist
-
Dominguez, C.; Prieto, L.; Valli, M. J.; Massey, S. M.; Bures, M.; Wright, R. A.; Johnson, B. G.; Andis, S. L.; Kingston, A.; Schoepp, D. D.; Monn, J. A. Methyl Substitution of 2-Aminobicyclo[3.1.0]hexane 2,6-Dicarboxylate (LY354740) Determines Functional Activity at Metabotropic Glutamate Receptors: Identification of a Subtype Selective mGlu2 Receptor Agonist J. Med. Chem. 2005, 48, 3605-3612 10.1021/jm040222y
-
(2005)
J. Med. Chem.
, vol.48
, pp. 3605-3612
-
-
Dominguez, C.1
Prieto, L.2
Valli, M.J.3
Massey, S.M.4
Bures, M.5
Wright, R.A.6
Johnson, B.G.7
Andis, S.L.8
Kingston, A.9
Schoepp, D.D.10
Monn, J.A.11
-
16
-
-
38949207272
-
The mGlu2 but not the mGlu3 Receptor Mediates the Actions of the mGluR2/3 Agonist, LY379268, in Mouse Models Predictive of Antipsychotic Activity
-
Woolley, M. L.; Pemberton, D. J.; Bate, S.; Corti, C.; Jones, D. N. C. The mGlu2 but not the mGlu3 Receptor Mediates the Actions of the mGluR2/3 Agonist, LY379268, in Mouse Models Predictive of Antipsychotic Activity Psychopharmacology 2008, 196, 431-440 10.1007/s00213-007-0974-x
-
(2008)
Psychopharmacology
, vol.196
, pp. 431-440
-
-
Woolley, M.L.1
Pemberton, D.J.2
Bate, S.3
Corti, C.4
Jones, D.N.C.5
-
17
-
-
2542609191
-
A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor
-
Zaveri, N. T.; Jiang, F.; Olsen, C. M.; Deschamps, J. R.; Parrish, D.; Polgar, W.; Toll, L. A Novel Series of Piperidin-4-yl-1,3-Dihydroindol-2-ones as Agonist and Antagonist Ligands at the Nociceptin Receptor J. Med. Chem. 2004, 47, 2973-2976 10.1021/jm034249d
-
(2004)
J. Med. Chem.
, vol.47
, pp. 2973-2976
-
-
Zaveri, N.T.1
Jiang, F.2
Olsen, C.M.3
Deschamps, J.R.4
Parrish, D.5
Polgar, W.6
Toll, L.7
-
18
-
-
0034610435
-
Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated with Fenfluramine and Other Serotonergic Medications
-
Rothman, R. B.; Baumann, M. H.; Savage, J. E.; Rauser, L.; McBride, A.; Hufeisen, S. J.; Roth, B. L. Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated with Fenfluramine and Other Serotonergic Medications Circulation 2000, 102, 2836-2841 10.1161/01.CIR.102.23.2836
-
(2000)
Circulation
, vol.102
, pp. 2836-2841
-
-
Rothman, R.B.1
Baumann, M.H.2
Savage, J.E.3
Rauser, L.4
McBride, A.5
Hufeisen, S.J.6
Roth, B.L.7
-
19
-
-
40849124264
-
Characterization of the Molecular Fragment that is Responsible for Agonism of Pergolide at Serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A Receptors
-
Goernemann, T.; Huebner, H.; Gmeiner, P.; Horowski, R.; Latte, K. P.; Flieger, M.; Pertz, H. H. Characterization of the Molecular Fragment that is Responsible for Agonism of Pergolide at Serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A Receptors J. Pharmacol. Exp. Ther. 2007, 324, 1136-1145 10.1124/jpet.107.133165
-
(2007)
J. Pharmacol. Exp. Ther.
, vol.324
, pp. 1136-1145
-
-
Goernemann, T.1
Huebner, H.2
Gmeiner, P.3
Horowski, R.4
Latte, K.P.5
Flieger, M.6
Pertz, H.H.7
-
20
-
-
33646929505
-
Lisuride, a Dopamine Receptor Agonist with 5-HT2B Receptor Antagonist Properties: Absence of Cardiac Valvulopathy Adverse Drug Reaction Reports Supports the Concept of a Crucial Role for 5-HT2B Receptor Agonism in Cardiac Valvular Fibrosis
-
Hofmann, C.; Penner, U.; Dorow, R.; Pertz, H. H.; Jähnichen, S.; Horowski, R.; Latté, K. P.; Palla, D.; Schurad, B. Lisuride, a Dopamine Receptor Agonist With 5-HT2B Receptor Antagonist Properties: Absence of Cardiac Valvulopathy Adverse Drug Reaction Reports Supports the Concept of a Crucial Role for 5-HT2B Receptor Agonism in Cardiac Valvular Fibrosis Clin. Neuropharmacol. 2006, 29, 80-86 10.1097/00002826-200603000-00005
-
(2006)
Clin. Neuropharmacol.
, vol.29
, pp. 80-86
-
-
Hofmann, C.1
Penner, U.2
Dorow, R.3
Pertz, H.H.4
Jähnichen, S.5
Horowski, R.6
Latté, K.P.7
Palla, D.8
Schurad, B.9
-
21
-
-
33845974147
-
Valvular Heart Disease and the Use of Dopamine Agonists for Parkinson's Disease
-
Zanettini, R.; Antonini, A.; Gatto, G.; Gentile, R.; Tesei, S.; Pezzoli, G. Valvular Heart Disease and the Use of Dopamine Agonists for Parkinson's Disease N. Engl. J. Med. 2007, 356, 39-46 10.1056/NEJMoa054830
-
(2007)
N. Engl. J. Med.
, vol.356
, pp. 39-46
-
-
Zanettini, R.1
Antonini, A.2
Gatto, G.3
Gentile, R.4
Tesei, S.5
Pezzoli, G.6
-
22
-
-
79959518063
-
The Bulky N(6) Substituent of Cabergoline Is Responsible for Agonism of This Drug at 5-Hydroxytryptamine (5-HT)2A and 5-HT2B Receptors and Thus Is a Determinant of Valvular Heart Disease
-
Kekewska, A.; Hübner, H.; Gmeiner, P.; Pertz, H. H. The Bulky N(6) Substituent of Cabergoline Is Responsible for Agonism of This Drug at 5-Hydroxytryptamine (5-HT)2A and 5-HT2B Receptors and Thus Is a Determinant of Valvular Heart Disease J. Pharmacol. Exp. Ther. 2011, 338, 381-391 10.1124/jpet.111.181255
-
(2011)
J. Pharmacol. Exp. Ther.
, vol.338
, pp. 381-391
-
-
Kekewska, A.1
Hübner, H.2
Gmeiner, P.3
Pertz, H.H.4
-
23
-
-
84873949983
-
Synthesis of Novel Analogs of Cabergoline: Improving Cardiovascular Safety by Removing 5-HT2B Receptor Agonism
-
Dosa, P. I.; Ward, T.; Walters, M. A.; Kim, S. W. Synthesis of Novel Analogs of Cabergoline: Improving Cardiovascular Safety by Removing 5-HT2B Receptor Agonism ACS Med. Chem. Lett. 2013, 4, 254-258 10.1021/ml3003814
-
(2013)
ACS Med. Chem. Lett.
, vol.4
, pp. 254-258
-
-
Dosa, P.I.1
Ward, T.2
Walters, M.A.3
Kim, S.W.4
-
24
-
-
0031434924
-
Differences between Natural and Recombinant G Protein-coupled Receptor Systems with Varying Receptor/G Protein Stoichiometry
-
Kenakin, T. Differences Between Natural and Recombinant G Protein-coupled Receptor Systems with Varying Receptor/G Protein Stoichiometry Trends Pharmacol. Sci. 1997, 18, 456-464 10.1016/S0165-6147(97)01136-X
-
(1997)
Trends Pharmacol. Sci.
, vol.18
, pp. 456-464
-
-
Kenakin, T.1
-
25
-
-
0030915526
-
Agonist and Inverse Agonist Efficacy at Human Recombinant Serotonin 5-HT1A Receptors as a Function of Receptor:G-protein Stoichiometry
-
Newman-Tancredi, A.; Conte, C.; Chaput, C.; VerriÈLe, L.; Millan, M. J. Agonist and Inverse Agonist Efficacy at Human Recombinant Serotonin 5-HT1A Receptors as a Function of Receptor:G-protein Stoichiometry Neuropharmacology 1997, 36, 451-459 10.1016/S0028-3908(97)00022-1
-
(1997)
Neuropharmacology
, vol.36
, pp. 451-459
-
-
Newman-Tancredi, A.1
Conte, C.2
Chaput, C.3
VerriÈLe, L.4
Millan, M.J.5
-
26
-
-
0035848578
-
Nonpeptide Cholecystokinin-2 Receptor Agonists
-
Kalindjian, S. B.; Dunstone, D. J.; Low, C. M. R.; Pether, M. J.; Roberts, S. P.; Tozer, M. J.; Watt, G. F.; Shankley, N. P. Nonpeptide Cholecystokinin-2 Receptor Agonists J. Med. Chem. 2001, 44, 1125-1133 10.1021/jm0010668
-
(2001)
