Identification of positive modulators of TRPM5 channel from a high-throughput screen using a fluorescent membrane potential assay
Virginio, Caterina, Aldegheri, Laura, Nola, Selena, Brodbeck, Daniela, Brault, Laurent, Raveglia, Luca F., Barilli, Alessio, Sabat, Mark, Myers, Richard
Published in SLAS discovery (01.01.2022)
Published in SLAS discovery (01.01.2022)
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Development of Orally Bioavailable Bicyclic Pyrazolones as Inhibitors of Tumor Necrosis Factor-α Production
Clark, Michael P, Laughlin, Steven K, Laufersweiler, Matthew J, Bookland, Roger G, Brugel, Todd A, Golebiowski, Adam, Sabat, Mark P, Townes, Jennifer A, VanRens, John C, Djung, Jane F, Natchus, Michael G, De, Biswanath, Hsieh, Lily C, Xu, Susan C, Walter, Rick L, Mekel, Marlene J, Heitmeyer, Sandra A, Brown, Kimberly K, Juergens, Karen, Taiwo, Yetunde O, Janusz, Michael J
Published in Journal of medicinal chemistry (20.05.2004)
Published in Journal of medicinal chemistry (20.05.2004)
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Journal Article
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3)
Clark, Michael P., George, Kelly M., Bookland, Roger G., Chen, Jack, Laughlin, Steven K., Thakur, Kumar D., Lee, Wenlin, Davis, Jan R., Cabrera, Ed J., Brugel, Todd A., VanRens, John C., Laufersweiler, Matthew J., Maier, Jennifer A., Sabat, Mark P., Golebiowski, Adam, Easwaran, Vijay, Webster, Mark E., De, Biswanath, Zhang, George
Published in Bioorganic & medicinal chemistry letters (01.03.2007)
Published in Bioorganic & medicinal chemistry letters (01.03.2007)
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Journal Article
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-α) production
Laughlin, Steven K., Clark, Michael P., Djung, Jane F., Golebiowski, Adam, Brugel, Todd A., Sabat, Mark, Bookland, Roger G., Laufersweiler, Matthew J., VanRens, John C., Townes, Jennifer A., De, Biswanath, Hsieh, Lily C., Xu, Susan C., Walter, Richard L., Mekel, Marlene J., Janusz, Michael J.
Published in Bioorganic & medicinal chemistry letters (02.05.2005)
Published in Bioorganic & medicinal chemistry letters (02.05.2005)
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Journal Article
The development of monocyclic pyrazolone based cytokine synthesis inhibitors
Golebiowski, Adam, Townes, Jennifer A., Laufersweiler, Matthew J., Brugel, Todd A., Clark, Michael P., Clark, Cynthia M., Djung, Jane F., Laughlin, Steven K., Sabat, Mark P., Bookland, Roger G., VanRens, John C., De, Biswanath, Hsieh, Lily C., Janusz, Michael J., Walter, Richard L., Webster, Mark E., Mekel, Marlene J.
Published in Bioorganic & medicinal chemistry letters (02.05.2005)
Published in Bioorganic & medicinal chemistry letters (02.05.2005)
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Journal Article
Structures of the TRPM5 channel elucidate mechanisms of activation and inhibition
Ruan, Zheng, Haley, Emery, Orozco, Ian J., Sabat, Mark, Myers, Richard, Roth, Rebecca, Du, Juan, Lü, Wei
Published in Nature structural & molecular biology (01.07.2021)
Published in Nature structural & molecular biology (01.07.2021)
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Journal Article
The development of novel inhibitors of tumor necrosis factor-α (TNF-α) production based on substituted [5,5]-bicyclic pyrazolones
Laufersweiler, Matthew J, Brugel, Todd A, Clark, Michael P, Golebiowski, Adam, Bookland, Roger G, Laughlin, Steven K, Sabat, Mark P, Townes, Jennifer A, VanRens, John C, De, Biswanath, Hsieh, Lily C, Heitmeyer, Sandra A, Juergens, Karen, Brown, Kimberly K, Mekel, Marlene J, Walter, Richard L, Janusz, Michael J
Published in Bioorganic & medicinal chemistry letters (16.08.2004)
Published in Bioorganic & medicinal chemistry letters (16.08.2004)
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Journal Article
Structures of the TRPM5 channel elucidate mechanisms of activation and inhibition
Haley, Emery D., Ruan, Zheng, Orozco, Ian J., Roth, Becca, Sabat, Mark, Myers, Richard, Du, Juan, Lu, Wei
Published in Biophysical journal (11.02.2022)
Published in Biophysical journal (11.02.2022)
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Journal Article
Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton’s Tyrosine Kinase
Smith, Christopher R., Dougan, Douglas R., Komandla, Mallareddy, Kanouni, Toufike, Knight, Beverly, Lawson, J. David, Sabat, Mark, Taylor, Ewan R., Vu, Phong, Wyrick, Corey
Published in Journal of medicinal chemistry (23.07.2015)
Published in Journal of medicinal chemistry (23.07.2015)
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Journal Article
Tuft cell-derived acetylcholine promotes epithelial chloride secretion and intestinal helminth clearance
