Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Serafim, Ricardo A.M.; da Silva Santiago, Andre; Schwalm, Martin P.; Hu, Zexi; dos Reis, Caio V.; Takarada, Jessica E.; Mezzomo, Priscila; Massirer, Katlin B.; Kudolo, Mark; Gerstenecker, Stefan; Chaikuad, Apirat; Zender, Lars; Knapp, Stefan; Laufer, Stefan; Cou?ago, Rafael M.; Gehringer, Matthias

doi:10.1021/acs.jmedchem.1c01165

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Journal Article · 31 January 2022 · J. Med. Chem.

DOI:https://doi.org/10.1021/acs.jmedchem.1c01165· OSTI ID:1847130

Serafim, Ricardo A.M.; da Silva Santiago, Andre; Schwalm, Martin P.; Hu, Zexi; dos Reis, Caio V.; Takarada, Jessica E.; Mezzomo, Priscila; Massirer, Katlin B.; Kudolo, Mark; Gerstenecker, Stefan; Chaikuad, Apirat; Zender, Lars; Knapp, Stefan; Laufer, Stefan; Cou?ago, Rafael M.; Gehringer, Matthias

Research Organization:: Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)

Sponsoring Organization:: DOE - Office Of Science; NIH

OSTI ID:: 1847130

Journal Information:: J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (4) Vol. 65

Country of Publication:: United States

Language:: ENGLISH

References (75)

