Systematic Study of the Glutathione Reactivity of N‑Phenylacrylamides: 2. Effects of Acrylamide Substitution
Birkholz, Adam, Kopecky, David J, Volak, Laurie P, Bartberger, Michael D, Chen, Yuping, Tegley, Christopher M, Arvedson, Tara, McCarter, John D, Fotsch, Christopher, Cee, Victor J
Published in Journal of medicinal chemistry (22.10.2020)
Published in Journal of medicinal chemistry (22.10.2020)
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Kinetic characterization and identification of a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 using a time-resolved fluorescence resonance energy transfer-based assay technology
Dao, Jennifer H., Kurzeja, Robert J.M., Morachis, Jose M., Veith, Henrike, Lewis, Jeffery, Yu, Violeta, Tegley, Christopher M., Tagari, Philip
Published in Analytical biochemistry (15.01.2009)
Published in Analytical biochemistry (15.01.2009)
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Different Modes of Inhibitor Binding to Prolyl Hydroxylase by Combined Use of X-ray Crystallography and NMR Spectroscopy of Paramagnetic Complexes
Poppe, Leszek, Tegley, Christopher M, Li, Vivian, Lewis, Jeffrey, Zondlo, James, Yang, Evelyn, Kurzeja, Robert JM, Syed, Rashid
Published in Journal of the American Chemical Society (25.11.2009)
Published in Journal of the American Chemical Society (25.11.2009)
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Uncompetitive, adduct-forming SARM1 inhibitors are neuroprotective in preclinical models of nerve injury and disease
Bratkowski, Matthew, Burdett, Thomas C., Danao, Jean, Wang, Xidao, Mathur, Prakhyat, Gu, Weijing, Beckstead, Jennifer A., Talreja, Santosh, Yang, Yu-San, Danko, Gregory, Park, Jae Hong, Walton, Mary, Brown, Sean P., Tegley, Christopher M., Joseph, Prem Raj B., Reynolds, Charles H., Sambashivan, Shilpa
Published in Neuron (Cambridge, Mass.) (16.11.2022)
Published in Neuron (Cambridge, Mass.) (16.11.2022)
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Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones
van Oeveren, Arjan, Pio, Barbara A., Tegley, Christopher M., Higuchi, Robert I., Wu, Min, Jones, Todd K., Marschke, Keith B., Negro-Vilar, Andrés, Zhi, Lin
Published in Bioorganic & medicinal chemistry letters (15.03.2007)
Published in Bioorganic & medicinal chemistry letters (15.03.2007)
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Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species
Foti, Robert S, Biswas, Kaustav, Aral, Jennifer, Be, Xuhai, Berry, Loren, Cheng, Yuan, Conner, Kip, Falsey, James R, Glaus, Charles, Herberich, Brad, Hickman, Dean, Ikotun, Tayo, Li, Hongyan, Long, Jason, Huang, Liyue, Miranda, Les P, Murray, Justin, Moyer, Bryan, Netirojjanakul, Chawita, Nixey, Thomas E, Sham, Kelvin, Soto, Marcus, Tegley, Christopher M, Tran, Linh, Wu, Bin, Yin, Lin, Rock, Dan A
Published in Drug metabolism and disposition (01.10.2019)
Published in Drug metabolism and disposition (01.10.2019)
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Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx‑1 Peptide–Antibody Conjugates
Biswas, Kaustav, Nixey, Thomas E, Murray, Justin K, Falsey, James R, Yin, Li, Liu, Hantao, Gingras, Jacinthe, Hall, Brian E, Herberich, Brad, Holder, Jerry Ryan, Li, Hongyan, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, Soriano, Brian D, Soto, Marcus, Tran, Linh, Tegley, Christopher M, Zou, Anrou, Gunasekaran, Kannan, Moyer, Bryan D, Doherty, Liz, Miranda, Les P
Published in ACS chemical biology (15.09.2017)
Published in ACS chemical biology (15.09.2017)
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Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint
Pennington, Lewis D, Bartberger, Michael D, Croghan, Michael D, Andrews, Kristin L, Ashton, Kate S, Bourbeau, Matthew P, Chen, Jie, Chmait, Samer, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Hong, Fang-Tsao, Hungate, Randall W, Jordan, Steven R, Kong, Ke, Liu, Longbin, Michelsen, Klaus, Moyer, Carolyn, Nishimura, Nobuko, Norman, Mark H, Reichelt, Andreas, Siegmund, Aaron C, Sivits, Glenn, Tadesse, Seifu, Tegley, Christopher M, Van, Gwyneth, Yang, Kevin C, Yao, Guomin, Zhang, Jiandong, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (24.12.2015)
Published in Journal of medicinal chemistry (24.12.2015)
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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors
Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L. Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J. Russell, Cee, Victor J
Published in Journal of medicinal chemistry (09.01.2020)
Published in Journal of medicinal chemistry (09.01.2020)
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Journal Article
Discovery of a Covalent Inhibitor of KRAS G12C (AMG 510) for the Treatment of Solid Tumors
Lanman, Brian A, Allen, Jennifer R, Allen, John G, Amegadzie, Albert K, Ashton, Kate S, Booker, Shon K, Chen, Jian Jeffrey, Chen, Ning, Frohn, Michael J, Goodman, Guy, Kopecky, David J, Liu, Longbin, Lopez, Patricia, Low, Jonathan D, Ma, Vu, Minatti, Ana E, Nguyen, Thomas T, Nishimura, Nobuko, Pickrell, Alexander J, Reed, Anthony B, Shin, Youngsook, Siegmund, Aaron C, Tamayo, Nuria A, Tegley, Christopher M, Walton, Mary C, Wang, Hui-Ling, Wurz, Ryan P, Xue, May, Yang, Kevin C, Achanta, Pragathi, Bartberger, Michael D, Canon, Jude, Hollis, L Steven, McCarter, John D, Mohr, Christopher, Rex, Karen, Saiki, Anne Y, San Miguel, Tisha, Volak, Laurie P, Wang, Kevin H, Whittington, Douglas A, Zech, Stephan G, Lipford, J Russell, Cee, Victor J
Published in Journal of medicinal chemistry (09.01.2020)
Published in Journal of medicinal chemistry (09.01.2020)
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Engineering Na V 1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics
Murray, Justin K, Wu, Bin, Tegley, Christopher M, Nixey, Thomas E, Falsey, James R, Herberich, Brad, Yin, Li, Sham, Kelvin, Long, Jason, Aral, Jennifer, Cheng, Yuan, Netirojjanakul, Chawita, Doherty, Liz, Glaus, Charles, Ikotun, Tayo, Li, Hongyan, Tran, Linh, Soto, Marcus, Salimi-Moosavi, Hossein, Ligutti, Joseph, Amagasu, Shanti, Andrews, Kristin L, Be, Xuhai, Lin, Min-Hwa Jasmine, Foti, Robert S, Ilch, Christopher P, Youngblood, Beth, Kornecook, Thomas J, Karow, Margaret, Walker, Kenneth W, Moyer, Bryan D, Biswas, Kaustav, Miranda, Les P
Published in ACS chemical biology (19.04.2019)
Published in ACS chemical biology (19.04.2019)
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Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4- f]quinoline derivatives as progesterone receptor modulators
Zhi, Lin, Tegley, Christopher M, Pio, Barbara, Edwards, James P, Jones, Todd K, Marschke, Keith B, Mais, Dale E, Risek, Boris, Schrader, William T
Published in Bioorganic & medicinal chemistry letters (16.06.2003)
Published in Bioorganic & medicinal chemistry letters (16.06.2003)
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Journal Article
Engineering Antibody Reactivity for Efficient Derivatization to Generate Na V 1.7 Inhibitory GpTx-1 Peptide-Antibody Conjugates
Biswas, Kaustav, Nixey, Thomas E, Murray, Justin K, Falsey, James R, Yin, Li, Liu, Hantao, Gingras, Jacinthe, Hall, Brian E, Herberich, Brad, Holder, Jerry Ryan, Li, Hongyan, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, Soriano, Brian D, Soto, Marcus, Tran, Linh, Tegley, Christopher M, Zou, Anrou, Gunasekaran, Kannan, Moyer, Bryan D, Doherty, Liz, Miranda, Les P
Published in ACS chemical biology (15.09.2017)
Published in ACS chemical biology (15.09.2017)
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Discovery of N -(1-Acryloylazetidin-3-yl)-2-(1 H -indol-1-yl)acetamides as Covalent Inhibitors of KRAS G12C