Billipp, Tyler E., Fung, Connie, Webeck, Lily M., Sargent, Derek B., Gologorsky, Matthew B., Chen, Zuojia, McDaniel, Margaret M., Kasal, Darshan N., McGinty, John W., Barrow, Kaitlyn A., Rich, Lucille M., Barilli, Alessio, Sabat, Mark, Debley, Jason S., Wu, Chuan, Myers, Richard, Howitt, Michael R., von Moltke, Jakob
Published in Immunity (Cambridge, Mass.) (11.06.2024)
Published in Immunity (Cambridge, Mass.) (11.06.2024)
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From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents
Barilli, Alessio, Aldegheri, Laura, Bianchi, Federica, Brault, Laurent, Brodbeck, Daniela, Castelletti, Laura, Feriani, Aldo, Lingard, Iain, Myers, Richard, Nola, Selena, Piccoli, Laura, Pompilio, Daniela, Raveglia, Luca F, Salvagno, Cristian, Tassini, Sabrina, Virginio, Caterina, Sabat, Mark
Published in Journal of medicinal chemistry (13.05.2021)
Published in Journal of medicinal chemistry (13.05.2021)
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Journal Article
Development of N-2,4-pyrimidine-N-phenyl-N′-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-α) synthesis. Part 1
Brugel, Todd A., Maier, Jennifer A., Clark, Michael P., Sabat, Mark, Golebiowski, Adam, Bookland, Roger G., Laufersweiler, Matthew J., Laughlin, Steven K., VanRens, John C., De, Biswanath, Hsieh, Lily C., Mekel, Marlene J., Janusz, Michael J.
Published in Bioorganic & medicinal chemistry letters (01.07.2006)
Published in Bioorganic & medicinal chemistry letters (01.07.2006)
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Journal Article
Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)‑5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro‑3H‑1,2,4-triazol-3-one, by Fragment-Based Drug Design
Sabat, Mark, Dougan, Douglas R, Knight, Beverly, Lawson, J. David, Scorah, Nicholas, Smith, Christopher R, Taylor, Ewan R, Vu, Phong, Wyrick, Corey, Wang, Haixia, Balakrishna, Deepika, Hixon, Mark, Madakamutil, Loui, McConn, Donavon
Published in Journal of medicinal chemistry (09.09.2021)
Published in Journal of medicinal chemistry (09.09.2021)
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Journal Article
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp(3) character and an exquisite selectivity profile
Bigi-Botterill, Simone V., Ivetac, Anthony, Bradshaw, Erica L., Cole, Derek, Dougan, Douglas R., Ermolieff, Jacques, Halkowycz, Petro, Johnson, Ben, McBride, Christopher, Pickens, Jason, Sabat, Mark, Swann, Steven
Published in Bioorganic & medicinal chemistry letters (01.09.2020)
Published in Bioorganic & medicinal chemistry letters (01.09.2020)
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Journal Article
Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 ( S )-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H -1,2,4-triazol-3-one, by Fragment-Based Drug Design”
Sabat, Mark, Dougan, Douglas R, Ermolieff, Jacques, Halkowycz, Petro, Knight, Beverly, Lawson, J. David, Scorah, Nicholas, Smith, Christopher R, Taylor, Ewan R, Vu, Phong, Wyrick, Corey, Wang, Haixia, Balakrishna, Deepika, Hixon, Mark, Madakamutil, Loui, McConn, Donavon
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Journal Article
Correction to “Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)‑5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro‑3H‑1,2,4-triazol-3-one, by Fragment-Based Drug Design”
Sabat, Mark, Dougan, Douglas R, Ermolieff, Jacques, Halkowycz, Petro, Knight, Beverly, Lawson, J. David, Scorah, Nicholas, Smith, Christopher R, Taylor, Ewan R, Vu, Phong, Wyrick, Corey, Wang, Haixia, Balakrishna, Deepika, Hixon, Mark, Madakamutil, Loui, McConn, Donavon
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Journal Article
Design and Discovery of a Potent and Selective Inhibitor of Integrin αvβ1
Sabat, Mark, Carney, Daniel W., Hernandez-Torres, Gloria, Gibson, Tony S., Balakrishna, Deepika, Zou, Hua, Xu, Rui, Chen, Chien-Hung, de Jong, Ron, Dougan, Douglas R., Qin, Ling, Bigi-Botterill, Simone V., Chambers, Alison, Miura, Joanne, Johnson, Lucas K., Ermolieff, Jacques, Johns, Deidre, Selimkhanov, Jangir, Kwok, Lily, DeMent, Kevin, Proffitt, Chris, Vu, Phong, Lindsey, Erick A., Ivetac, Tony, Jennings, Andy, Wang, Haixia, Manam, Padma, Santos, Cipriano, Fullenwider, Cody, Manohar, Rohan, Flick, Andrew C.
Published in Journal of medicinal chemistry (27.06.2024)
Published in Journal of medicinal chemistry (27.06.2024)
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Journal Article
Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors
Sabat, Mark, Wang, Haixia, Scorah, Nick, Lawson, J. David, Atienza, Joy, Kamran, Ruhi, Hixon, Mark S., Dougan, Douglas R.
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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