J. Med. Chem.
, vol.44
, pp. 1125-1133
-
-
Kalindjian, S.B.1
Dunstone, D.J.2
Low, C.M.R.3
Pether, M.J.4
Roberts, S.P.5
Tozer, M.J.6
Watt, G.F.7
Shankley, N.P.8
-
27
-
-
0034676327
-
Novel Design of Nonpeptide AVP V2 Receptor Agonists: Structural Requirements for an Agonist Having 1-(4-Aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a Template
-
Kondo, K.; Ogawa, H.; Shinohara, T.; Kurimura, M.; Tanada, Y.; Kan, K.; Yamashita, H.; Nakamura, S.; Hirano, T.; Yamamura, Y.; Mori, T.; Tominaga, M.; Itai, A. Novel Design of Nonpeptide AVP V2 Receptor Agonists: Structural Requirements for an Agonist Having 1-(4-Aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a Template J. Med. Chem. 2000, 43, 4388-4397 10.1021/jm000108p
-
(2000)
J. Med. Chem.
, vol.43
, pp. 4388-4397
-
-
Kondo, K.1
Ogawa, H.2
Shinohara, T.3
Kurimura, M.4
Tanada, Y.5
Kan, K.6
Yamashita, H.7
Nakamura, S.8
Hirano, T.9
Yamamura, Y.10
Mori, T.11
Tominaga, M.12
Itai, A.13
-
28
-
-
61449164022
-
Guanidine and 2-Aminoimidazoline Aromatic Derivatives as α2-Adrenoceptor Ligands: Searching for Structure-Activity Relationships
-
Rodriguez, F.; Rozas, I.; Ortega, J. E.; Erdozain, A. M.; Meana, J. J.; Callado, L. F. Guanidine and 2-Aminoimidazoline Aromatic Derivatives as α2-Adrenoceptor Ligands: Searching for Structure-Activity Relationships J. Med. Chem. 2009, 52, 601-609 10.1021/jm800838r
-
(2009)
J. Med. Chem.
, vol.52
, pp. 601-609
-
-
Rodriguez, F.1
Rozas, I.2
Ortega, J.E.3
Erdozain, A.M.4
Meana, J.J.5
Callado, L.F.6
-
29
-
-
37349076564
-
N-(Substituted-anilinoethyl)amides: Design, Synthesis, and Pharmacological Characterization of a New Class of Melatonin Receptor Ligands
-
Rivara, S.; Lodola, A.; Mor, M.; Bedini, A.; Spadoni, G.; Lucini, V.; Pannacci, M.; Fraschini, F.; Scaglione, F.; Sanchez, R. O.; Gobbi, G.; Tarzia, G. N-(Substituted-anilinoethyl)amides: Design, Synthesis, and Pharmacological Characterization of a New Class of Melatonin Receptor Ligands J. Med. Chem. 2007, 50, 6618-6626 10.1021/jm700957j
-
(2007)
J. Med. Chem.
, vol.50
, pp. 6618-6626
-
-
Rivara, S.1
Lodola, A.2
Mor, M.3
Bedini, A.4
Spadoni, G.5
Lucini, V.6
Pannacci, M.7
Fraschini, F.8
Scaglione, F.9
Sanchez, R.O.10
Gobbi, G.11
Tarzia, G.12
-
30
-
-
0035927440
-
Transformation of a κ-Opioid Receptor Antagonist to a κ-Agonist by Transfer of a Guanidinium Group from the 5′- to 6′-Position of Naltrindole
-
Sharma, S. K.; Jones, R. M.; Metzger, T. G.; Ferguson, D. M.; Portoghese, P. S. Transformation of a κ-Opioid Receptor Antagonist to a κ-Agonist by Transfer of a Guanidinium Group from the 5′- to 6′-Position of Naltrindole J. Med. Chem. 2001, 44, 2073-2079 10.1021/jm010095v
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2073-2079
-
-
Sharma, S.K.1
Jones, R.M.2
Metzger, T.G.3
Ferguson, D.M.4
Portoghese, P.S.5
-
31
-
-
10744234014
-
Synthesis and Structure-Activity Relationships of Conformationally Constrained Histamine H3 Receptor Agonists
-
Kitbunnadaj, R.; Zuiderveld, O. P.; De Esch, I. J. P.; Vollinga, R. C.; Bakker, R.; Lutz, M.; Spek, A. L.; Cavoy, E.; Deltent, M.-F.; Menge, W. M. P. B.; Timmerman, H.; Leurs, R. Synthesis and Structure-Activity Relationships of Conformationally Constrained Histamine H3 Receptor Agonists J. Med. Chem. 2003, 46, 5445-5457 10.1021/jm030905y
-
(2003)
J. Med. Chem.
, vol.46
, pp. 5445-5457
-
-
Kitbunnadaj, R.1
Zuiderveld, O.P.2
De Esch, I.J.P.3
Vollinga, R.C.4
Bakker, R.5
Lutz, M.6
Spek, A.L.7
Cavoy, E.8
Deltent, M.-F.9
Menge, W.M.P.B.10
Timmerman, H.11
Leurs, R.12
-
32
-
-
84922879972
-
Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands
-
Wallinder, C.; Sköld, C.; Botros, M.; Guimond, M.-O.; Hallberg, M.; Gallo-Payet, N.; Karlén, A.; Alterman, M. Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands ACS Med. Chem. Lett. 2015, 6, 178-182 10.1021/ml500427r
-
(2015)
ACS Med. Chem. Lett.
, vol.6
, pp. 178-182
-
-
Wallinder, C.1
Sköld, C.2
Botros, M.3
Guimond, M.-O.4
Hallberg, M.5
Gallo-Payet, N.6
Karlén, A.7
Alterman, M.8
-
33
-
-
84900307488
-
EMA401, an Orally Administered Highly Selective Angiotensin II Type 2 Receptor Antagonist, as a Novel Treatment for Postherpetic Neuralgia: a Randomised, Double-blind, Placebo-controlled Phase 2 Clinical Trial
-
Rice, A. S. C.; Dworkin, R. H.; McCarthy, T. D.; Anand, P.; Bountra, C.; McCloud, P. I.; Hill, J.; Cutter, G.; Kitson, G.; Desem, N.; Raff, M. EMA401, an Orally Administered Highly Selective Angiotensin II Type 2 Receptor Antagonist, as a Novel Treatment for Postherpetic Neuralgia: a Randomised, Double-blind, Placebo-controlled Phase 2 Clinical Trial Lancet 2014, 383, 1637-1647 10.1016/S0140-6736(13)62337-5
-
(2014)
Lancet
, vol.383
, pp. 1637-1647
-
-
Rice, A.S.C.1
Dworkin, R.H.2
McCarthy, T.D.3
Anand, P.4
Bountra, C.5
McCloud, P.I.6
Hill, J.7
Cutter, G.8
Kitson, G.9
Desem, N.10
Raff, M.11
-
34
-
-
84863240765
-
From the First Selective Non-Peptide AT2 Receptor Agonist to Structurally Related Antagonists
-
Murugaiah, A. M. S.; Wu, X.; Wallinder, C.; Mahalingam, A. K.; Wan, Y.; Sköld, C.; Botros, M.; Guimond, M.-O.; Joshi, A.; Nyberg, F.; Gallo-Payet, N.; Hallberg, A.; Alterman, M. From the First Selective Non-Peptide AT2 Receptor Agonist to Structurally Related Antagonists J. Med. Chem. 2012, 55, 2265-2278 10.1021/jm2015099
-
(2012)
J. Med. Chem.
, vol.55
, pp. 2265-2278
-
-
Murugaiah, A.M.S.1
Wu, X.2
Wallinder, C.3
Mahalingam, A.K.4
Wan, Y.5
Sköld, C.6
Botros, M.7
Guimond, M.-O.8
Joshi, A.9
Nyberg, F.10
Gallo-Payet, N.11
Hallberg, A.12
Alterman, M.13
-
35
-
-
0031035850
-
Dual Agonistic and Antagonistic Property of Nonpeptide Angiotensin AT1 Ligands: Susceptibility to Receptor Mutations
-
Perlman, S.; Costa-Neto, C. M.; Miyakawa, A. A.; Schambye, H. T.; Hjorth, S. A.; Paiva, A. C. M.; Rivero, R. A.; Greenlee, W. J.; Schwartz, T. W. Dual Agonistic and Antagonistic Property of Nonpeptide Angiotensin AT1 Ligands: Susceptibility to Receptor Mutations Mol. Pharmacol. 1997, 51, 301-311 10.1124/mol.51.2.301
-
(1997)
Mol. Pharmacol.
, vol.51
, pp. 301-311
-
-
Perlman, S.1
Costa-Neto, C.M.2
Miyakawa, A.A.3
Schambye, H.T.4
Hjorth, S.A.5
Paiva, A.C.M.6
Rivero, R.A.7
Greenlee, W.J.8
Schwartz, T.W.9
-
36
-
-
0037142332
-
Synthesis and Structure-Affinity-Activity Relationships of Novel Benzofuran Derivatives as MT2Melatonin Receptor Selective Ligands
-
Wallez, V.; Durieux-Poissonnier, S.; Chavatte, P.; Boutin, J. A.; Audinot, V.; Nicolas, J.-P.; Bennejean, C.; Delagrange, P.; Renard, P.; Lesieur, D. Synthesis and Structure-Affinity-Activity Relationships of Novel Benzofuran Derivatives as MT2Melatonin Receptor Selective Ligands J. Med. Chem. 2002, 45, 2788-2800 10.1021/jm0005252
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2788-2800
-
-
Wallez, V.1
Durieux-Poissonnier, S.2
Chavatte, P.3
Boutin, J.A.4
Audinot, V.5
Nicolas, J.-P.6
Bennejean, C.7
Delagrange, P.8
Renard, P.9
Lesieur, D.10
-
37
-
-
0037011792
-
α2-Adrenoreceptors Profile Modulation and High Antinociceptive Activity of (S)-(-)-2-[1-(Biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole
-
Gentili, F.; Bousquet, P.; Brasili, L.; Caretto, M.; Carrieri, A.; Dontenwill, M.; Giannella, M.; Marucci, G.; Perfumi, M.; Piergentili, A.; Quaglia, W.; Rascente, C.; Pigini, M. α2-Adrenoreceptors Profile Modulation and High Antinociceptive Activity of (S)-(-)-2-[1-(Biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole J. Med. Chem. 2002, 45, 32-40 10.1021/jm0110082
-
(2002)
J. Med. Chem.
, vol.45
, pp. 32-40
-
-
Gentili, F.1
Bousquet, P.2
Brasili, L.3
Caretto, M.4
Carrieri, A.5
Dontenwill, M.6
Giannella, M.7
Marucci, G.8
Perfumi, M.9
Piergentili, A.10
Quaglia, W.11
Rascente, C.12
Pigini, M.13
-
38
-
-
84906933886
-
GPCR Structures in Drug Design, Emerging Opportunities with New Structures
-
Tautermann, C. S. GPCR Structures in Drug Design, Emerging Opportunities with New Structures Bioorg. Med. Chem. Lett. 2014, 24, 4073-4079 10.1016/j.bmcl.2014.07.009
-
(2014)
Bioorg. Med. Chem. Lett.