Mps1 kinase regulates tumor cell viability via its novel role in mitochondria Zhang, X.; Ling, Y.; Guo, Y. Cell Death & Disease, Vol. 7, Issue 7 https://doi.org/10.1038/cddis.2016.193	journal	July 2016
Systematic Study of the Glutathione Reactivity of N -Phenylacrylamides: 2. Effects of Acrylamide Substitution Birkholz, Adam; Kopecky, David J.; Volak, Laurie P. Journal of Medicinal Chemistry, Vol. 63, Issue 20 https://doi.org/10.1021/acs.jmedchem.0c00749	journal	September 2020
Covalent inhibitors design and discovery De Cesco, Stephane; Kurian, Jerry; Dufresne, Caroline European Journal of Medicinal Chemistry, Vol. 138 https://doi.org/10.1016/j.ejmech.2017.06.019	journal	September 2017
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma Joshi, Jaya Julie; Coffey, Heather; Corcoran, Erik Cancer Research, Vol. 77, Issue 24 https://doi.org/10.1158/0008-5472.CAN-17-1865	journal	December 2017
Mps1 Phosphorylates Borealin to Control Aurora B Activity and Chromosome Alignment Jelluma, Nannette; Brenkman, Arjan B.; van den Broek, Niels J. F. Cell, Vol. 132, Issue 2 https://doi.org/10.1016/j.cell.2007.11.046	journal	January 2008
Unmasking senescence: context-dependent effects of SASP in cancer Faget, Douglas V.; Ren, Qihao; Stewart, Sheila A. Nature Reviews Cancer, Vol. 19, Issue 8 https://doi.org/10.1038/s41568-019-0156-2	journal	June 2019
Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK Forster, Michael; Liang, Xiaojun Julia; Schröder, Martin International Journal of Molecular Sciences, Vol. 21, Issue 23 https://doi.org/10.3390/ijms21239269	journal	December 2020
Targeting the Mitotic Checkpoint to Kill Tumor Cells Janssen, Aniek; Kops, Geert J.; Medema, René H. Hormones and Cancer, Vol. 2, Issue 2 https://doi.org/10.1007/s12672-010-0059-x	journal	December 2010
Rapidly distinguishing reversible and irreversible CYP450 inhibitors by using fluorometric kinetic analyses Yan, Z.; Rafferty, B.; Caldwell, G. W. European Journal of Drug Metabolism and Pharmacokinetics, Vol. 27, Issue 4 https://doi.org/10.1007/BF03192339	journal	December 2002
Features and development of Coot Emsley, P.; Lohkamp, B.; Scott, W. G. Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 4 https://doi.org/10.1107/S0907444910007493	journal	March 2010
TTK inhibition radiosensitizes basal-like breast cancer through impaired homologous recombination Chandler, Benjamin C.; Moubadder, Leah; Ritter, Cassandra L. Journal of Clinical Investigation, Vol. 130, Issue 2 https://doi.org/10.1172/JCI130435	journal	December 2019
Kinase Drug Discovery – What’s Next in the Field? Cohen, Philip; Alessi, Dario R. ACS Chemical Biology, Vol. 8, Issue 1 https://doi.org/10.1021/cb300610s	journal	December 2012
Characterization of novel MPS1 inhibitors with preclinical anticancer activity Jemaà, M.; Galluzzi, L.; Kepp, O. Cell Death & Differentiation, Vol. 20, Issue 11 https://doi.org/10.1038/cdd.2013.105	journal	August 2013
Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2 Berger, Benedict-Tilman; Amaral, Marta; Kokh, Daria B. Cell Chemical Biology, Vol. 28, Issue 5 https://doi.org/10.1016/j.chembiol.2021.01.003	journal	May 2021
Mitotic checkpoint kinase Mps1/TTK predicts prognosis of colon cancer patients and regulates tumor proliferation and differentiation via PKCα/ERK1/2 and PI3K/Akt pathway Zhang, Li; Jiang, Baofei; Zhu, Ni Medical Oncology, Vol. 37, Issue 1 https://doi.org/10.1007/s12032-019-1320-y	journal	November 2019
Binding Kinetics Survey of the Drugged Kinome Georgi, Victoria; Schiele, Felix; Berger, Benedict-Tilman Journal of the American Chemical Society, Vol. 140, Issue 46 https://doi.org/10.1021/jacs.8b08048	journal	October 2018
Mechanism-Based Inhibition: Deriving K _I and k _inact Directly from Time-Dependent IC ₅₀ Values Krippendorff, Ben-Fillippo; Neuhaus, Roland; Lienau, Philip Journal of Biomolecular Screening, Vol. 14, Issue 8 https://doi.org/10.1177/1087057109336751	journal	August 2009
Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries Sung, Hyuna; Ferlay, Jacques; Siegel, Rebecca L. CA: A Cancer Journal for Clinicians, Vol. 71, Issue 3 https://doi.org/10.3322/caac.21660	journal	February 2021
Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase Schulze, Volker K.; Klar, Ulrich; Kosemund, Dirk Journal of Medicinal Chemistry, Vol. 63, Issue 15 https://doi.org/10.1021/acs.jmedchem.9b02035	journal	April 2020
Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks Barf, Tjeerd; Kaptein, Allard Journal of Medicinal Chemistry, Vol. 55, Issue 14 https://doi.org/10.1021/jm3003203	journal	June 2012
