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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Vazquez, Michael L ; Kaila, Neelu ; Strohbach, Joseph W ; Trzupek, John D ; Brown, Matthew F ; Flanagan, Mark E ; Mitton-Fry, Mark J ; Johnson, Timothy A ; TenBrink, Ruth E ; Arnold, Eric P ; Basak, Arindrajit ; Heasley, Steven E ; Kwon, Soojin ; Langille, Jonathan ; Parikh, Mihir D ; Griffin, Sarah H ; Casavant, Jeffrey M ; Duclos, Brian A ; Fenwick, Ashley E ; Harris, Thomas M ; Han, Seungil ; Caspers, Nicole ; Dowty, Martin E ; Yang, Xin ; Banker, Mary Ellen ; Hegen, Martin ; Symanowicz, Peter T ; Li, Li ; Wang, Lu ; Lin, Tsung H ; Jussif, Jason ; Clark, James D ; Telliez, Jean-Baptiste ; Robinson, Ralph P ; Unwalla, Ray

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.1130-1152 [Periódico revisado por pares]

United States: American Chemical Society

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2
Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor
Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor
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Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor

Garcia Fortanet, Jorge ; Chen, Christine Hiu-Tung ; Chen, Ying-Nan P ; Chen, Zhouliang ; Deng, Zhan ; Firestone, Brant ; Fekkes, Peter ; Fodor, Michelle ; Fortin, Pascal D ; Fridrich, Cary ; Grunenfelder, Denise ; Ho, Samuel ; Kang, Zhao B ; Karki, Rajesh ; Kato, Mitsunori ; Keen, Nick ; LaBonte, Laura R ; Larrow, Jay ; Lenoir, Francois ; Liu, Gang ; Liu, Shumei ; Lombardo, Franco ; Majumdar, Dyuti ; Meyer, Matthew J ; Palermo, Mark ; Perez, Lawrence ; Pu, Minying ; Ramsey, Timothy ; Sellers, William R ; Shultz, Michael D ; Stams, Travis ; Towler, Christopher ; Wang, Ping ; Williams, Sarah L ; Zhang, Ji-Hu ; LaMarche, Matthew J

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.7773-7782 [Periódico revisado por pares]

United States: American Chemical Society

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3
Discovery of BIO-8169A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation
Discovery of BIO-8169A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation
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Discovery of BIO-8169A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation

Pfaffenbach, Magnus ; Bolduc, Philippe N. ; Xin, Zhili ; Gao, Fang ; Evans, Ryan ; Fang, Terry ; Chodaparambil, Jayanth V. ; Henry, Kate L. ; Li, Pei ; Mathieu, Steven ; Metrick, Claire ; Vera Rebollar, Jorge A. ; Gu, Rong-Fang ; Mccarl, Christie-Ann ; Silbereis, John ; Peterson, Emily A.

Journal of medicinal chemistry, 2024-05, Vol.67 (10), p.8383-8395 [Periódico revisado por pares]

United States: American Chemical Society

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4
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B
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Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B

Mackman, Richard L ; Mish, Michael ; Chin, Gregory ; Perry, Jason K ; Appleby, Todd ; Aktoudianakis, Vangelis ; Metobo, Sammy ; Pyun, Peter ; Niu, Congrong ; Daffis, Stephane ; Yu, Helen ; Zheng, Jim ; Villasenor, Armando G ; Zablocki, Jeff ; Chamberlain, Jason ; Jin, Haolun ; Lee, Gary ; Suekawa-Pirrone, Kimberley ; Santos, Rex ; Delaney, William E ; Fletcher, Simon P

Journal of medicinal chemistry, 2020-09, Vol.63 (18), p.10188-10203 [Periódico revisado por pares]

United States: American Chemical Society

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5
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy
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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Dilger, Andrew K ; Pabbisetty, Kumar B ; Corte, James R ; De Lucca, Indawati ; Fang, Tianan ; Yang, Wu ; Pinto, Donald J. P ; Wang, Yufeng ; Zhu, Yeheng ; Mathur, Arvind ; Li, Jianqing ; Hou, Xiaoping ; Smith, Daniel ; Sun, Dawn ; Zhang, Huiping ; Krishnananthan, Subramaniam ; Wu, Dauh-Rurng ; Myers, Joseph E ; Sheriff, Steven ; Rossi, Karen A ; Chacko, Silvi ; Zheng, Joanna J ; Galella, Michael A ; Ziemba, Theresa ; Dierks, Elizabeth A ; Bozarth, Jeffrey M ; Wu, Yiming ; Crain, Earl ; Wong, Pancras C ; Luettgen, Joseph M ; Wexler, Ruth R ; Ewing, William R

