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18 Results  for Everything (Includes Articles)

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1
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Irreversible protein kinase inhibitors: balancing the benefits and risks

Barf, Tjeerd ; Kaptein, Allard

Journal of medicinal chemistry, 26 July 2012, Vol.55(14), pp.6243-62 [Peer Reviewed Journal]

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Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series

Oubrie, Arthur ; Kaptein, Allard ; de Zwart, Edwin ; Hoogenboom, Niels ; Goorden, Rianne ; van de Kar, Bas ; van Hoek, Maaike ; de Kimpe, Vera ; van Der Heijden, Ruud ; Borsboom, Judith ; Kazemier, Bert ; de Roos, Jeroen ; Scheffers, Michiel ; Lommerse, Jos ; Schultz-Fademrecht, Carsten ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 01 January 2012, Vol.22(1), pp.613-618 [Peer Reviewed Journal]

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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

The Journal of pharmacology and experimental therapeutics, November 2017, Vol.363(2), pp.240-252 [Peer Reviewed Journal]

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Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors

Kaptein, Allard ; Oubrie, Arthur ; Zwart, Edwin de ; Hoogenboom, Niels ; Wit, Joeri de ; Kar, Bas van de ; Hoek, Maaike van ; Vogel, Gerard ; Kimpe, Vera de ; Schultz-Fademrecht, Carsten ; Borsboom, Judith ; Zeeland, Mario van ; Versteegh, Judith ; Kazemier, Bert ; Roos, Jeroen de ; Wijnands, Frank ; Dulos, John ; Jaeger, Martin ; Leandro-Garcia, Paula ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(12), pp.3823-3827 [Peer Reviewed Journal]

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Structure-based lead identification of ATP-competitive MK2 inhibitors

Barf, Tjeerd ; Kaptein, Allard ; Wilde, Sander de ; Heijden, Ruud van Der ; Someren, Richard van ; Demont, Dennis ; Schultz-Fademrecht, Carsten ; Versteegh, Judith ; Zeeland, Mario van ; Seegers, Nicole ; Kazemier, Bert ; Kar, Bas van de ; Hoek, Maaike van ; Roos, Jeroen de ; Klop, Henri ; Smeets, Ruben ; Hofstra, Claudia ; Hornberg, Jorrit ; Oubrie, Arthur

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(12), pp.3818-3822 [Peer Reviewed Journal]

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5-(Sulfonyl)oxy-tryptamines and ethylamino side chain restricted derivatives. Structure–affinity relationships for h5-HT 1B and h5-HT 1D receptors
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5-(Sulfonyl)oxy-tryptamines and ethylamino side chain restricted derivatives. Structure–affinity relationships for h5-HT 1B and h5-HT 1D receptors

Barf, Tjeerd ; Wikström, Håkan ; Pauwels, Petrus J. ; Palmier, Christiane ; Tardif, Stephanie ; Lundmark, Max ; Sundell, Staffan

Bioorganic & Medicinal Chemistry, 09/1998, Vol.6(9), pp.1469-1479 [Peer Reviewed Journal]

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7
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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

Journal of medicinal chemistry, 31 January 2002, Vol.45(3), pp.598-622 [Peer Reviewed Journal]

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8
5-HT 1D Receptor Agonist Properties of Novel 2-[5-[[(Trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and Their Use as Synthetic Intermediates
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5-HT 1D 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.

Journal of Medicinal Chemistry, 01/1996, Vol.39(24), pp.4717-4726 [Peer Reviewed Journal]

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9
Arylsulfonamidothiazoles as a New Class of Potential Antidiabetic Drugs. Discovery of Potent and Selective Inhibitors of the 11β-Hydroxysteroid Dehydrogenase Type 1
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Arylsulfonamidothiazoles as a New Class of Potential Antidiabetic Drugs. Discovery of Potent and Selective Inhibitors of the 11β-Hydroxysteroid Dehydrogenase Type 1

Barf, Tjeerd ; Vallgårda, Jerk ; Emond, Rikard ; Häggström, Charlotta ; Kurz, Guido ; Nygren, Alf ; Larwood, Vivienne ; Mosialou, Erifili ; Axelsson, Kent ; Olsson, Rolf ; Engblom, Lars ; Edling, Naimie ; Rönquist-Nii, Yuko ; Öhman, Birgitta ; Alberts

Journal of Medicinal Chemistry, 08/2002, Vol.45(18), pp.3813-3815 [Peer Reviewed Journal]

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Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1

Barf, Tjeerd ; Vallgårda, Jerk ; Emond, Rikard ; Häggström, Charlotta ; Kurz, Guido ; Nygren, Alf ; Larwood, Vivienne ; Mosialou, Erifili ; Axelsson, Kent ; Olsson, Rolf ; Engblom, Lars ; Edling, Naimie ; Rönquist-Nii, Yuko ; Ohman, Birgitta ; Alberts, Peteris ; Abrahmsén

Journal of medicinal chemistry, 29 August 2002, Vol.45(18), pp.3813-5 [Peer Reviewed Journal]

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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

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(6), pp.1745-1748 [Peer Reviewed Journal]

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Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1 H)-ones: a novel class of selective human A-FABP inhibitors

Ringom, Rune ; Axen, Eva ; Uppenberg, Jonas ; Lundbäck, Thomas ; Rondahl, Lena ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(17), pp.4449-4452 [Peer Reviewed Journal]

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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

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(17), pp.4445-4448 [Peer Reviewed Journal]

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14
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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

Clinical Lymphoma, Myeloma and Leukemia, September 2019, Vol.19, pp.S316-S317 [Peer Reviewed Journal]

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15
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Active site variability of type 1 11β-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons

Hult, Malin ; Shafqat, Naeem ; Elleby, Björn ; Mitschke, Doreen ; Svensson, Stefan ; Forsgren, Margareta ; Barf, Tjeerd ; Vallgårda, Jerk ; Abrahmsen, Lars ; Oppermann, Udo

Molecular and Cellular Endocrinology, 2006, Vol.248(1), pp.26-33 [Peer Reviewed Journal]

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16
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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

Bioorganic & Medicinal Chemistry Letters, 15 July 2020, Vol.30(14) [Peer Reviewed Journal]

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Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis via SYK activation

Van Der Wel, Tom ; Hilhorst, Riet ; Den Dulk, Hans ; Van Den Hooven, Tim ; Prins, Nienke ; Wijnakker, Joost ; Florea, Bogdan ; Lenselink, Eelke ; Van Westen, Gerard ; Ruijtenbeek, Rob ; Overkleeft, Herman ; Barf, Tjeerd ; Van Der Stelt, Mario Van Der Stelt, Mario (pacrepositoryorg)

BioRxiv, Nov 13, 2019

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Characterization of the radioactive metabolites of the 5-HT 1A receptor radioligand, [O- methl- 11C]WAY-100635, in monkey and human plasma by HPLC: Comparison of the behaviour of an identified radioactive metabolite with parent radioligand in monkey using PET

Osman, Safiye ; Lundkvist, Camilla ; Pike, Victor W ; Halldin, Christer ; Mccarron, Julie A ; Swahn, Carl-Gunnar ; Ginovart, Natalie ; Luthra, Sajinder K ; Bench, Christopher J ; Grasby, Paul M ; Wikström, Håkan ; Barf, Tjeerd ; Cliffe, Ian A ; Fletcher, Allan ; Farde, Lars

Nuclear Medicine and Biology, 1996, Vol.23(5), pp.627-634 [Peer Reviewed Journal]

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