A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets
Uitdehaag, Joost CM, Verkaar, Folkert, Alwan, Husam, de Man, Jos, Buijsman, Rogier C, Zaman, Guido JR
Published in British journal of pharmacology (01.06.2012)
Published in British journal of pharmacology (01.06.2012)
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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, Prinsen, Martine B W, de Man, Jos, Buijsman, Rogier C, Uitdehaag, Joost C M
Published in Molecular cancer therapeutics (01.11.2017)
Published in Molecular cancer therapeutics (01.11.2017)
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Properties and applications of starch-converting enzymes of the α-amylase family
van der Maarel, Marc J.E.C, van der Veen, Bart, Uitdehaag, Joost C.M, Leemhuis, Hans, Dijkhuizen, L
Published in Journal of Biotechnology (28.03.2002)
Published in Journal of Biotechnology (28.03.2002)
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Book Review
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3D Modeling of Novel Transforming JAK Mutations in T-Cell Acute Lymphoblastic Leukemia Reveals Altered Pseudokinase-Kinase Domain Interactions That Result in Constitutive JAK Kinase Activity
Canté-Barrett, Kirsten, Uitdehaag, Joost CM, Buijs-Gladdines, Jessica GCAM, Smits, Wilco K, Buijsman, Rogier C, Zaman, Guido JR, Pieters, Rob, Meijerink, Jules PP
Published in Blood (03.12.2015)
Published in Blood (03.12.2015)
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Abstract 2646: The unique binding mode of NTRC 0066-0, a novel inhibitor of the spindle assembly checkpoint kinase TTK (Mps1), leads to long target residence time and potent antitumor activity
de Man, Jos, Uitdehaag, Joost C.M., Willemsen-Seegers, Nicole, Sterrenburg, Jan Gerard, de Wit, Joeri J.P., de Roos, Jeroen A.D.M., Prinsen, Martine B.W., Buijsman, Rogier C., Zaman, Guido J.R.
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors
Cai, Jiaqiang, Robinson, John, Belshaw, Simone, Everett, Kathryn, Fradera, Xavier, van Zeeland, Mario, van Berkom, Leon, van Rijnsbergen, Peter, Popplestone, Lucy, Baugh, Mark, Dempster, Maureen, Bruin, John, Hamilton, William, Kinghorn, Emma, Westwood, Paul, Kerr, Jennifer, Rankovic, Zoran, Arbuckle, Wullie, Bennett, D. Jonathan, Jones, Philip S., Long, Clive, Martin, Iain, Uitdehaag, Joost C.M., Meulemans, Tommi
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
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Journal Article
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important
Cai, Jiaqiang, Fradera, Xavier, van Zeeland, Mario, Dempster, Maureen, Cameron, Kenneth S., Bennett, D. Jonathan, Robinson, John, Popplestone, Lucy, Baugh, Mark, Westwood, Paul, Bruin, John, Hamilton, William, Kinghorn, Emma, Long, Clive, Uitdehaag, Joost C.M.
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
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Journal Article
Multidimensional profiling of CSF1R screening hits and inhibitors: assessing cellular activity, target residence time, and selectivity in a higher throughput way
Uitdehaag, Joost C M, Sünnen, Cecile M, van Doornmalen, Antoon M, de Rouw, Nikki, Oubrie, Arthur, Azevedo, Rita, Ziebell, Michael, Nickbarg, Elliott, Karstens, Willem-Jan, Ruygrok, Simone
Published in Journal of biomolecular screening (01.10.2011)
Published in Journal of biomolecular screening (01.10.2011)
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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors
Cai, Jiaqiang, Baugh, Mark, Black, Darcey, Long, Clive, Jonathan Bennett, D., Dempster, Maureen, Fradera, Xavier, Gillespie, Jonathan, Andrews, Fiona, Boucharens, Sylviane, Bruin, John, Cameron, Kenneth S., Cumming, Iain, Hamilton, William, Jones, Philip S., Kaptein, Allard, Kinghorn, Emma, Maidment, Maurice, Martin, Iain, Mitchell, Ann, Rankovic, Zoran, Robinson, John, Scullion, Paul, Uitdehaag, Joost C.M., Vink, Paul, Westwood, Paul, van Zeeland, Mario, van Berkom, Leon, Bastiani, Martijn, Meulemans, Tommi
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
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2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors
Cai, Jiaqiang, Bennett, D. Jonathan, Rankovic, Zoran, Dempster, Maureen, Fradera, Xavier, Gillespie, Jonathan, Cumming, Iain, Finlay, William, Baugh, Mark, Boucharens, Sylviane, Bruin, John, Cameron, Kenneth S., Hamilton, William, Kerr, Jennifer, Kinghorn, Emma, McGarry, George, Robinson, John, Scullion, Paul, Uitdehaag, Joost C.M., van Zeeland, Mario, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, Francois, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
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Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: Improving selectivity over hERG
Rankovic, Zoran, Cai, Jiaqiang, Kerr, Jennifer, Fradera, Xavier, Robinson, John, Mistry, Ashvin, Finlay, William, McGarry, George, Andrews, Fiona, Caulfield, Wilson, Cumming, Iain, Dempster, Maureen, Waller, John, Arbuckle, Wullie, Anderson, Mark, Martin, Iain, Mitchell, Ann, Long, Clive, Baugh, Mark, Westwood, Paul, Kinghorn, Emma, Jones, Phil, Uitdehaag, Joost C.M., van Zeeland, Mario, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, François, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric
Published in Bioorganic & medicinal chemistry letters (01.11.2010)
Published in Bioorganic & medicinal chemistry letters (01.11.2010)
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Comparison of the Cancer Gene Targeting and Biochemical Selectivities of All Targeted Kinase Inhibitors Approved for Clinical Use: e92146
Uitdehaag, Joost CM, de Roos, D M, van Doornmalen, Antoon M, Prinsen, Martine BW, de Man, Jos, Tanizawa, Yoshinori, Kawase, Yusuke, Yoshino, Kohichiro, Buijsman, Rogier C, Zaman, Guido JR
Published in PloS one (01.03.2014)
Published in PloS one (01.03.2014)
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Pharmacological validation of TDO as a target for Parkinson’s disease
Perez‐Pardo, Paula, Grobben, Yvonne, Willemsen‐Seegers, Nicole, Hartog, Mitch, Tutone, Michaela, Muller, Michelle, Adolfs, Youri, Pasterkamp, Ronald Jeroen, Vu‐Pham, Diep, Doornmalen, Antoon M., Cauter, Freek, Wit, Joeri, Gerard Sterrenburg, Jan, Uitdehaag, Joost C.M., Man, Jos, Buijsman, Rogier C., Zaman, Guido J.R., Kraneveld, Aletta D.
Published in The FEBS journal (01.07.2021)
Published in The FEBS journal (01.07.2021)
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