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Items: 21

1.

Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile.

Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, van Hoek M, de Zwart E, Mittag D, Demont D, Verkaik S, Krantz F, Pearson PG, Ulrich R, Kaptein A.

J Pharmacol Exp Ther. 2017 Nov;363(2):240-252. doi: 10.1124/jpet.117.242909. Epub 2017 Sep 7.

PMID:
28882879
2.

Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study.

Liu N, Hoogendoorn S, van de Kar B, Kaptein A, Barf T, Driessen C, Filippov DV, van der Marel GA, van der Stelt M, Overkleeft HS.

Org Biomol Chem. 2015 May 14;13(18):5147-57. doi: 10.1039/c5ob00474h.

PMID:
25849561
3.

Irreversible protein kinase inhibitors: balancing the benefits and risks.

Barf T, Kaptein A.

J Med Chem. 2012 Jul 26;55(14):6243-62. doi: 10.1021/jm3003203. Epub 2012 Jun 8. Review. No abstract available.

PMID:
22621397
4.

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

Oubrie A, Kaptein A, de Zwart E, Hoogenboom N, Goorden R, van de Kar B, van Hoek M, de Kimpe V, van der Heijden R, Borsboom J, Kazemier B, de Roos J, Scheffers M, Lommerse J, Schultz-Fademrecht C, Barf T.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):613-8. doi: 10.1016/j.bmcl.2011.10.071. Epub 2011 Nov 3.

PMID:
22119462
5.

Structure-based lead identification of ATP-competitive MK2 inhibitors.

Barf T, Kaptein A, de Wilde S, van der Heijden R, van Someren R, Demont D, Schultz-Fademrecht C, Versteegh J, van Zeeland M, Seegers N, Kazemier B, van de Kar B, van Hoek M, de Roos J, Klop H, Smeets R, Hofstra C, Hornberg J, Oubrie A.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3818-22. doi: 10.1016/j.bmcl.2011.04.018. Epub 2011 Apr 16.

PMID:
21565500
6.

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

Kaptein A, Oubrie A, de Zwart E, Hoogenboom N, de Wit J, van de Kar B, van Hoek M, Vogel G, de Kimpe V, Schultz-Fademrecht C, Borsboom J, van Zeeland M, Versteegh J, Kazemier B, de Roos J, Wijnands F, Dulos J, Jaeger M, Leandro-Garcia P, Barf T.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3823-7. doi: 10.1016/j.bmcl.2011.04.016. Epub 2011 Apr 16.

PMID:
21565498
7.

Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance.

Klüter S, Simard JR, Rode HB, Grütter C, Pawar V, Raaijmakers HC, Barf TA, Rabiller M, van Otterlo WA, Rauh D.

Chembiochem. 2010 Dec 10;11(18):2557-66. doi: 10.1002/cbic.201000352.

PMID:
21080395
8.

N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors.

Barf T, Lehmann F, Hammer K, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Rondahl L, Lundbäck T.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1745-8. doi: 10.1016/j.bmcl.2009.01.084. Epub 2009 Jan 30.

PMID:
19217286
9.

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

Hult M, Shafqat N, Elleby B, Mitschke D, Svensson S, Forsgren M, Barf T, Vallgårda J, Abrahmsen L, Oppermann U.

Mol Cell Endocrinol. 2006 Mar 27;248(1-2):26-33. Epub 2006 Jan 20.

PMID:
16431016
10.
11.

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

Ringom R, Axen E, Uppenberg J, Lundbäck T, Rondahl L, Barf T.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4449-52.

PMID:
15357970
12.

Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.

Lehmann F, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Lundbäck T, Rondahl L, Barf T.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4445-8.

PMID:
15357969
13.

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

Barf T, Vallgårda J, Emond R, Häggström C, Kurz G, Nygren A, Larwood V, Mosialou E, Axelsson K, Olsson R, Engblom L, Edling N, Rönquist-Nii Y, Ohman B, Alberts P, Abrahmsén L.

J Med Chem. 2002 Aug 29;45(18):3813-5.

PMID:
12190302
14.

Synthesis and biological activity of a novel class of small molecular weight peptidomimetic competitive inhibitors of protein tyrosine phosphatase 1B.

Larsen SD, Barf T, Liljebris C, May PD, Ogg D, O'Sullivan TJ, Palazuk BJ, Schostarez HJ, Stevens FC, Bleasdale JE.

J Med Chem. 2002 Jan 31;45(3):598-622.

PMID:
11806712
15.

5-(Sulfonyl)oxy-tryptamines and ethylamino side chain restricted derivatives. Structure-affinity relationships for h5-HT1B and h5-HT1D receptors.

Barf T, Wikström H, Pauwels PJ, Palmier C, Tardif S, Lundmark M, Sundell S.

Bioorg Med Chem. 1998 Sep;6(9):1469-79.

PMID:
9801818
16.

Autoradiographic localization of 5-HT1A receptors in the post-mortem human brain using [3H]WAY-100635 and [11C]way-100635.

Hall H, Lundkvist C, Halldin C, Farde L, Pike VW, McCarron JA, Fletcher A, Cliffe IA, Barf T, Wikström H, Sedvall G.

Brain Res. 1997 Jan 16;745(1-2):96-108.

PMID:
9037397
17.

5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.

Barf TA, de Boer P, Wikström H, Peroutka SJ, Swensson K, Ennis MD, Ghazal NB, McGuire JC, Smith MW.

J Med Chem. 1996 Nov 22;39(24):4717-26.

PMID:
8941384
18.

Investigations with GMC2021 in experimental models predictive of antimigraine activity and coronary side-effect potential.

Saxena PR, De Vries P, Heiligers JP, Maassen VanDenBrink A, Bax WA, Barf T, Wikström H.

Eur J Pharmacol. 1996 Sep 19;312(1):53-62.

PMID:
8891578
19.

Characterization of the radioactive metabolites of the 5-HT1A receptor radioligand, [O-methyl-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 S, Lundkvist C, Pike VW, Halldin C, McCarron JA, Swahn CG, Ginovart N, Luthra SK, Bench CJ, Grasby PM, Wikström H, Barf T, Cliffe IA, Fletcher A, Farde L.

Nucl Med Biol. 1996 Jul;23(5):627-34.

PMID:
8905828
20.

Potential anxiolytic properties of R-(+)-8-OSO2CF3-PAT, a 5-HT 1A receptor agonist.

Barf T, Korte SM, Korte-Bouws G, Sonesson C, Damsma G, Bohus B, Wikström H.

Eur J Pharmacol. 1996 Feb 22;297(3):205-11.

PMID:
8666051
21.

Synthesis and evaluation of pharmacological and pharmacokinetic properties of monopropyl analogs of 5-, 7-, and 8-[[(trifluoromethyl)sulfonyl]oxy]-2-aminotetralins: central dopamine and serotonin receptor activity.

Sonesson C, Barf T, Nilsson J, Dijkstra D, Carlsson A, Svensson K, Smith MW, Martin IJ, Duncan JN, King LJ, et al.

J Med Chem. 1995 Apr 14;38(8):1319-29.

PMID:
7731017

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