, vol.24
, pp. 4073-4079
-
-
Tautermann, C.S.1
-
39
-
-
18244393501
-
Structural Basis for Antagonist-mediated Recruitment of Nuclear Co-repressors by PPAR[alpha]
-
Xu, H. E.; Stanley, T. B.; Montana, V. G.; Lambert, M. H.; Shearer, B. G.; Cobb, J. E.; McKee, D. D.; Galardi, C. M.; Plunket, K. D.; Nolte, R. T.; Parks, D. J.; Moore, J. T.; Kliewer, S. A.; Willson, T. M.; Stimmel, J. B. Structural Basis for Antagonist-mediated Recruitment of Nuclear Co-repressors by PPAR[alpha] Nature 2002, 415, 813-817 10.1038/415813a
-
(2002)
Nature
, vol.415
, pp. 813-817
-
-
Xu, H.E.1
Stanley, T.B.2
Montana, V.G.3
Lambert, M.H.4
Shearer, B.G.5
Cobb, J.E.6
McKee, D.D.7
Galardi, C.M.8
Plunket, K.D.9
Nolte, R.T.10
Parks, D.J.11
Moore, J.T.12
Kliewer, S.A.13
Willson, T.M.14
Stimmel, J.B.15
-
40
-
-
51849099001
-
Discovery of the First Potent and Orally Efficacious Agonist of the Orphan G-Protein Coupled Receptor 119
-
Semple, G.; Fioravanti, B.; Pereira, G.; Calderon, I.; Uy, J.; Choi, K.; Xiong, Y.; Ren, A.; Morgan, M.; Dave, V.; Thomsen, W.; Unett, D. J.; Xing, C.; Bossie, S.; Carroll, C.; Chu, Z.-L.; Grottick, A. J.; Hauser, E. K.; Leonard, J.; Jones, R. M. Discovery of the First Potent and Orally Efficacious Agonist of the Orphan G-Protein Coupled Receptor 119 J. Med. Chem. 2008, 51, 5172-5175 10.1021/jm8006867
-
(2008)
J. Med. Chem.
, vol.51
, pp. 5172-5175
-
-
Semple, G.1
Fioravanti, B.2
Pereira, G.3
Calderon, I.4
Uy, J.5
Choi, K.6
Xiong, Y.7
Ren, A.8
Morgan, M.9
Dave, V.10
Thomsen, W.11
Unett, D.J.12
Xing, C.13
Bossie, S.14
Carroll, C.15
Chu, Z.-L.16
Grottick, A.J.17
Hauser, E.K.18
Leonard, J.19
Jones, R.M.20
more..
-
41
-
-
67349140294
-
In Vivo Effects of a GPR30 Antagonist
-
Dennis, M. K.; Burai, R.; Ramesh, C.; Petrie, W. K.; Alcon, S. N.; Nayak, T. K.; Bologa, C. G.; Leitao, A.; Brailoiu, E.; Deliu, E.; Dun, N. J.; Sklar, L. A.; Hathaway, H. J.; Arterburn, J. B.; Oprea, T. I.; Prossnitz, E. R. In Vivo Effects of a GPR30 Antagonist Nat. Chem. Biol. 2009, 5, 421-427 10.1038/nchembio.168
-
(2009)
Nat. Chem. Biol.
, vol.5
, pp. 421-427
-
-
Dennis, M.K.1
Burai, R.2
Ramesh, C.3
Petrie, W.K.4
Alcon, S.N.5
Nayak, T.K.6
Bologa, C.G.7
Leitao, A.8
Brailoiu, E.9
Deliu, E.10
Dun, N.J.11
Sklar, L.A.12
Hathaway, H.J.13
Arterburn, J.B.14
Oprea, T.I.15
Prossnitz, E.R.16
-
42
-
-
33646366423
-
Virtual and Biomolecular Screening Converge on a Selective Agonist for GPR30
-
Bologa, C. G.; Revankar, C. M.; Young, S. M.; Edwards, B. S.; Arterburn, J. B.; Kiselyov, A. S.; Parker, M. A.; Tkachenko, S. E.; Savchuck, N. P.; Sklar, L. A.; Oprea, T. I.; Prossnitz, E. R. Virtual and Biomolecular Screening Converge on a Selective Agonist for GPR30 Nat. Chem. Biol. 2006, 2, 207-212 10.1038/nchembio775
-
(2006)
Nat. Chem. Biol.
, vol.2
, pp. 207-212
-
-
Bologa, C.G.1
Revankar, C.M.2
Young, S.M.3
Edwards, B.S.4
Arterburn, J.B.5
Kiselyov, A.S.6
Parker, M.A.7
Tkachenko, S.E.8
Savchuck, N.P.9
Sklar, L.A.10
Oprea, T.I.11
Prossnitz, E.R.12
-
43
-
-
81255160989
-
Identification of a GPER/GPR30 Antagonist with Improved Estrogen Receptor Counterselectivity
-
Dennis, M. K.; Field, A. S.; Burai, R.; Ramesh, C.; Petrie, W. K.; Bologa, C. G.; Oprea, T. I.; Yamaguchi, Y.; Hayashi, S.-I.; Sklar, L. A.; Hathaway, H. J.; Arterburn, J. B.; Prossnitz, E. R. Identification of a GPER/GPR30 Antagonist with Improved Estrogen Receptor Counterselectivity J. Steroid Biochem. Mol. Biol. 2011, 127, 358-366 10.1016/j.jsbmb.2011.07.002
-
(2011)
J. Steroid Biochem. Mol. Biol.
, vol.127
, pp. 358-366
-
-
Dennis, M.K.1
Field, A.S.2
Burai, R.3
Ramesh, C.4
Petrie, W.K.5
Bologa, C.G.6
Oprea, T.I.7
Yamaguchi, Y.8
Hayashi, S.-I.9
Sklar, L.A.10
Hathaway, H.J.11
Arterburn, J.B.12
Prossnitz, E.R.13
-
44
-
-
10644271578
-
Structure-Affinity Relationship Study on N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-Piperazinealkylamides, a New Class of 5-Hydroxytryptamine7 Receptor Agents
-
Leopoldo, M.; Berardi, F.; Colabufo, N. A.; Contino, M.; Lacivita, E.; Niso, M.; Perrone, R.; Tortorella, V. Structure-Affinity Relationship Study on N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-Piperazinealkylamides, a New Class of 5-Hydroxytryptamine7 Receptor Agents J. Med. Chem. 2004, 47, 6616-6624 10.1021/jm049702f
-
(2004)
J. Med. Chem.
, vol.47
, pp. 6616-6624
-
-
Leopoldo, M.1
Berardi, F.2
Colabufo, N.A.3
Contino, M.4
Lacivita, E.5
Niso, M.6
Perrone, R.7
Tortorella, V.8
-
45
-
-
79954597841
-
Pharmacological Blockade of 5-HT7 Receptors as a Putative Fast Acting Antidepressant Strategy
-
Mnie-Filali, O.; Faure, C.; Lambas-Senas, L.; Mansari, M. E.; Belblidia, H.; Gondard, E.; Etievant, A.; Scarna, H.; Didier, A.; Berod, A.; Blier, P.; Haddjeri, N. Pharmacological Blockade of 5-HT7 Receptors as a Putative Fast Acting Antidepressant Strategy Neuropsychopharmacology 2011, 36, 1275-1288 10.1038/npp.2011.13
-
(2011)
Neuropsychopharmacology
, vol.36
, pp. 1275-1288
-
-
Mnie-Filali, O.1
Faure, C.2
Lambas-Senas, L.3
Mansari, M.E.4
Belblidia, H.5
Gondard, E.6
Etievant, A.7
Scarna, H.8
Didier, A.9
Berod, A.10
Blier, P.11
Haddjeri, N.12
-
46
-
-
84876800938
-
Targeted Inhibition of Serotonin Type 7 (5-HT7) Receptor Function Modulates Immune Responses and Reduces the Severity of Intestinal Inflammation
-
Kim, J. J.; Bridle, B. W.; Ghia, J.-E.; Wang, H.; Syed, S. N.; Manocha, M. M.; Rengasamy, P.; Shajib, M. S.; Wan, Y.; Hedlund, P. B.; Khan, W. I. Targeted Inhibition of Serotonin Type 7 (5-HT7) Receptor Function Modulates Immune Responses and Reduces the Severity of Intestinal Inflammation J. Immunol. 2013, 190, 4795-4804 10.4049/jimmunol.1201887
-
(2013)
