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In silico design of novel probes for the atypical opioid receptor MRGPRX2
In silico design of novel probes for the atypical opioid receptor MRGPRX2
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In silico design of novel probes for the atypical opioid receptor MRGPRX2

Lansu, Katherine ; Karpiak, Joel ; Liu, Jing ; Huang, Xi-Ping ; McCorvy, John D ; Kroeze, Wesley K ; Che, Tao ; Nagase, Hiroshi ; Carroll, Frank I ; Jin, Jian ; Shoichet, Brian K ; Roth, Bryan L

Nature chemical biology, 2017-05, Vol.13 (5), p.529-536 [Periódico revisado por pares]

United States: Nature Publishing Group

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12
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors
Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors
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Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

Zhang, Tinghu ; Kwiatkowski, Nicholas ; Olson, Calla M ; Dixon-Clarke, Sarah E ; Abraham, Brian J ; Greifenberg, Ann K ; Ficarro, Scott B ; Elkins, Jonathan M ; Liang, Yanke ; Hannett, Nancy M ; Manz, Theresa ; Hao, Mingfeng ; Bartkowiak, Bartlomiej ; Greenleaf, Arno L ; Marto, Jarrod A ; Geyer, Matthias ; Bullock, Alex N ; Young, Richard A ; Gray, Nathanael S

Nature chemical biology, 2016-10, Vol.12 (10), p.876-884 [Periódico revisado por pares]

United States: Nature Publishing Group

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13
Synthetic Entries to and Biological Activity of Pyrrolopyrimidines
Synthetic Entries to and Biological Activity of Pyrrolopyrimidines
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Synthetic Entries to and Biological Activity of Pyrrolopyrimidines

De Coen, Laurens M ; Heugebaert, Thomas S. A ; García, Daniel ; Stevens, Christian V

Chemical reviews, 2016-01, Vol.116 (1), p.80-139 [Periódico revisado por pares]

United States: American Chemical Society

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14
Rhodium(III)-Catalyzed Imidoyl C–H Activation for Annulations to Azolopyrimidines
Rhodium(III)-Catalyzed Imidoyl C–H Activation for Annulations to Azolopyrimidines
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Rhodium(III)-Catalyzed Imidoyl C–H Activation for Annulations to Azolopyrimidines

Halskov, Kim Søholm ; Witten, Michael R ; Hoang, Gia L ; Mercado, Brandon Q ; Ellman, Jonathan A

Organic letters, 2018-04, Vol.20 (8), p.2464-2467 [Periódico revisado por pares]

United States: American Chemical Society

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15
Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials
Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials
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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Marsilje, Thomas H ; Pei, Wei ; Chen, Bei ; Lu, Wenshuo ; Uno, Tetsuo ; Jin, Yunho ; Jiang, Tao ; Kim, Sungjoon ; Li, Nanxin ; Warmuth, Markus ; Sarkisova, Yelena ; Sun, Frank ; Steffy, Auzon ; Pferdekamper, AnneMarie C ; Li, Allen G ; Joseph, Sean B ; Kim, Young ; Liu, Bo ; Tuntland, Tove ; Cui, Xiaoming ; Gray, Nathanael S ; Steensma, Ruo ; Wan, Yongqin ; Jiang, Jiqing ; Chopiuk, Greg ; Li, Jie ; Gordon, W. Perry ; Richmond, Wendy ; Johnson, Kevin ; Chang, Jonathan ; Groessl, Todd ; He, You-Qun ; Phimister, Andrew ; Aycinena, Alex ; Lee, Christian C ; Bursulaya, Badry ; Karanewsky, Donald S ; Seidel, H. Martin ; Harris, Jennifer L ; Michellys, Pierre-Yves

Journal of medicinal chemistry, 2013-07, Vol.56 (14), p.5675-5690 [Periódico revisado por pares]

United States: American Chemical Society

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16
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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17
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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18
Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles
Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles
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Synthesis and antimicrobial activity of pyrimidinyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles

Madhu Sekhar, M. ; Nagarjuna, U. ; Padmavathi, V. ; Padmaja, A. ; Reddy, N. Vasudeva ; Vijaya, T.

European journal of medicinal chemistry, 2018-02, Vol.145, p.1-10 [Periódico revisado por pares]

France: Elsevier Masson SAS

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19
Molecular basis of USP7 inhibition by selective small-molecule inhibitors
Molecular basis of USP7 inhibition by selective small-molecule inhibitors
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Molecular basis of USP7 inhibition by selective small-molecule inhibitors

Turnbull, Andrew P ; Ioannidis, Stephanos ; Krajewski, Wojciech W ; Pinto-Fernandez, Adan ; Heride, Claire ; Martin, Agnes C L ; Tonkin, Louise M ; Townsend, Elizabeth C ; Buker, Shane M ; Lancia, David R ; Caravella, Justin A ; Toms, Angela V ; Charlton, Thomas M ; Lahdenranta, Johanna ; Wilker, Erik ; Follows, Bruce C ; Evans, Nicola J ; Stead, Lucy ; Alli, Cristina ; Zarayskiy, Vladislav V ; Talbot, Adam C ; Buckmelter, Alexandre J ; Wang, Minghua ; McKinnon, Crystal L ; Saab, Fabienne ; McGouran, Joanna F ; Century, Hannah ; Gersch, Malte ; Pittman, Marc S ; Marshall, C Gary ; Raynham, Tony M ; Simcox, Mary ; Stewart, Lorna M D ; McLoughlin, Sheila B ; Escobedo, Jaime A ; Bair, Kenneth W ; Dinsmore, Christopher J ; Hammonds, Tim R ; Kim, Sunkyu ; Urbé, Sylvie ; Clague, Michael J ; Kessler, Benedikt M ; Komander, David

Nature (London), 2017-10, Vol.550 (7677), p.481-486 [Periódico revisado por pares]

England: Nature Publishing Group

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20
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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