DAP Kinase-Related Apoptosis-Inducing Protein Kinase 2 (DRAK2) Is a Key Regulator and Molecular Marker in Chronic Lymphocytic Leukemia Szoltysek, Katarzyna; Ciardullo, Carmela; Zhou, Peixun International Journal of Molecular Sciences, Vol. 21, Issue 20 https://doi.org/10.3390/ijms21207663	journal	October 2020
Targeting the Mitotic Checkpoint for Cancer Therapy with NMS-P715, an Inhibitor of MPS1 Kinase Colombo, Riccardo; Caldarelli, Marina; Mennecozzi, Milena Cancer Research, Vol. 70, Issue 24 https://doi.org/10.1158/0008-5472.CAN-10-2101	journal	December 2010
Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity Uitdehaag, Joost C. M.; de Man, Jos; Willemsen-Seegers, Nicole Journal of Molecular Biology, Vol. 429, Issue 14 https://doi.org/10.1016/j.jmb.2017.05.014	journal	July 2017
The Dark Kinase Knowledgebase: an online compendium of knowledge and experimental results of understudied kinases Berginski, Matthew E.; Moret, Nienke; Liu, Changchang Nucleic Acids Research, Vol. 49, Issue D1 https://doi.org/10.1093/nar/gkaa853	journal	October 2020
MolProbity : all-atom structure validation for macromolecular crystallography Chen, Vincent B.; Arendall, W. Bryan; Headd, Jeffrey J. Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 1 https://doi.org/10.1107/S0907444909042073	journal	December 2009
Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity Wengner, Antje M.; Siemeister, Gerhard; Koppitz, Marcus Molecular Cancer Therapeutics, Vol. 15, Issue 4 https://doi.org/10.1158/1535-7163.MCT-15-0500	journal	February 2016
High-throughput production of human proteins for crystallization: The SGC experience Savitsky, Pavel; Bray, James; Cooper, Christopher D. O. Journal of Structural Biology, Vol. 172, Issue 1 https://doi.org/10.1016/j.jsb.2010.06.008	journal	October 2010
The resurgence of covalent drugs Singh, Juswinder; Petter, Russell C.; Baillie, Thomas A. Nature Reviews Drug Discovery, Vol. 10, Issue 4 https://doi.org/10.1038/nrd3410	journal	April 2011
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer Weiss, Andreas; Adler, Flavia; Buhles, Alexandra Molecular Cancer Therapeutics, Vol. 18, Issue 12 https://doi.org/10.1158/1535-7163.MCT-18-1291	journal	August 2019
Drug–target residence time and its implications for lead optimization Copeland, Robert A.; Pompliano, David L.; Meek, Thomas D. Nature Reviews Drug Discovery, Vol. 5, Issue 9 https://doi.org/10.1038/nrd2082	journal	August 2006
First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant FGF19 Signaling as a Driver Event in Hepatocellular Carcinoma Kim, Richard D.; Sarker, Debashis; Meyer, Tim Cancer Discovery, Vol. 9, Issue 12 https://doi.org/10.1158/2159-8290.CD-19-0555	journal	October 2019
First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway Hagel, M.; Miduturu, C.; Sheets, M. Cancer Discovery, Vol. 5, Issue 4 https://doi.org/10.1158/2159-8290.CD-14-1029	journal	March 2015
Covalent inhibitors: back on track? Gehringer, Matthias Future Medicinal Chemistry, Vol. 12, Issue 15 https://doi.org/10.4155/fmc-2020-0118	journal	August 2020
Hallmarks of Cancer: The Next Generation Hanahan, Douglas; Weinberg, Robert A. Cell, Vol. 144, Issue 5 https://doi.org/10.1016/j.cell.2011.02.013	journal	March 2011
Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective Wang, Shutao; Zhang, Muxin; Liang, Di European Journal of Medicinal Chemistry, Vol. 175 https://doi.org/10.1016/j.ejmech.2019.04.047	journal	August 2019
A signature of chromosomal instability inferred from gene expression profiles predicts clinical outcome in multiple human cancers Carter, Scott L.; Eklund, Aron C.; Kohane, Isaac S. Nature Genetics, Vol. 38, Issue 9 https://doi.org/10.1038/ng1861	journal	August 2006
Bub3 reads phosphorylated MELT repeats to promote spindle assembly checkpoint signaling Primorac, Ivana; Weir, John R.; Chiroli, Elena eLife, Vol. 2 https://doi.org/10.7554/eLife.01030	journal	September 2013
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity Anastassiadis, Theonie; Deacon, Sean W.; Devarajan, Karthik Nature Biotechnology, Vol. 29, Issue 11 https://doi.org/10.1038/nbt.2017	journal	October 2011
Overview of the CCP 4 suite and current developments Winn, Martyn D.; Ballard, Charles C.; Cowtan, Kevin D. Acta Crystallographica Section D Biological Crystallography, Vol. 67, Issue 4 https://doi.org/10.1107/S0907444910045749	journal	March 2011