J. Immunol.
, vol.190
, pp. 4795-4804
-
-
Kim, J.J.1
Bridle, B.W.2
Ghia, J.-E.3
Wang, H.4
Syed, S.N.5
Manocha, M.M.6
Rengasamy, P.7
Shajib, M.S.8
Wan, Y.9
Hedlund, P.B.10
Khan, W.I.11
-
47
-
-
0037068473
-
Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT1A Receptors
-
Orús, L.; Pérez-Silanes, S.; Oficialdegui, A.-M.; Martínez-Esparza, J.; Del Castillo, J.-C.; Mourelle, M.; Langer, T.; Guccione, S.; Donzella, G.; Krovat, E. M.; Poptodorov, K.; Lasheras, B.; Ballaz, S.; Hervías, I.; Tordera, R.; Del Río, J.; Monge, A. Synthesis and Molecular Modeling of New 1-Aryl-3-[4-arylpiperazin-1-yl]-1-propane Derivatives with High Affinity at the Serotonin Transporter and at 5-HT1A Receptors J. Med. Chem. 2002, 45, 4128-4139 10.1021/jm0111200
-
(2002)
J. Med. Chem.
, vol.45
, pp. 4128-4139
-
-
Orús, L.1
Pérez-Silanes, S.2
Oficialdegui, A.-M.3
Martínez-Esparza, J.4
Del Castillo, J.-C.5
Mourelle, M.6
Langer, T.7
Guccione, S.8
Donzella, G.9
Krovat, E.M.10
Poptodorov, K.11
Lasheras, B.12
Ballaz, S.13
Hervías, I.14
Tordera, R.15
Del Río, J.16
Monge, A.17
-
48
-
-
84908374192
-
Potent Heterocyclic Ligands for Human Complement C3a Receptor
-
Reid, R. C.; Yau, M.-K.; Singh, R.; Hamidon, J. K.; Lim, J.; Stoermer, M. J.; Fairlie, D. P. Potent Heterocyclic Ligands for Human Complement C3a Receptor J. Med. Chem. 2014, 57, 8459-8470 10.1021/jm500956p
-
(2014)
J. Med. Chem.
, vol.57
, pp. 8459-8470
-
-
Reid, R.C.1
Yau, M.-K.2
Singh, R.3
Hamidon, J.K.4
Lim, J.5
Stoermer, M.J.6
Fairlie, D.P.7
-
49
-
-
32344450371
-
Pyrrolizidine Esters and Amides as 5-HT4 Receptor Agonists and Antagonists
-
Becker, D. P.; Flynn, D. L.; Moormann, A. E.; Nosal, R.; Villamil, C. I.; Loeffler, R.; Gullikson, G. W.; Moummi, C.; Yang, D.-C. Pyrrolizidine Esters and Amides as 5-HT4 Receptor Agonists and Antagonists J. Med. Chem. 2006, 49, 1125-1139 10.1021/jm0509501
-
(2006)
J. Med. Chem.
, vol.49
, pp. 1125-1139
-
-
Becker, D.P.1
Flynn, D.L.2
Moormann, A.E.3
Nosal, R.4
Villamil, C.I.5
Loeffler, R.6
Gullikson, G.W.7
Moummi, C.8
Yang, D.-C.9
-
50
-
-
19944430163
-
Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists
-
Cole, D. C.; Lennox, W. J.; Lombardi, S.; Ellingboe, J. W.; Bernotas, R. C.; Tawa, G. J.; Mazandarani, H.; Smith, D. L.; Zhang, G.; Coupet, J.; Schechter, L. E. Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists J. Med. Chem. 2005, 48, 353-356 10.1021/jm049243i
-
(2005)
J. Med. Chem.
, vol.48
, pp. 353-356
-
-
Cole, D.C.1
Lennox, W.J.2
Lombardi, S.3
Ellingboe, J.W.4
Bernotas, R.C.5
Tawa, G.J.6
Mazandarani, H.7
Smith, D.L.8
Zhang, G.9
Coupet, J.10
Schechter, L.E.11
-
51
-
-
77249089823
-
Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist
-
Liu, Z.; Zhang, H.; Ye, N.; Zhang, J.; Wu, Q.; Sun, P.; Li, L.; Zhen, X.; Zhang, A. Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist J. Med. Chem. 2010, 53, 1319-1328 10.1021/jm9015763
-
(2010)
J. Med. Chem.
, vol.53
, pp. 1319-1328
-
-
Liu, Z.1
Zhang, H.2
Ye, N.3
Zhang, J.4
Wu, Q.5
Sun, P.6
Li, L.7
Zhen, X.8
Zhang, A.9
-
52
-
-
32344436490
-
Novel Benzodiazepine Photoaffinity Probe Stereoselectively Labels a Site Deep within the Membrane-Spanning Domain of the Cholecystokinin Receptor
-
Hadac, E. M.; Dawson, E. S.; Darrow, J. W.; Sugg, E. E.; Lybrand, T. P.; Miller, L. J. Novel Benzodiazepine Photoaffinity Probe Stereoselectively Labels a Site Deep within the Membrane-Spanning Domain of the Cholecystokinin Receptor J. Med. Chem. 2006, 49, 850-863 10.1021/jm049072h
-
(2006)
J. Med. Chem.
, vol.49
, pp. 850-863
-
-
Hadac, E.M.1
Dawson, E.S.2
Darrow, J.W.3
Sugg, E.E.4
Lybrand, T.P.5
Miller, L.J.6
-
53
-
-
35649017162
-
Synthesis and Characterization of Pyrrolidine Derivatives as Potent Agonists of the Human Melanocortin-4 Receptor
-
Jiang, W.; Tran, J. A.; Tucci, F. C.; Fleck, B. A.; Hoare, S. R.; Markison, S.; Wen, J.; Chen, C. W.; Marinkovic, D.; Arellano, M.; Foster, A. C.; Chen, C. Synthesis and Characterization of Pyrrolidine Derivatives as Potent Agonists of the Human Melanocortin-4 Receptor Bioorg. Med. Chem. Lett. 2007, 17, 6546-6552 10.1016/j.bmcl.2007.09.079
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 6546-6552
-
-
Jiang, W.1
Tran, J.A.2
Tucci, F.C.3
Fleck, B.A.4
Hoare, S.R.5
Markison, S.6
Wen, J.7
Chen, C.W.8
Marinkovic, D.9
Arellano, M.10
Foster, A.C.11
Chen, C.12
-
54
-
-
37549009542
-
Identification and Characterization of Pyrrolidine Diastereoisomers as Potent Functional Agonists and Antagonists of the Human Melanocortin-4 Receptor
-
Chen, C.; Jiang, W.; Tran, J. A.; Tucci, F. C.; Fleck, B. A.; Markison, S.; Wen, J.; Madan, A.; Hoare, S. R.; Foster, A. C.; Marinkovic, D.; Chen, C. W.; Arellano, M.; Saunders, J. Identification and Characterization of Pyrrolidine Diastereoisomers as Potent Functional Agonists and Antagonists of the Human Melanocortin-4 Receptor Bioorg. Med. Chem. Lett. 2008, 18, 129-136 10.1016/j.bmcl.2007.10.115
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 129-136
-
-
Chen, C.1
Jiang, W.2
Tran, J.A.3
Tucci, F.C.4
Fleck, B.A.5
Markison, S.6
Wen, J.7
Madan, A.8
Hoare, S.R.9
Foster, A.C.10
Marinkovic, D.11
Chen, C.W.12
Arellano, M.13
Saunders, J.14
-
55
-
-
84882530434
-
Conformational Restriction and/or Steric Hindrance in Medicinal Chemistry
-
3rd ed. Wermuth, C. G. Academic Press: New York, Chapter 17
-
Mann, A., Conformational Restriction and/or Steric Hindrance in Medicinal Chemistry. In The Practice of Medicinal Chemistry, 3rd ed.; Wermuth, C. G., Ed.; Academic Press: New York, 2008; Chapter 17, pp 363-379.
