Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
van der Wel, Tom, Hilhorst, Riet, den Dulk, Hans, van den Hooven, Tim, Prins, Nienke M., Wijnakker, Joost A. P. M., Florea, Bogdan I., Lenselink, Eelke B., van Westen, Gerard J. P., Ruijtenbeek, Rob, Overkleeft, Herman S., Kaptein, Allard, Barf, Tjeerd, van der Stelt, Mario
Published in Nature communications (25.06.2020)
Published in Nature communications (25.06.2020)
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Journal Article
Potency and Selectivity of BTK Inhibitors in Clinical Development for B-Cell Malignancies
Kaptein, Allard, de Bruin, Gerjan, Emmelot-van Hoek, Maaike, van de Kar, Bas, de Jong, Anouk, Gulrajani, Michael, Demont, Dennis, Covey, Todd, Mittag, Diana, Barf, Tjeerd
Published in Blood (29.11.2018)
Published in Blood (29.11.2018)
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Journal Article
N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors
Barf, Tjeerd, Lehmann, Fredrik, Hammer, Kristin, Haile, Saba, Axen, Eva, Medina, Carmen, Uppenberg, Jonas, Svensson, Stefan, Rondahl, Lena, Lundbäck, Thomas
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
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Journal Article
Characterization of Irreversible Kinase Inhibitors by Directly Detecting Covalent Bond Formation: A Tool for Dissecting Kinase Drug Resistance
Klüter, Sabine, Simard, Jeffrey R, Rode, Haridas B, Grütter, Christian, Pawar, Vijaykumar, Raaijmakers, Hans C.A, Barf, Tjeerd A, Rabiller, Matthias, van Otterlo, Willem A.L, Rauh, Daniel
Published in Chembiochem : a European journal of chemical biology (10.12.2010)
Published in Chembiochem : a European journal of chemical biology (10.12.2010)
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Journal Article
Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target
Lehmann, Fredik, Haile, Saba, Axen, Eva, Medina, Carmen, Uppenberg, Jonas, Svensson, Stefan, Lundbäck, Thomas, Rondahl, Lena, Barf, Tjeerd
Published in Bioorganic & medicinal chemistry letters (06.09.2004)
Published in Bioorganic & medicinal chemistry letters (06.09.2004)
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Journal Article
Synthesis and Biological Activity of a Novel Class of Small Molecular Weight Peptidomimetic Competitive Inhibitors of Protein Tyrosine Phosphatase 1B
Larsen, Scott D, Barf, Tjeerd, Liljebris, Charlotta, May, Paul D, Ogg, Derek, O'Sullivan, Theresa J, Palazuk, Barbara J, Schostarez, Heinrich J, Stevens, F. Craig, Bleasdale, John E
Published in Journal of medicinal chemistry (31.01.2002)
Published in Journal of medicinal chemistry (31.01.2002)
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Journal Article
Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile
Barf, Tjeerd, Covey, Todd, Izumi, Raquel, van de Kar, Bas, Gulrajani, Michael, van Lith, Bart, van Hoek, Maaike, de Zwart, Edwin, Mittag, Diana, Demont, Dennis, Verkaik, Saskia, Krantz, Fanny, Pearson, Paul G, Ulrich, Roger, Kaptein, Allard
Published in The Journal of pharmacology and experimental therapeutics (01.11.2017)
Published in The Journal of pharmacology and experimental therapeutics (01.11.2017)
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Journal Article
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors
Hoogenboom, Niels, Demont, Dennis, de Zwart, Edwin, Verkaik, Saskia, Emmelot, Maaike, van de Kar, Bas, Kaptein, Allard, Barf, Tjeerd
Published in Bioorganic & medicinal chemistry letters (15.11.2021)
Published in Bioorganic & medicinal chemistry letters (15.11.2021)
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Journal Article
Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors
Podoll, Terry, Pearson, Paul G, Kaptein, Allard, Evarts, Jerry, de Bruin, Gerjan, Emmelot-van Hoek, Maaike, de Jong, Anouk, van Lith, Bart, Sun, Hao, Byard, Stephen, Fretland, Adrian, Hoogenboom, Niels, Barf, Tjeerd, Slatter, J Greg
Published in The Journal of pharmacology and experimental therapeutics (01.01.2023)
Published in The Journal of pharmacology and experimental therapeutics (01.01.2023)
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Journal Article
Discovery of quinoline-based irreversible BTK inhibitors
de Bruin, Gerjan, Demont, Dennis, de Zwart, Edwin, Verkaik, Saskia, Hoogenboom, Niels, van de Kar, Bas, van Lith, Bart, Emmelot- van Hoek, Maaike, Gulrajani, Michael, Covey, Todd, Kaptein, Allard, Barf, Tjeerd
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
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Journal Article
Abstract 2194: Preclinical pharmacological profiling of ACP-5862, the major metabolite of the covalent BTK inhibitor acalabrutinib, displays intrinsic BTK inhibitory activity
Kaptein, Allard, Podoll, Terry, Bruin, Gerjan de, Hoek, Maaike Emmelot-van, Jong, Anouk de, Lith, Bart van, Hoogenboom, Niels, Barf, Tjeerd, Ware, Joseph, Slatter, J. Greg
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract 4049: Preclinical pharmacology profile of GTX-0196: A novel, potent and highly selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of hematologic malignancies
Kaptein, Allard, Lain, Sonia, Brunen, Diede, van Wezel, Edward, Barf, Tjeerd
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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Journal Article
5-HT1D Receptor Agonist Properties of Novel 2-[5-[[(Trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and Their Use as Synthetic Intermediates
Barf, Tjeerd A, de Boer, Peter, Wikström, Håkan, Peroutka, Stephen J, Svensson, Kjell, Ennis, Michael D, Ghazal, Nabil B, McGuire, James C, Smith, Martin W
Published in Journal of medicinal chemistry (22.11.1996)
Published in Journal of medicinal chemistry (22.11.1996)
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Journal Article
Potency and Selectivity of BTK Inhibitors in Clinical Development for B-Cell Malignancies
Kaptein, Allard, de Bruin, Gerjan, Hoek, Maaike Emmelot-van, van de Kar, Bas, de Jong, Anouk, Gulrajani, Michael, Demont, Dennis, Covey, Todd, Mittag, Diana, Barf, Tjeerd
Published in Clinical lymphoma, myeloma and leukemia (01.09.2019)
Published in Clinical lymphoma, myeloma and leukemia (01.09.2019)
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Journal Article
Abstract 2624: The novel Bruton's tyrosine kinase inhibitor ACP-196 shows in vivo efficacy against human chronic lymphocytic leukemia cells xenografted to the NSG mouse model
Niemann, Carsten U., Montraveta, Arnau, Herman, Sarah E. M., Ingallinera, Tim, Barf, Tjeerd, Colomer, Dolors, Wiestner, Adrian
Published in Cancer research (Chicago, Ill.) (01.10.2014)
Published in Cancer research (Chicago, Ill.) (01.10.2014)
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Journal Article
Potential anxiolytic properties of R-(+)-8-OSO2CF3-PAT, a 5-HT1A receptor agonist
BARF, T, KORTE, S. M, KORTE-BOWS, G, SONESSON, C, DAMSMA, G, BOHUS, B, WIKSTRÖM, H
Published in European journal of pharmacology (22.02.1996)
Published in European journal of pharmacology (22.02.1996)
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Journal Article
Abstract 2596: ACP-196: a novel covalent Bruton's tyrosine kinase (Btk) inhibitor with improved selectivity and in vivo target coverage in chronic lymphocytic leukemia (CLL) patients
Covey, Todd, Barf, Tjeerd, Gulrajani, Michael, Krantz, Fanny, van Lith, Bart, Bibikova, Elena, van de Kar, Bas, de Zwart, Edwin, Hamdy, Ahmed, Izumi, Raquel, Kaptein, Allard
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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