Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor
Fleck, Beth A, Hoare, Sam R J, Pick, Rebecca R, Bradbury, Margaret J, Grigoriadis, Dimitri E
Published in The Journal of pharmacology and experimental therapeutics (01.05.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.05.2012)
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Allosteric Ligands for the Corticotropin Releasing Factor Type 1 Receptor Modulate Conformational States Involved in Receptor Activation
Hoare, Sam R J, Fleck, Beth A, Gross, Raymond S, Crowe, Paul D, Williams, John P, Grigoriadis, Dimitri E
Published in Molecular pharmacology (01.05.2008)
Published in Molecular pharmacology (01.05.2008)
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Studies on the structure–activity relationship of bicifadine analogs as monoamine transporter inhibitors
Zhang, Mingzhu, Jovic, Florence, Vickers, Troy, Dyck, Brian, Tamiya, Junko, Grey, Jonathan, Tran, Joe A., Fleck, Beth A., Pick, Rebecca, Foster, Alan C., Chen, Chen
Published in Bioorganic & medicinal chemistry (01.07.2008)
Published in Bioorganic & medicinal chemistry (01.07.2008)
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The importance of target binding kinetics for measuring target binding affinity in drug discovery: a case study from a CRF1 receptor antagonist program
Hoare, Sam R.J., Fleck, Beth A., Williams, John P., Grigoriadis, Dimitri E.
Published in Drug discovery today (01.01.2020)
Published in Drug discovery today (01.01.2020)
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Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors
TAMIYA, Junko, DYCK, Brian, FOSTER, Alan C, CHEN CHEN, MINGZHU ZHANG, PHAN, Kasey, FLECK, Beth A, APARICIO, Anna, JOVIC, Florence, TRAN, Joe A, VICKERS, Troy, GREY, Jonathan
Published in Bioorganic & medicinal chemistry (01.06.2008)
Published in Bioorganic & medicinal chemistry (01.06.2008)
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Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors
Chen, Chen, Dyck, Brian, Fleck, Beth A., Foster, Alan C., Grey, Jonathan, Jovic, Florence, Mesleh, Michael, Phan, Kasey, Tamiya, Junko, Vickers, Troy, Zhang, Mingzhu
Published in Bioorganic & medicinal chemistry (15.02.2008)
Published in Bioorganic & medicinal chemistry (15.02.2008)
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Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors
Vickers, Troy, Dyck, Brian, Tamiya, Junko, Zhang, Mingzhu, Jovic, Florence, Grey, Jonathan, Fleck, Beth A., Aparicio, Anna, Johns, Michael, Jin, Liping, Tang, Hui, Foster, Alan C., Chen, Chen
Published in Bioorganic & medicinal chemistry (01.06.2008)
Published in Bioorganic & medicinal chemistry (01.06.2008)
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Design, Synthesis, In Vitro, and In Vivo Characterization of Phenylpiperazines and Pyridinylpiperazines as Potent and Selective Antagonists of the Melanocortin-4 Receptor
Tran, Joe A, Jiang, Wanlong, Tucci, Fabio C, Fleck, Beth A, Wen, Jenny, Sai, Yang, Madan, Ajay, Chen, Ta Kung, Markison, Stacy, Foster, Alan C, Hoare, Sam R, Marks, Daniel, Harman, John, Chen, Caroline W, Arellano, Melissa, Marinkovic, Dragan, Bozigian, Haig, Saunders, John, Chen, Chen
Published in Journal of medicinal chemistry (13.12.2007)
Published in Journal of medicinal chemistry (13.12.2007)
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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines
Tucci, Fabio C., White, Nicole S., Markison, Stacy, Joppa, Margaret, Tran, Joe A., Fleck, Beth A., Madan, Ajay, Dyck, Brian P., Parker, Jessica, Pontillo, Joseph, Melissa Arellano, L., Marinkovic, Dragan, Jiang, Wanlong, Chen, Caroline W., Gogas, Kathleen R., Goodfellow, Val S., Saunders, John, Foster, Alan C., Chen, Chen
Published in Bioorganic & medicinal chemistry letters (01.10.2005)
Published in Bioorganic & medicinal chemistry letters (01.10.2005)
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A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice
Pontillo, Joseph, Tran, Joseph A., Markison, Stacy, Joppa, Margaret, Fleck, Beth A., Marinkovic, Dragan, Arellano, Melissa, Tucci, Fabio C., Lanier, Marion, Nelson, Jodie, Saunders, John, Hoare, Sam R.J., Foster, Alan C., Chen, Chen
Published in Bioorganic & medicinal chemistry letters (16.05.2005)
Published in Bioorganic & medicinal chemistry letters (16.05.2005)
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The Regulation of Feeding and Metabolic Rate and the Prevention of Murine Cancer Cachexia with a Small-Molecule Melanocortin-4 Receptor Antagonist
Markison, Stacy, Foster, Alan C, Chen, Chen, Brookhart, Gregor B, Hesse, Amy, Hoare, Sam R. J, Fleck, Beth A, Brown, Brock T, Marks, Daniel L
Published in Endocrinology (Philadelphia) (01.06.2005)
Published in Endocrinology (Philadelphia) (01.06.2005)
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Synthesis and structure–activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint
Hudson, Sarah, Kiankarimi, Mehrak, Eccles, Wendy, Mostofi, Yalda S., Genicot, Marc J., Dwight, Wesley, Fleck, Beth A., Gogas, Kathleen, Wade, Warren S.