-
(2008)
The Practice of Medicinal Chemistry
, pp. 363-379
-
-
Mann, A.1
-
56
-
-
33845477636
-
Elucidation of the Bioactive Conformation of the N-Substituted trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidine Class of μ-Opioid Receptor Antagonists
-
Le Bourdonnec, B.; Goodman, A. J.; Michaut, M.; Ye, H.-F.; Graczyk, T. M.; Belanger, S.; Herbertz, T.; Yap, G. P. A.; DeHaven, R. N.; Dolle, R. E. Elucidation of the Bioactive Conformation of the N-Substituted trans-3,4-Dimethyl-4-(3-hydroxyphenyl)piperidine Class of μ-Opioid Receptor Antagonists J. Med. Chem. 2006, 49, 7278-7289 10.1021/jm060486f
-
(2006)
J. Med. Chem.
, vol.49
, pp. 7278-7289
-
-
Le Bourdonnec, B.1
Goodman, A.J.2
Michaut, M.3
Ye, H.-F.4
Graczyk, T.M.5
Belanger, S.6
Herbertz, T.7
Yap, G.P.A.8
DeHaven, R.N.9
Dolle, R.E.10
-
57
-
-
0037179640
-
Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary
-
Gao, Z.-G.; Kim, S.-K.; Biadatti, T.; Chen, W.; Lee, K.; Barak, D.; Kim, S. G.; Johnson, C. R.; Jacobson, K. A. Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary J. Med. Chem. 2002, 45, 4471-4484 10.1021/jm020211+
-
(2002)
J. Med. Chem.
, vol.45
, pp. 4471-4484
-
-
Gao, Z.-G.1
Kim, S.-K.2
Biadatti, T.3
Chen, W.4
Lee, K.5
Barak, D.6
Kim, S.G.7
Johnson, C.R.8
Jacobson, K.A.9
-
58
-
-
77953476011
-
Agonist/Antagonist Modulation in a Series of 2-Aryl Benzimidazole H4 Receptor Ligands
-
Savall, B. M.; Edwards, J. P.; Venable, J. D.; Buzard, D. J.; Thurmond, R.; Hack, M.; McGovern, P. Agonist/Antagonist Modulation in a Series of 2-Aryl Benzimidazole H4 Receptor Ligands Bioorg. Med. Chem. Lett. 2010, 20, 3367-3371 10.1016/j.bmcl.2010.04.017
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 3367-3371
-
-
Savall, B.M.1
Edwards, J.P.2
Venable, J.D.3
Buzard, D.J.4
Thurmond, R.5
Hack, M.6
McGovern, P.7
-
59
-
-
0033548623
-
Role of Aromaticity of Agonist Switches of Angiotensin II in the Activation of the AT1 Receptor
-
Miura, S.-i.; Feng, Y.-H.; Husain, A.; Karnik, S. S. Role of Aromaticity of Agonist Switches of Angiotensin II in the Activation of the AT1 Receptor J. Biol. Chem. 1999, 274, 7103-7110 10.1074/jbc.274.11.7103
-
(1999)
J. Biol. Chem.
, vol.274
, pp. 7103-7110
-
-
Miura S.-i.1
Feng, Y.-H.2
Husain, A.3
Karnik, S.S.4
-
60
-
-
0022450133
-
Amino-Aromatic Interactions in Proteins
-
Burley, S. K.; Petsko, G. A. Amino-Aromatic Interactions in Proteins FEBS Lett. 1986, 203, 139-143 10.1016/0014-5793(86)80730-X
-
(1986)
FEBS Lett.
, vol.203
, pp. 139-143
-
-
Burley, S.K.1
Petsko, G.A.2
-
61
-
-
84862249834
-
Small Molecules with Similar Structures Exhibit Agonist, Neutral Antagonist or Inverse Agonist Activity toward Angiotensin II Type 1 Receptor
-
Miura, S.-i.; Kiya, Y.; Hanzawa, H.; Nakao, N.; Fujino, M.; Imaizumi, S.; Matsuo, Y.; Yanagisawa, H.; Koike, H.; Komuro, I.; Karnik, S. S.; Saku, K. Small Molecules with Similar Structures Exhibit Agonist, Neutral Antagonist or Inverse Agonist Activity toward Angiotensin II Type 1 Receptor PLoS One 2012, 7, e37974 10.1371/journal.pone.0037974
-
(2012)
PLoS One
, vol.7
-
-
Miura S.-i.1
Kiya, Y.2
Hanzawa, H.3
Nakao, N.4
Fujino, M.5
Imaizumi, S.6
Matsuo, Y.7
Yanagisawa, H.8
Koike, H.9
Komuro, I.10
Karnik, S.S.11
Saku, K.12
-
62
-
-
33845325214
-
Dioxane and Oxathiane Nuclei: Suitable Substructures for Muscarinic Agonists
-
Piergentili, A.; Quaglia, W.; Giannella, M.; Bello, F. D.; Bruni, B.; Buccioni, M.; Carrieri, A.; Ciattini, S. Dioxane and Oxathiane Nuclei: Suitable Substructures for Muscarinic Agonists Bioorg. Med. Chem. 2007, 15, 886-896 10.1016/j.bmc.2006.10.040
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 886-896
-
-
Piergentili, A.1
Quaglia, W.2
Giannella, M.3
Bello, F.D.4
Bruni, B.5
Buccioni, M.6
Carrieri, A.7
Ciattini, S.8
-
63
-
-
84857387188
-
1,4-Dioxane, a Suitable Scaffold for the Development of Novel M3Muscarinic Receptor Antagonists
-
Del Bello, F.; Barocelli, E.; Bertoni, S.; Bonifazi, A.; Camalli, M.; Campi, G.; Giannella, M.; Matucci, R.; Nesi, M.; Pigini, M.; Quaglia, W.; Piergentili, A. 1,4-Dioxane, a Suitable Scaffold for the Development of Novel M3Muscarinic Receptor Antagonists J. Med. Chem. 2012, 55, 1783-1787 10.1021/jm2013216
-
(2012)
J. Med. Chem.
, vol.55
, pp. 1783-1787
-
-
Del Bello, F.1
Barocelli, E.2
Bertoni, S.3
Bonifazi, A.4
Camalli, M.5
Campi, G.6
Giannella, M.7
Matucci, R.8
Nesi, M.9
Pigini, M.10
Quaglia, W.11
Piergentili, A.12
-
64
-
-
2442650309
-
Discovery of the First Non-Peptide Full Agonists for the Human Bradykinin B2 Receptor Incorporating 4-(2-Picolyloxy)quinoline and 1-(2-Picolyl)benzimidazole Frameworks
-
Sawada, Y.; Kayakiri, H.; Abe, Y.; Mizutani, T.; Inamura, N.; Asano, M.; Hatori, C.; Aramori, I.; Oku, T.; Tanaka, H. Discovery of the First Non-Peptide Full Agonists for the Human Bradykinin B2 Receptor Incorporating 4-(2-Picolyloxy)quinoline and 1-(2-Picolyl)benzimidazole Frameworks J. Med. Chem. 2004, 47, 2853-2863 10.1021/jm030468n
-
(2004)
J. Med. Chem.
, vol.47
, pp. 2853-2863
-
-
Sawada, Y.1
Kayakiri, H.2
Abe, Y.3
Mizutani, T.4
Inamura, N.5
Asano, M.6
Hatori, C.7
Aramori, I.8
Oku, T.9
Tanaka, H.10
-
65
-
-
2342505852
-
A New Class of Nonpeptide Bradykinin B2 Receptor Ligand, Incorporating a 4-Aminoquinoline Framework. Identification of a Key Pharmacophore to Determine Species Difference and Agonist/Antagonist Profile
-
Sawada, Y.; Kayakiri, H.; Abe, Y.; Mizutani, T.; Inamura, N.; Asano, M.; Aramori, I.; Hatori, C.; Oku, T.; Tanaka, H. A New Class of Nonpeptide Bradykinin B2 Receptor Ligand, Incorporating a 4-Aminoquinoline Framework. Identification of a Key Pharmacophore To Determine Species Difference and Agonist/Antagonist Profile J. Med. Chem. 2004, 47, 2667-2677 10.1021/jm030326t
-
(2004)
J. Med. Chem.
, vol.47
, pp. 2667-2677
-
-
Sawada, Y.1
Kayakiri, H.2
Abe, Y.3
Mizutani, T.4
Inamura, N.5
Asano, M.6
Aramori, I.7
Hatori, C.8
Oku, T.9
Tanaka, H.10
-
66
-
-
15444343988
-
Pharmacological Characterization of a Nonpeptide Bradykinin B2 Receptor Antagonist, FR165649, and Agonist, FR190997
-
Asano, M.; Hatori, C.; Sawai, H.; Johki, S.; Inamura, N.; Kayakiri, H.; Satoh, S.; Abe, Y.; Inoue, T.; Sawada, Y.; Mizutani, T.; Oku, T.; Nakahara, K. Pharmacological Characterization of a Nonpeptide Bradykinin B2 Receptor Antagonist, FR165649, and Agonist, FR190997 Br. J. Pharmacol. 1998, 124, 441-446 10.1038/sj.bjp.0701813
-
(1998)
Br. J. Pharmacol.
, vol.124
, pp. 441-446
-
-
Asano, M.1
Hatori, C.2
Sawai, H.3
Johki, S.4
Inamura, N.5
Kayakiri, H.6
Satoh, S.7
Abe, Y.8
Inoue, T.9
Sawada, Y.10
Mizutani, T.11
Oku, T.12
Nakahara, K.13
-
67
-
-
50249099198
-
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 2. Synthesis and Structure-Activity Relationship of Potent and Selective Cannabinoid-2 Receptor Agonists Endowed with Analgesic Activity in Vivo
-
Pasquini, S.; Botta, L.; Semeraro, T.; Mugnaini, C.; Ligresti, A.; Palazzo, E.; Maione, S.; Di Marzo, V.; Corelli, F. Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 2. Synthesis and Structure-Activity Relationship of Potent and Selective Cannabinoid-2 Receptor Agonists Endowed with Analgesic Activity in Vivo J. Med. Chem. 2008, 51, 5075-5084 10.1021/jm800552f
-
(2008)
J. Med. Chem.
, vol.51
, pp. 5075-5084
-
-
Pasquini, S.1
Botta, L.2
Semeraro, T.3
Mugnaini, C.4
Ligresti, A.5
Palazzo, E.6
Maione, S.7
Di Marzo, V.8
Corelli, F.9
-
68
-
-
77955866101
-
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 3. Synthesis, Structure-Affinity Relationships, and Pharmacological Characterization of 6-Substituted 4-Quinolone-3-carboxamides as Highly Selective Cannabinoid-2 Receptor Ligands
-
Pasquini, S.; Ligresti, A.; Mugnaini, C.; Semeraro, T.; Cicione, L.; De Rosa, M.; Guida, F.; Luongo, L.; De Chiaro, M.; Cascio, M. G.; Bolognini, D.; Marini, P.; Pertwee, R.; Maione, S.; Marzo, V. D.; Corelli, F. Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 3. Synthesis, Structure-Affinity Relationships, and Pharmacological Characterization of 6-Substituted 4-Quinolone-3-carboxamides as Highly Selective Cannabinoid-2 Receptor Ligands J. Med. Chem. 2010, 53, 5915-5928 10.1021/jm100123x
-
(2010)