High levels of the Mps1 checkpoint protein are protective of aneuploidy in breast cancer cells Daniel, Jewel; Coulter, Jonathan; Woo, Ju-Hyung Proceedings of the National Academy of Sciences, Vol. 108, Issue 13 https://doi.org/10.1073/pnas.1007645108	journal	March 2011
Inhibition of mitotic kinase Mps1 promotes cell death in neuroblastoma Simon Serrano, Sonia; Sime, Wondossen; Abassi, Yasmin Scientific Reports, Vol. 10, Issue 1 https://doi.org/10.1038/s41598-020-68829-y	journal	July 2020
Pharmacokinetics and the drug–target residence time concept Dahl, Göran; Akerud, Tomas Drug Discovery Today, Vol. 18, Issue 15-16 https://doi.org/10.1016/j.drudis.2013.02.010	journal	August 2013
Mobocertinib: First Approval Markham, Anthony Drugs, Vol. 81, Issue 17 https://doi.org/10.1007/s40265-021-01632-9	journal	October 2021
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology Gehringer, Matthias; Laufer, Stefan A. Journal of Medicinal Chemistry, Vol. 62, Issue 12 https://doi.org/10.1021/acs.jmedchem.8b01153	journal	December 2018
Mps1 kinase activity restrains anaphase during an unperturbed mitosis and targets Mad2 to kinetochores Tighe, Anthony; Staples, Oliver; Taylor, Stephen Journal of Cell Biology, Vol. 181, Issue 6 https://doi.org/10.1083/jcb.200712028	journal	June 2008
Effects of the Selective MPS1 Inhibitor MPS1-IN-3 on Glioblastoma Sensitivity to Antimitotic Drugs Tannous, Bakhos A.; Kerami, Mariam; Van der Stoop, Petra M. JNCI: Journal of the National Cancer Institute, Vol. 105, Issue 17 https://doi.org/10.1093/jnci/djt168	journal	August 2013
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d ]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N ² -(2-Ethoxy-4-(4-methyl-4 H -1,2,4-triazol-3-yl)phenyl)-6-methyl- N ⁸ -neopentylpyrido[3,4- d ]pyrimidine-2,8-diamine (BOS172722) Woodward, Hannah L.; Innocenti, Paolo; Cheung, Kwai-Ming J. Journal of Medicinal Chemistry, Vol. 61, Issue 18 https://doi.org/10.1021/acs.jmedchem.8b00690	journal	September 2018
The Cysteinome of Protein Kinases as a Target in Drug Development Chaikuad, Apirat; Koch, Pierre; Laufer, Stefan A. Angewandte Chemie International Edition, Vol. 57, Issue 16 https://doi.org/10.1002/anie.201707875	journal	February 2018
Target engagement and drug residence time can be observed in living cells with BRET Robers, Matthew B.; Dart, Melanie L.; Woodroofe, Carolyn C. Nature Communications, Vol. 6, Issue 1 https://doi.org/10.1038/ncomms10091	journal	December 2015
Death-associated protein kinase (DAPK) family modulators: Current and future therapeutic outcomes Farag, Ahmed Karam; Roh, Eun Joo Medicinal Research Reviews, Vol. 39, Issue 1 https://doi.org/10.1002/med.21518	journal	June 2018
Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction Yung-Chi, Cheng; Prusoff, William H. Biochemical Pharmacology, Vol. 22, Issue 23 https://doi.org/10.1016/0006-2952(73)90196-2	journal	December 1973
Advances in covalent kinase inhibitors Abdeldayem, Ayah; Raouf, Yasir S.; Constantinescu, Stefan N. Chemical Society Reviews, Vol. 49, Issue 9 https://doi.org/10.1039/C9CS00720B	journal	January 2020
MPS1/Mph1 phosphorylates the kinetochore protein KNL1/Spc7 to recruit SAC components Yamagishi, Yuya; Yang, Ching-Hui; Tanno, Yuji Nature Cell Biology, Vol. 14, Issue 7 https://doi.org/10.1038/ncb2515	journal	June 2012
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors Huang, Minhao; Huang, Yongjun; Guo, Jing European Journal of Medicinal Chemistry, Vol. 211 https://doi.org/10.1016/j.ejmech.2020.113023	journal	February 2021
XDS Kabsch, Wolfgang Acta Crystallographica Section D Biological Crystallography, Vol. 66, Issue 2 https://doi.org/10.1107/S0907444909047337	journal	January 2010
Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs) Roskoski, Robert Pharmacological Research, Vol. 165 https://doi.org/10.1016/j.phrs.2021.105422	journal	March 2021
Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2) Gerstenecker, Stefan; Haarer, Lisa; Schröder, Martin Cancers, Vol. 13, Issue 20 https://doi.org/10.3390/cancers13205133	journal	October 2021
Synthetic Lethal Strategy Identifies a Potent and Selective TTK and CLK1/2 Inhibitor for Treatment of Triple-Negative Breast Cancer with a Compromised G ₁ –S Checkpoint Zhu, Dan; Xu, Shuichan; Deyanat-Yazdi, Gordafaried Molecular Cancer Therapeutics, Vol. 17, Issue 8 https://doi.org/10.1158/1535-7163.MCT-17-1084	journal	June 2018
Chemical Probes for Understudied Kinases: Challenges and Opportunities Serafim, Ricardo A. M.; Elkins, Jonathan M.; Zuercher, William J. Journal of Medicinal Chemistry, Vol. 65, Issue 2 https://doi.org/10.1021/acs.jmedchem.1c00980	journal	September 2021