Journal of medicinal chemistry, 2022-02, Vol.65 (3), p.1770-1785 [Periódico revisado por pares]

United States: American Chemical Society

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6
Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential
Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential
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Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

Coteron, Jose M ; Marco, María ; Esquivias, Jorge ; Deng, Xiaoyi ; White, Karen L ; White, John ; Koltun, Maria ; El Mazouni, Farah ; Kokkonda, Sreekanth ; Katneni, Kasiram ; Bhamidipati, Ravi ; Shackleford, David M ; Angulo-Barturen, Iñigo ; Ferrer, Santiago B ; Jiménez-Díaz, María Belén ; Gamo, Francisco-Javier ; Goldsmith, Elizabeth J ; Charman, William N ; Bathurst, Ian ; Floyd, David ; Matthews, David ; Burrows, Jeremy N ; Rathod, Pradipsinh K ; Charman, Susan A ; Phillips, Margaret A

Journal of medicinal chemistry, 2011-08, Vol.54 (15), p.5540-5561 [Periódico revisado por pares]

United States: American Chemical Society

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7
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Zhou, Bing ; Hu, Jiantao ; Xu, Fuming ; Chen, Zhuo ; Bai, Longchuan ; Fernandez-Salas, Ester ; Lin, Mei ; Liu, Liu ; Yang, Chao-Yie ; Zhao, Yujun ; McEachern, Donna ; Przybranowski, Sally ; Wen, Bo ; Sun, Duxin ; Wang, Shaomeng

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.462-481 [Periódico revisado por pares]

United States: American Chemical Society

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8
Nanomolar Potency and Metabolically Stable Inhibitors of Kidney Urea Transporter UT-B
Nanomolar Potency and Metabolically Stable Inhibitors of Kidney Urea Transporter UT-B
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Nanomolar Potency and Metabolically Stable Inhibitors of Kidney Urea Transporter UT-B

Anderson, Marc O ; Zhang, Jicheng ; Liu, Yan ; Yao, Chenjuan ; Phuan, Puay-Wah ; Verkman, A. S

Journal of medicinal chemistry, 2012-06, Vol.55 (12), p.5942-5950 [Periódico revisado por pares]

United States: American Chemical Society

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9
Discovery of the Irreversible Covalent FGFR Inhibitor 8‑(3-(4-Acryloyl­piperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)­pyrido[2,3‑d]­pyrimidin-7(8H)‑one (PRN1371) for the Treatment of Solid Tumors
Discovery of the Irreversible Covalent FGFR Inhibitor 8‑(3-(4-Acryloyl­piperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)­pyrido[2,3‑d]­pyrimidin-7(8H)‑one (PRN1371) for the Treatment of Solid Tumors
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Discovery of the Irreversible Covalent FGFR Inhibitor 8‑(3-(4-Acryloyl­piperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)­pyrido[2,3‑d]­pyrimidin-7(8H)‑one (PRN1371) for the Treatment of Solid Tumors

Brameld, Ken A ; Owens, Timothy D ; Verner, Erik ; Venetsanakos, Eleni ; Bradshaw, J. Michael ; Phan, Vernon T ; Tam, Danny ; Leung, Kwan ; Shu, Jin ; LaStant, Jacob ; Loughhead, David G ; Ton, Tony ; Karr, Dane E ; Gerritsen, Mary E ; Goldstein, David M ; Funk, Jens Oliver

Journal of medicinal chemistry, 2017-08, Vol.60 (15), p.6516-6527 [Periódico revisado por pares]

United States: American Chemical Society

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10
Design, Synthesis, and Evaluation of Thiophene[3,2‑d]pyrimidine Derivatives as HIV‑1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles
Design, Synthesis, and Evaluation of Thiophene[3,2‑d]pyrimidine Derivatives as HIV‑1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles
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Design, Synthesis, and Evaluation of Thiophene[3,2‑d]pyrimidine Derivatives as HIV‑1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles

Kang, Dongwei ; Fang, Zengjun ; Li, Zhenyu ; Huang, Boshi ; Zhang, Heng ; Lu, Xueyi ; Xu, Haoran ; Zhou, Zhongxia ; Ding, Xiao ; Daelemans, Dirk ; De Clercq, Erik ; Pannecouque, Christophe ; Zhan, Peng ; Liu, Xinyong

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.7991-8007 [Periódico revisado por pares]

United States: American Chemical Society

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