J. Med. Chem.
, vol.53
, pp. 5915-5928
-
-
Pasquini, S.1
Ligresti, A.2
Mugnaini, C.3
Semeraro, T.4
Cicione, L.5
De Rosa, M.6
Guida, F.7
Luongo, L.8
De Chiaro, M.9
Cascio, M.G.10
Bolognini, D.11
Marini, P.12
Pertwee, R.13
Maione, S.14
Marzo, V.D.15
Corelli, F.16
-
69
-
-
77649339814
-
In Vitro and in Vivo Pharmacological Characterization of Two Novel Selective Cannabinoid CB2 Receptor Inverse Agonists
-
Cascio, M. G.; Bolognini, D.; Pertwee, R. G.; Palazzo, E.; Corelli, F.; Pasquini, S.; Di Marzo, V.; Maione, S. In Vitro and in Vivo Pharmacological Characterization of Two Novel Selective Cannabinoid CB2 Receptor Inverse Agonists Pharmacol. Res. 2010, 61, 349-354 10.1016/j.phrs.2009.11.011
-
(2010)
Pharmacol. Res.
, vol.61
, pp. 349-354
-
-
Cascio, M.G.1
Bolognini, D.2
Pertwee, R.G.3
Palazzo, E.4
Corelli, F.5
Pasquini, S.6
Di Marzo, V.7
Maione, S.8
-
70
-
-
19944432031
-
Identification of Agonists and Antagonists of the Human Melanocortin-4 Receptor from Piperazinebenzylamines
-
Tran, J. A.; Pontillo, J.; Arellano, M.; White, N. S.; Fleck, B. A.; Marinkovic, D.; Tucci, F. C.; Lanier, M.; Nelson, J.; Saunders, J.; Foster, A. C.; Chen, C. Identification of Agonists and Antagonists of the Human Melanocortin-4 Receptor from Piperazinebenzylamines Bioorg. Med. Chem. Lett. 2005, 15, 833-837 10.1016/j.bmcl.2004.10.096
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 833-837
-
-
Tran, J.A.1
Pontillo, J.2
Arellano, M.3
White, N.S.4
Fleck, B.A.5
Marinkovic, D.6
Tucci, F.C.7
Lanier, M.8
Nelson, J.9
Saunders, J.10
Foster, A.C.11
Chen, C.12
-
71
-
-
0346729873
-
Synthesis of Novel Melanocortin 4 Receptor Agonists and Antagonists Containing a Succinamide Core
-
Xi, N.; Hale, C.; Kelly, M. G.; Norman, M. H.; Stec, M.; Xu, S.; Baumgartner, J. W.; Fotsch, C. Synthesis of Novel Melanocortin 4 Receptor Agonists and Antagonists Containing a Succinamide Core Bioorg. Med. Chem. Lett. 2004, 14, 377-381 10.1016/j.bmcl.2003.10.056
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 377-381
-
-
Xi, N.1
Hale, C.2
Kelly, M.G.3
Norman, M.H.4
Stec, M.5
Xu, S.6
Baumgartner, J.W.7
Fotsch, C.8
-
72
-
-
84866863717
-
7-Alkyl-3-benzylcoumarins: A Versatile Scaffold for the Development of Potent and Selective Cannabinoid Receptor Agonists and Antagonists
-
Rempel, V.; Volz, N.; Hinz, S.; Karcz, T.; Meliciani, I.; Nieger, M.; Wenzel, W.; Bräse, S.; Müller, C. E. 7-Alkyl-3-benzylcoumarins: A Versatile Scaffold for the Development of Potent and Selective Cannabinoid Receptor Agonists and Antagonists J. Med. Chem. 2012, 55, 7967-7977 10.1021/jm3008213
-
(2012)
J. Med. Chem.
, vol.55
, pp. 7967-7977
-
-
Rempel, V.1
Volz, N.2
Hinz, S.3
Karcz, T.4
Meliciani, I.5
Nieger, M.6
Wenzel, W.7
Bräse, S.8
Müller, C.E.9
-
73
-
-
0037021476
-
Methoxy Group as an Acceptor of Proton in Hydrogen Bonds
-
Palusiak, M.; Grabowski, S. J. Methoxy Group as an Acceptor of Proton in Hydrogen Bonds J. Mol. Struct. 2002, 642, 97-104 10.1016/S0022-2860(02)00406-4
-
(2002)
J. Mol. Struct.
, vol.642
, pp. 97-104
-
-
Palusiak, M.1
Grabowski, S.J.2
-
74
-
-
34247239893
-
Synthesis and Pharmacological in Vitro and in Vivo Evaluations of Novel Triazole Derivatives as Ligands of the Ghrelin Receptor. 1
-
Demange, L.; Boeglin, D.; Moulin, A.; Mousseaux, D.; Ryan, J.; Bergé, G.; Gagne, D.; Heitz, A.; Perrissoud, D.; Locatelli, V.; Torsello, A.; Galleyrand, J.-C.; Fehrentz, J.-A.; Martinez, J. Synthesis and Pharmacological in Vitro and in Vivo Evaluations of Novel Triazole Derivatives as Ligands of the Ghrelin Receptor. 1 J. Med. Chem. 2007, 50, 1939-1957 10.1021/jm070024h
-
(2007)
J. Med. Chem.
, vol.50
, pp. 1939-1957
-
-
Demange, L.1
Boeglin, D.2
Moulin, A.3
Mousseaux, D.4
Ryan, J.5
Bergé, G.6
Gagne, D.7
Heitz, A.8
Perrissoud, D.9
Locatelli, V.10
Torsello, A.11
Galleyrand, J.-C.12
Fehrentz, J.-A.13
Martinez, J.14
-
75
-
-
36148975300
-
Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations
-
Moulin, A.; Demange, L.; Bergé, G.; Gagne, D.; Ryan, J.; Mousseaux, D.; Heitz, A.; Perrissoud, D.; Locatelli, V.; Torsello, A.; Galleyrand, J.-C.; Fehrentz, J.-A.; Martinez, J. Toward Potent Ghrelin Receptor Ligands Based on Trisubstituted 1,2,4-Triazole Structure. 2. Synthesis and Pharmacological in Vitro and in Vivo Evaluations J. Med. Chem. 2007, 50, 5790-5806 10.1021/jm0704550
-
(2007)
J. Med. Chem.
, vol.50
, pp. 5790-5806
-
-
Moulin, A.1
Demange, L.2
Bergé, G.3
Gagne, D.4
Ryan, J.5
Mousseaux, D.6
Heitz, A.7
Perrissoud, D.8
Locatelli, V.9
Torsello, A.10
Galleyrand, J.-C.11
Fehrentz, J.-A.12
Martinez, J.13
-
76
-
-
79953213637
-
Molecular Switches" on mGluR Allosteric Ligands That Modulate Modes of Pharmacology
-
Wood, M. R.; Hopkins, C. R.; Brogan, J. T.; Conn, P. J.; Lindsley, C. W. Molecular Switches" on mGluR Allosteric Ligands That Modulate Modes of Pharmacology Biochemistry 2011, 50, 2403-2410 10.1021/bi200129s
-
(2011)
Biochemistry
, vol.50
, pp. 2403-2410
-
-
Wood, M.R.1
Hopkins, C.R.2
Brogan, J.T.3
Conn, P.J.4
Lindsley, C.W.5
-
77
-
-
84907811678
-
A Double Effect Molecular Switch Leads to a Novel Potent Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5
-
Gomez-Santacana, X.; Rovira, X.; Dalton, J. A.; Goudet, C.; Pin, J. P.; Gorostiza, P.; Giraldo, J.; Llebaria, A. A Double Effect Molecular Switch Leads to a Novel Potent Negative Allosteric Modulator of Metabotropic Glutamate Receptor 5 MedChemComm 2014, 5, 1548-1554 10.1039/C4MD00208C
-
(2014)
MedChemComm
, vol.5
, pp. 1548-1554
-
-
Gomez-Santacana, X.1
Rovira, X.2
Dalton, J.A.3
Goudet, C.4
Pin, J.P.5
Gorostiza, P.6
Giraldo, J.7
Llebaria, A.8
-
78
-
-
84865113433
-
N-Aryl Pyrrolidinonyl Oxadiazoles as Potent mGluR5 Positive Allosteric Modulators
-
Packiarajan, M.; Mazza Ferreira, C. G.; Hong, S.-P.; White, A. D.; Chandrasena, G.; Pu, X.; Brodbeck, R. M.; Robichaud, A. J. N-Aryl Pyrrolidinonyl Oxadiazoles as Potent mGluR5 Positive Allosteric Modulators Bioorg. Med. Chem. Lett. 2012, 22, 5658-5662 10.1016/j.bmcl.2012.06.094
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 5658-5662
-
-
Packiarajan, M.1
Mazza Ferreira, C.G.2
Hong, S.-P.3
White, A.D.4
Chandrasena, G.5
Pu, X.6
Brodbeck, R.M.7
Robichaud, A.J.8
-
79
-
-
84907367626
-
Biased Agonism at G Protein-Coupled Receptors: the Promise and the Challenges - A Medicinal Chemistry Perspective
-
Shonberg, J.; Lopez, L.; Scammells, P. J.; Christopoulos, A.; Capuano, B.; Lane, J. R. Biased Agonism at G Protein-Coupled Receptors: The Promise and the Challenges-A Medicinal Chemistry Perspective Med. Res. Rev. 2014, 34, 1286-1330 10.1002/med.21318
-
(2014)
Med. Res. Rev.