TTK Inhibitors as a Targeted Therapy for CTNNB1 ( β -catenin) Mutant Cancers Zaman, Guido J. R.; de Roos, Jeroen A. D. M.; Libouban, Marion A. A. Molecular Cancer Therapeutics, Vol. 16, Issue 11 https://doi.org/10.1158/1535-7163.MCT-17-0342	journal	July 2017
Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1–C-Mad2 core complex Hewitt, Laura; Tighe, Anthony; Santaguida, Stefano The Journal of Cell Biology, Vol. 190, Issue 1 https://doi.org/10.1083/jcb.201002133	journal	July 2010
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors Keeley, A.; Ábrányi-Balogh, P.; Keserű, G. M. MedChemComm, Vol. 10, Issue 2 https://doi.org/10.1039/C8MD00327K	journal	January 2019
A quantitative analysis of kinase inhibitor selectivity Karaman, Mazen W.; Herrgard, Sanna; Treiber, Daniel K. Nature Biotechnology, Vol. 26, Issue 1 https://doi.org/10.1038/nbt1358	journal	January 2008
Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance Schwartz, P. A.; Kuzmic, P.; Solowiej, J. Proceedings of the National Academy of Sciences, Vol. 111, Issue 1 https://doi.org/10.1073/pnas.1313733111	journal	December 2013
Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry Reddi, Rambabu N.; Resnick, Efrat; Rogel, Adi Journal of the American Chemical Society, Vol. 143, Issue 13 https://doi.org/10.1021/jacs.0c10644	journal	March 2021
Systematic Study of the Glutathione (GSH) Reactivity of N -Arylacrylamides: 1. Effects of Aryl Substitution Cee, Victor J.; Volak, Laurie P.; Chen, Yuping Journal of Medicinal Chemistry, Vol. 58, Issue 23 https://doi.org/10.1021/acs.jmedchem.5b01018	journal	November 2015
TC Mps1 12, a novel Mps1 inhibitor, suppresses the growth of hepatocellular carcinoma cells via the accumulation of chromosomal instability: Effect of Mps1 inhibitor on hepatocellular carcinoma cells Choi, Minji; Min, Yoo Hong; Pyo, Jaehyuk British Journal of Pharmacology, Vol. 174, Issue 12 https://doi.org/10.1111/bph.13782	journal	April 2017
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function Kwiatkowski, Nicholas; Jelluma, Nannette; Filippakopoulos, Panagis Nature Chemical Biology, Vol. 6, Issue 5 https://doi.org/10.1038/nchembio.345	journal	April 2010
Phosphodependent Recruitment of Bub1 and Bub3 to Spc7/KNL1 by Mph1 Kinase Maintains the Spindle Checkpoint Shepperd, Lindsey A.; Meadows, John C.; Sochaj, Alicja M. Current Biology, Vol. 22, Issue 10 https://doi.org/10.1016/j.cub.2012.03.051	journal	May 2012
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement Vasta, James D.; Corona, Cesear R.; Wilkinson, Jennifer Cell Chemical Biology, Vol. 25, Issue 2 https://doi.org/10.1016/j.chembiol.2017.10.010	journal	February 2018
Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer Mason, Jacqueline M.; Wei, Xin; Fletcher, Graham C. Proceedings of the National Academy of Sciences, Vol. 114, Issue 12 https://doi.org/10.1073/pnas.1700234114	journal	March 2017
The MPS1 Family of Protein Kinases Liu, Xuedong; Winey, Mark Annual Review of Biochemistry, Vol. 81, Issue 1 https://doi.org/10.1146/annurev-biochem-061611-090435	journal	July 2012
Inhibition of the spindle assembly checkpoint kinase TTK enhances the efficacy of docetaxel in a triple-negative breast cancer model Maia, A. R. R.; de Man, J.; Boon, U. Annals of Oncology, Vol. 26, Issue 10 https://doi.org/10.1093/annonc/mdv293	journal	October 2015
Selective Inhibition of Pancreatic Ductal Adenocarcinoma Cell Growth by the Mitotic MPS1 Kinase Inhibitor NMS-P715 Slee, Roger B.; Grimes, Brenda R.; Bansal, Ruchi Molecular Cancer Therapeutics, Vol. 13, Issue 2 https://doi.org/10.1158/1535-7163.MCT-13-0324	journal	November 2013
Utility of the dual-specificity protein kinase TTK as a therapeutic target for intrahepatic spread of liver cancer Miao, Ruoyu; Wu, Yan; Zhang, Haohai Scientific Reports, Vol. 6, Issue 1 https://doi.org/10.1038/srep33121	journal	September 2016

Similar Records

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Journal Article · 2022 · J. Med. Chem. · OSTI ID:1860409

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

Journal Article · 2015 · Proc. Natl. Acad. Sci. USA · OSTI ID:1164187

Development of Selective Covalent Janus Kinase 3 Inhibitors

Journal Article · 2015 · Journal of Medicinal Chemistry · OSTI ID:1430281

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Citation Formats

References (75)

Similar Records

Related Subjects