Shin, Youngsook, Jeong, Joon Won, Wurz, Ryan P, Achanta, Pragathi, Arvedson, Tara, Bartberger, Michael D, Campuzano, Iain D G, Fucini, Ray, Hansen, Stig K, Ingersoll, John, Iwig, Jeffrey S, Lipford, J Russell, Ma, Vu, Kopecky, David J, McCarter, John, San Miguel, Tisha, Mohr, Christopher, Sabet, Sudi, Saiki, Anne Y, Sawayama, Andrew, Sethofer, Steven, Tegley, Christopher M, Volak, Laurie P, Yang, Kevin, Lanman, Brian A, Erlanson, Daniel A, Cee, Victor J
Published in ACS medicinal chemistry letters (12.09.2019)
Published in ACS medicinal chemistry letters (12.09.2019)
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Journal Article
Discovery of N‑(1-Acryloylazetidin-3-yl)-2-(1H‑indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C
Shin, Youngsook, Jeong, Joon Won, Wurz, Ryan P, Achanta, Pragathi, Arvedson, Tara, Bartberger, Michael D, Campuzano, Iain D. G, Fucini, Ray, Hansen, Stig K, Ingersoll, John, Iwig, Jeffrey S, Lipford, J. Russell, Ma, Vu, Kopecky, David J, McCarter, John, San Miguel, Tisha, Mohr, Christopher, Sabet, Sudi, Saiki, Anne Y, Sawayama, Andrew, Sethofer, Steven, Tegley, Christopher M, Volak, Laurie P, Yang, Kevin, Lanman, Brian A, Erlanson, Daniel A, Cee, Victor J
Published in ACS medicinal chemistry letters (12.09.2019)
Published in ACS medicinal chemistry letters (12.09.2019)
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Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer’s disease
Chen, Jian Jeffrey, Qian, Wenyuan, Biswas, Kaustav, Yuan, Chester, Amegadzie, Albert, Liu, Qingyian, Nixey, Thomas, Zhu, Joe, Ncube, Mqhele, Rzasa, Robert M., Chavez, Frank, Chen, Ning, DeMorin, Frenel, Rumfelt, Shannon, Tegley, Christopher M., Allen, Jennifer R., Hitchcock, Stephen, Hungate, Randy, Bartberger, Michael D., Zalameda, Leeanne, Liu, Yichin, McCarter, John D., Zhang, Jianhua, Zhu, Li, Babu-Khan, Safura, Luo, Yi, Bradley, Jodi, Wen, Paul H., Reid, Darren L., Koegler, Frank, Dean, Charles, Hickman, Dean, Correll, Tiffany L., Williamson, Toni, Wood, Stephen
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
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Journal Article
Preparation, Resolution, and Biological Evaluation of 5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines: Potent, Orally Active, Nonsteroidal Progesterone Receptor Agonists
Edwards, James P, Zhi, Lin, Pooley, Charlotte L. F, Tegley, Christopher M, West, Sarah J, Wang, Ming-Wei, Gottardis, Marco M, Pathirana, Charles, Schrader, William T, Jones, Todd K
Published in Journal of medicinal chemistry (16.07.1998)
Published in Journal of medicinal chemistry (16.07.1998)
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Journal Article
Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation
Tegley, Christopher M., Viswanadhan, Vellarkad N., Biswas, Kaustav, Frohn, Michael J., Peterkin, Tanya A.N., Chang, Catherine, Bürli, Roland W., Dao, Jennifer H., Veith, Henrike, Rogers, Norma, Yoder, Sean C., Biddlecome, Gloria, Tagari, Philip, Allen, Jennifer R., Hungate, Randall W.
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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Journal Article
Discovery of ligands for Nurr1 by combined use of NMR screening with different isotopic and spin-labeling strategies
Poppe, Leszek, Harvey, Timothy S, Mohr, Christopher, Zondlo, James, Tegley, Christopher M, Nuanmanee, Opas, Cheetham, Janet
Published in Journal of biomolecular screening (01.04.2007)
Published in Journal of biomolecular screening (01.04.2007)
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Journal Article
5-Benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as Selective Progesterone Receptor Modulators
Zhi, Lin, Tegley, Christopher M, Pio, Barbara, Edwards, James P, Motamedi, Mehrnouch, Jones, Todd K, Marschke, Keith B, Mais, Dale E, Risek, Boris, Schrader, William T
Published in Journal of medicinal chemistry (11.09.2003)
Published in Journal of medicinal chemistry (11.09.2003)
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