, vol.34
, pp. 1286-1330
-
-
Shonberg, J.1
Lopez, L.2
Scammells, P.J.3
Christopoulos, A.4
Capuano, B.5
Lane, J.R.6
-
80
-
-
58849150709
-
Replacing Alkyl Sulfonamide with Aromatic Sulfonamide in Sulfonamide-type RXR Agonists Favors Switch Towards Antagonist Activity
-
Morishita, K.-i.; Yakushiji, N.; Ohsawa, F.; Takamatsu, K.; Matsuura, N.; Makishima, M.; Kawahata, M.; Yamaguchi, K.; Tai, A.; Sasaki, K.; Kakuta, H. Replacing Alkyl Sulfonamide with Aromatic Sulfonamide in Sulfonamide-type RXR Agonists Favors Switch Towards Antagonist Activity Bioorg. Med. Chem. Lett. 2009, 19, 1001-1003 10.1016/j.bmcl.2008.11.086
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 1001-1003
-
-
Morishita K.-i.1
Yakushiji, N.2
Ohsawa, F.3
Takamatsu, K.4
Matsuura, N.5
Makishima, M.6
Kawahata, M.7
Yamaguchi, K.8
Tai, A.9
Sasaki, K.10
Kakuta, H.11
-
81
-
-
72049089819
-
Oxime Derivatives Related to AP18: Agonists and Antagonists of the TRPA1 Receptor
-
DeFalco, J.; Steiger, D.; Gustafson, A.; Emerling, D. E.; Kelly, M. G.; Duncton, M. A. J. Oxime Derivatives Related to AP18: Agonists and Antagonists of the TRPA1 Receptor Bioorg. Med. Chem. Lett. 2010, 20, 276-279 10.1016/j.bmcl.2009.10.113
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 276-279
-
-
Defalco, J.1
Steiger, D.2
Gustafson, A.3
Emerling, D.E.4
Kelly, M.G.5
Duncton, M.A.J.6
-
82
-
-
84865516835
-
Discovery and Optimization of a Series of Liver X Receptor Antagonists
-
Jiao, X.; Kopecky, D. J.; Fisher, B.; Piper, D. E.; Labelle, M.; McKendry, S.; Harrison, M.; Jones, S.; Jaen, J.; Shiau, A. K.; Escaron, P.; Danao, J.; Chai, A.; Coward, P.; Kayser, F. Discovery and Optimization of a Series of Liver X Receptor Antagonists Bioorg. Med. Chem. Lett. 2012, 22, 5966-5970 10.1016/j.bmcl.2012.07.048
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 5966-5970
-
-
Jiao, X.1
Kopecky, D.J.2
Fisher, B.3
Piper, D.E.4
Labelle, M.5
McKendry, S.6
Harrison, M.7
Jones, S.8
Jaen, J.9
Shiau, A.K.10
Escaron, P.11
Danao, J.12
Chai, A.13
Coward, P.14
Kayser, F.15
-
83
-
-
84888862507
-
Substituted Phenyl as a Steroid A-ring Mimetic: Providing Agonist Activity to a Class of Arylsulfonamide Nonsteroidal Glucocorticoid Ligands
-
DiSalvo, D.; Kuzmich, D.; Bentzien, J.; Regan, J.; Kukulka, A.; Fadra-Khan, T.; Nelson, R.; Harcken, C.; Thomson, D.; Nabozny, G. Substituted Phenyl as a Steroid A-ring Mimetic: Providing Agonist Activity to a Class of Arylsulfonamide Nonsteroidal Glucocorticoid Ligands Bioorg. Med. Chem. Lett. 2013, 23, 6645-6649 10.1016/j.bmcl.2013.10.047
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 6645-6649
-
-
Disalvo, D.1
Kuzmich, D.2
Bentzien, J.3
Regan, J.4
Kukulka, A.5
Fadra-Khan, T.6
Nelson, R.7
Harcken, C.8
Thomson, D.9
Nabozny, G.10
-
84
-
-
83455258276
-
Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB
-
Nakayama, M.; Yamada, S.; Ohsawa, F.; Ohta, Y.; Kawata, K.; Makishima, M.; Kakuta, H. Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB ACS Med. Chem. Lett. 2011, 2, 896-900 10.1021/ml200197e
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 896-900
-
-
Nakayama, M.1
Yamada, S.2
Ohsawa, F.3
Ohta, Y.4
Kawata, K.5
Makishima, M.6
Kakuta, H.7
-
85
-
-
16844371411
-
Hammett Analysis of Selective Thyroid Hormone Receptor Modulators Reveals Structural and Electronic Requirements for Hormone Antagonists
-
Nguyen, N.-H.; Apriletti, J. W.; Baxter, J. D.; Scanlan, T. S. Hammett Analysis of Selective Thyroid Hormone Receptor Modulators Reveals Structural and Electronic Requirements for Hormone Antagonists J. Am. Chem. Soc. 2005, 127, 4599-4608 10.1021/ja0440093
-
(2005)
J. Am. Chem. Soc.
, vol.127
, pp. 4599-4608
-
-
Nguyen, N.-H.1
Apriletti, J.W.2
Baxter, J.D.3
Scanlan, T.S.4
-
86
-
-
36849024302
-
Modulators of the Structural Dynamics of the Retinoid X Receptor to Reveal Receptor Function
-
Nahoum, V.; Pérez, E.; Germain, P.; Rodríguez-Barrios, F.; Manzo, F.; Kammerer, S.; Lemaire, G.; Hirsch, O.; Royer, C. A.; Gronemeyer, H.; de Lera, A. R.; Bourguet, W. Modulators of the Structural Dynamics of the Retinoid X Receptor to Reveal Receptor Function Proc. Natl. Acad. Sci. U. S. A. 2007, 104, 17323-17328 10.1073/pnas.0705356104
-
(2007)
Proc. Natl. Acad. Sci. U. S. A.
, vol.104
, pp. 17323-17328
-
-
Nahoum, V.1
Pérez, E.2
Germain, P.3
Rodríguez-Barrios, F.4
Manzo, F.5
Kammerer, S.6
Lemaire, G.7
Hirsch, O.8
Royer, C.A.9
Gronemeyer, H.10
De Lera, A.R.11
Bourguet, W.12
-
87
-
-
0038460841
-
N-(3-Acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea Analogues: Novel Potent and High Affinity Antagonists and Partial Antagonists of the Vanilloid Receptor
-
Lee, J.; Lee, J.; Kang, M.; Shin, M.; Kim, J.-M.; Kang, S.-U.; Lim, J.-O.; Choi, H.-K.; Suh, Y.-G.; Park, H.-G.; Oh, U.; Kim, H.-D.; Park, Y.-H.; Ha, H.-J.; Kim, Y.-H.; Toth, A.; Wang, Y.; Tran, R.; Pearce, L. V.; Lundberg, D. J.; Blumberg, P. M. N-(3-Acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea Analogues: Novel Potent and High Affinity Antagonists and Partial Antagonists of the Vanilloid Receptor J. Med. Chem. 2003, 46, 3116-3126 10.1021/jm030089u
-
(2003)
J. Med. Chem.
, vol.46
, pp. 3116-3126
-
-
Lee, J.1
Lee, J.2
Kang, M.3
Shin, M.4
Kim, J.-M.5
Kang, S.-U.6
Lim, J.-O.7
Choi, H.-K.8
Suh, Y.-G.9
Park, H.-G.10
Oh, U.11
Kim, H.-D.12
Park, Y.-H.13
Ha, H.-J.14
Kim, Y.-H.15
Toth, A.16
Wang, Y.17
Tran, R.18
Pearce, L.V.19
Lundberg, D.J.20
Blumberg, P.M.21
more..
-
88
-
-
41149102488
-
Design, Synthesis, and SAR of New Pyrrole-Oxindole Progesterone Receptor Modulators Leading to 5-(7-Fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348)
-
Fensome, A.; Adams, W. R.; Adams, A. L.; Berrodin, T. J.; Cohen, J.; Huselton, C.; Illenberger, A.; Kern, J. C.; Hudak, V. A.; Marella, M. A.; Melenski, E. G.; McComas, C. C.; Mugford, C. A.; Slayden, O. D.; Yudt, M.; Zhang, Z.; Zhang, P.; Zhu, Y.; Winneker, R. C.; Wrobel, J. E. Design, Synthesis, and SAR of New Pyrrole-Oxindole Progesterone Receptor Modulators Leading to 5-(7-Fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348) J. Med. Chem. 2008, 51, 1861-1873 10.1021/jm701080t
-
(2008)
J. Med. Chem.
, vol.51
, pp. 1861-1873
-
-
Fensome, A.1
Adams, W.R.2
Adams, A.L.3
Berrodin, T.J.4
Cohen, J.5
Huselton, C.6
Illenberger, A.7
Kern, J.C.8
Hudak, V.A.9
Marella, M.A.10
Melenski, E.G.11
McComas, C.C.12
Mugford, C.A.13
Slayden, O.D.14
Yudt, M.15
Zhang, Z.16
Zhang, P.17
Zhu, Y.18
Winneker, R.C.19
Wrobel, J.E.20
more..