Published in Bioorganic & medicinal chemistry (15.08.2008)
Published in Bioorganic & medicinal chemistry (15.08.2008)
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Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI)
Wu, Dongpei, Pontillo, Joseph, Ching, Brett, Hudson, Sarah, Gao, Yinghong, Fleck, Beth A., Gogas, Kathleen, Wade, Warren S.
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor
Tran, Joe A., Chen, Caroline W., Jiang, Wanlong, Tucci, Fabio C., Fleck, Beth A., Marinkovic, Dragan, Arellano, Melissa, Chen, Chen
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
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Discovery of 1-{2-[(1S)-(3-Dimethylamino-propionyl)amino-2-methylpropyl]-4-methyl-phenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an Orally Active Antagonist of the Melanocortin-4 Receptor for the Potential Treatment of Cachexia
Chen, Chen, Jiang, Wanlong, Tucci, Fabio, Tran, Joe A, Fleck, Beth A, Hoare, Sam R, Joppa, Margaret, Markison, Stacy, Wen, Jenny, Sai, Yang, Johns, Michael, Madan, Ajay, Chen, Takung, Chen, Caroline W, Marinkovic, Dragan, Arellano, Melissa, Saunders, John, Foster, Alan C
Published in Journal of medicinal chemistry (01.11.2007)
Published in Journal of medicinal chemistry (01.11.2007)
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Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands
Tran, Joe A., Chen, Caroline W., Tucci, Fabio C., Jiang, Wanlong, Fleck, Beth A., Chen, Chen
Published in Bioorganic & medicinal chemistry (01.02.2008)
Published in Bioorganic & medicinal chemistry (01.02.2008)
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Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure–activity relationships and insurmountable antagonism
Sullivan, Susan K., Hoare, Sam R.J., Fleck, Beth A., Zhu, Yun-Fei, Heise, Christopher E., Struthers, R. Scott, Crowe, Paul D.
Published in Biochemical pharmacology (28.09.2006)
Published in Biochemical pharmacology (28.09.2006)
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Pharmacological and pharmacokinetic characterization of 2-piperazine-α-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists
Chen, Chen, Tucci, Fabio C., Jiang, Wanlong, Tran, Joe A., Fleck, Beth A., Hoare, Sam R., Wen, Jenny, Chen, Takung, Johns, Michael, Markison, Stacy, Foster, Alan C., Marinkovic, Dragan, Chen, Caroline W., Arellano, Melissa, Harman, John, Saunders, John, Bozigian, Haig, Marks, Daniel
Published in Bioorganic & medicinal chemistry (15.05.2008)
Published in Bioorganic & medicinal chemistry (15.05.2008)
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4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a Potent and Selective Melanocortin-4 Receptor AntagonistDesign, Synthesis, and Characterization
Chen, Pontillo, Joseph, Fleck, Beth A, Gao, Yinghong, Wen, Jenny, Tran, Joe A, Tucci, Fabio C, Marinkovic, Dragan, Foster, Alan C, Saunders, John
Published in Journal of medicinal chemistry (30.12.2004)
Published in Journal of medicinal chemistry (30.12.2004)
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