-
89
-
-
77955410115
-
Potent Antagonist for the Vitamin D Receptor: Vitamin D Analogues with Simple Side Chain Structure
-
Sakamaki, Y.; Inaba, Y.; Yoshimoto, N.; Yamamoto, K. Potent Antagonist for the Vitamin D Receptor: Vitamin D Analogues with Simple Side Chain Structure J. Med. Chem. 2010, 53, 5813-5826 10.1021/jm100649d
-
(2010)
J. Med. Chem.
, vol.53
, pp. 5813-5826
-
-
Sakamaki, Y.1
Inaba, Y.2
Yoshimoto, N.3
Yamamoto, K.4
-
90
-
-
22244474357
-
The Taming of Capsaicin. Reversal of the Vanilloid Activity of N-Acylvanillamines by Aromatic Iodination
-
Appendino, G.; Daddario, N.; Minassi, A.; Moriello, A. S.; De Petrocellis, L.; Di Marzo, V. The Taming of Capsaicin. Reversal of the Vanilloid Activity of N-Acylvanillamines by Aromatic Iodination J. Med. Chem. 2005, 48, 4663-4669 10.1021/jm050139q
-
(2005)
J. Med. Chem.
, vol.48
, pp. 4663-4669
-
-
Appendino, G.1
Daddario, N.2
Minassi, A.3
Moriello, A.S.4
De Petrocellis, L.5
Di Marzo, V.6
-
91
-
-
84922824050
-
Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators
-
Sundén, H.; Holland, M. C.; Poutiainen, P. K.; Jääskeläinen, T.; Pulkkinen, J. T.; Palvimo, J. J.; Olsson, R. Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators J. Med. Chem. 2015, 58, 1569-1574 10.1021/jm501995n
-
(2015)
J. Med. Chem.
, vol.58
, pp. 1569-1574
-
-
Sundén, H.1
Holland, M.C.2
Poutiainen, P.K.3
Jääskeläinen, T.4
Pulkkinen, J.T.5
Palvimo, J.J.6
Olsson, R.7
-
92
-
-
0035935697
-
Synthesis, Nicotinic Acetylcholine Receptor Binding, and Antinociceptive Properties of 2-exo-2-(2′-Substituted-3′-phenyl-5′-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel Nicotinic Antagonist
-
Carroll, F. I.; Lee, J. R.; Navarro, H. A.; Brieaddy, L. E.; Abraham, P.; Damaj, M. I.; Martin, B. R. Synthesis, Nicotinic Acetylcholine Receptor Binding, and Antinociceptive Properties of 2-exo-2-(2′-Substituted-3′-phenyl-5′-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel Nicotinic Antagonist J. Med. Chem. 2001, 44, 4039-4041 10.1021/jm015561v
-
(2001)
J. Med. Chem.
, vol.44
, pp. 4039-4041
-
-
Carroll, F.I.1
Lee, J.R.2
Navarro, H.A.3
Brieaddy, L.E.4
Abraham, P.5
Damaj, M.I.6
Martin, B.R.7
-
93
-
-
84864927786
-
Discovery of a Series of 2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as Novel Molecular Switches that Modulate Modes of Kv7.2 (KCNQ2) Channel Pharmacology: Identification of (S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a Potent, Brain Penetrant Kv7.2 Channel Inhibitor
-
Cheung, Y.-Y.; Yu, H.; Xu, K.; Zou, B.; Wu, M.; McManus, O. B.; Li, M.; Lindsley, C. W.; Hopkins, C. R. Discovery of a Series of 2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as Novel Molecular Switches that Modulate Modes of Kv7.2 (KCNQ2) Channel Pharmacology: Identification of (S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a Potent, Brain Penetrant Kv7.2 Channel Inhibitor J. Med. Chem. 2012, 55, 6975-6979 10.1021/jm300700v
-
(2012)
J. Med. Chem.
, vol.55
, pp. 6975-6979
-
-
Cheung, Y.-Y.1
Yu, H.2
Xu, K.3
Zou, B.4
Wu, M.5
McManus, O.B.6
Li, M.7
Lindsley, C.W.8
Hopkins, C.R.9
-
94
-
-
84924744510
-
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action
-
René, O.; Fauber, B. P.; Boenig, G. d. L.; Burton, B.; Eidenschenk, C.; Everett, C.; Gobbi, A.; Hymowitz, S. G.; Johnson, A. R.; Kiefer, J. R.; Liimatta, M.; Lockey, P.; Norman, M.; Ouyang, W.; Wallweber, H. A.; Wong, H. Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action ACS Med. Chem. Lett. 2015, 6, 276-281 10.1021/ml500420y
-
(2015)
ACS Med. Chem. Lett.
, vol.6
, pp. 276-281
-
-
René, O.1
Fauber, B.P.2
Boenig, G.D.L.3
Burton, B.4
Eidenschenk, C.5
Everett, C.6
Gobbi, A.7
Hymowitz, S.G.8
Johnson, A.R.9
Kiefer, J.R.10
Liimatta, M.11
Lockey, P.12
Norman, M.13
Ouyang, W.14
Wallweber, H.A.15
Wong, H.16
-
95
-
-
0032576697
-
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: A Novel Class of Nonsteroidal Human Progesterone Receptor Agonists
-
Zhi, L.; Tegley, C. M.; Kallel, E. A.; Marschke, K. B.; Mais, D. E.; Gottardis, M. M.; Jones, T. K. 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: A Novel Class of Nonsteroidal Human Progesterone Receptor Agonists J. Med. Chem. 1998, 41, 291-302 10.1021/jm9705768
-
(1998)
J. Med. Chem.
, vol.41
, pp. 291-302
-
-
Zhi, L.1
Tegley, C.M.2
Kallel, E.A.3
Marschke, K.B.4
Mais, D.E.5
Gottardis, M.M.6
Jones, T.K.7
-
96
-
-
12444262282
-
Development of Progesterone Receptor Antagonists from 1,2-Dihydrochromeno[3,4-f]quinoline Agonist Pharmacophore
-
Zhi, L.; Ringgenberg, J. D.; Edwards, J. P.; Tegley, C. M.; West, S. J.; Pio, B.; Motamedi, M.; Jones, T. K.; Marschke, K. B.; Mais, D. E.; Schrader, W. T. Development of Progesterone Receptor Antagonists from 1,2-Dihydrochromeno[3,4-f]quinoline Agonist Pharmacophore Bioorg. Med. Chem. Lett. 2003, 13, 2075-2078 10.1016/S0960-894X(03)00256-7
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 2075-2078
-
-
Zhi, L.1
Ringgenberg, J.D.2
Edwards, J.P.3
Tegley, C.M.4
West, S.J.5
Pio, B.6
Motamedi, M.7
Jones, T.K.8
Marschke, K.B.9
Mais, D.E.10
Schrader, W.T.11
-
97
-
-
79960898988
-
Benzothiazole-Based N-(Phenylsulfonyl)amides as a Novel Family of PPARα Antagonists
-
Ammazzalorso, A.; Giancristofaro, A.; D'Angelo, A.; Filippis, B. D.; Fantacuzzi, M.; Giampietro, L.; Maccallini, C.; Amoroso, R. Benzothiazole-Based N-(Phenylsulfonyl)amides as a Novel Family of PPARα Antagonists Bioorg. Med. Chem. Lett. 2011, 21, 4869-4872 10.1016/j.bmcl.2011.06.028
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 4869-4872
-
-
Ammazzalorso, A.1
Giancristofaro, A.2
D'Angelo, A.3
Filippis, B.D.4
Fantacuzzi, M.5
Giampietro, L.6
Maccallini, C.7
Amoroso, R.8
-
98
-
-
70350061743
-
Synthesis and Biological Evaluation of 2-Heteroarylthioalkanoic Acid Analogues of Clofibric Acid as Peroxisome Proliferator-Activated Receptor α Agonists
-
Giampietro, L.; Ammazzalorso, A.; Giancristofaro, A.; Lannutti, F.; Bettoni, G.; De Filippis, B.; Fantacuzzi, M.; Maccallini, C.; Petruzzelli, M.; Morgano, A.; Moschetta, A.; Amoroso, R. Synthesis and Biological Evaluation of 2-Heteroarylthioalkanoic Acid Analogues of Clofibric Acid as Peroxisome Proliferator-Activated Receptor α Agonists J. Med. Chem. 2009, 52, 6224-6232 10.1021/jm900878u
-
(2009)
J. Med. Chem.
, vol.52
, pp. 6224-6232
-
-
Giampietro, L.1
Ammazzalorso, A.2
Giancristofaro, A.3
Lannutti, F.4
Bettoni, G.5
De Filippis, B.6
Fantacuzzi, M.7
Maccallini, C.8
Petruzzelli, M.9
Morgano, A.10
Moschetta, A.11
Amoroso, R.12
-
99
-
-
71749096236
-
5-Aryl Indanones and Derivatives as Non-Steroidal Progesterone Receptor Modulators
-
Kern, J. C.; Terefenko, E.; Trybulski, E.; Berrodin, T. J.; Cohen, J.; Winneker, R. C.; Yudt, M. R.; Zhang, Z.; Zhu, Y.; Zhang, P. 5-Aryl Indanones and Derivatives as Non-Steroidal Progesterone Receptor Modulators Bioorg. Med. Chem. Lett. 2009, 19, 6666-6669 10.1016/j.bmcl.2009.10.008
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6666-6669
-
-
Kern, J.C.1
Terefenko, E.2
Trybulski, E.3
Berrodin, T.J.4
Cohen, J.5
Winneker, R.C.6
Yudt, M.R.7
Zhang, Z.8
Zhu, Y.9
Zhang, P.10
|