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AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Narjes F, Llinas A, von Berg S, Jirholt J, Lever S, Pehrson R, Collins M, Malmberg A, Svanberg P, Xue Y, Olsson RI, Malmberg J, Hughes G, Hossain N, Grindebacke H, Leffler A, Krutrök N, Bäck E, Ramnegård M, Lepistö M, Thunberg L, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG. Narjes F, et al. Among authors: hughes g. J Med Chem. 2021 Sep 23;64(18):13807-13829. doi: 10.1021/acs.jmedchem.1c01197. Epub 2021 Aug 31. J Med Chem. 2021. PMID: 34464130
Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
Ripa L, Sandmark J, Hughes G, Shamovsky I, Gunnarsson A, Johansson J, Llinas A, Collins M, Jung B, Novén A, Pemberton N, Mogemark M, Xiong Y, Li Q, Tångefjord S, Ek M, Åstrand A. Ripa L, et al. Among authors: hughes g. J Med Chem. 2023 Oct 26;66(20):14188-14207. doi: 10.1021/acs.jmedchem.3c01269. Epub 2023 Oct 5. J Med Chem. 2023. PMID: 37797307
1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.
Dziadulewicz EK, Ritchie TJ, Hallett A, Snell CR, Ko SY, Wrigglesworth R, Hughes GA, Dunstan AR, Bloomfield GC, Drake GS, Brown MC, Lee W, Burgess GM, Davis C, Yaqoob M, Perkins MN, Campbell EA, Davis AJ, Rang HP. Dziadulewicz EK, et al. Among authors: hughes ga. J Med Chem. 2000 Mar 9;43(5):769-71. doi: 10.1021/jm991155o. J Med Chem. 2000. PMID: 10715143 No abstract available.
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, Budd E, Butler R, Cheung AK, Choudhury H, Collingwood SP, Cox B, Danahay H, Edwards L, Everatt B, Glaenzel U, Glotin AL, Groot-Kormelink P, Hall E, Hatto J, Howsham C, Hughes G, King A, Koehler J, Kulkarni S, Lightfoot M, Nicholls I, Page C, Pergl-Wilson G, Popa MO, Robinson R, Rowlands D, Sharp T, Spendiff M, Stanley E, Steward O, Taylor RJ, Tranter P, Wagner T, Watson H, Williams G, Wright P, Young A, Sandham DA. Grand DL, et al. Among authors: hughes g. J Med Chem. 2021 Jun 10;64(11):7241-7260. doi: 10.1021/acs.jmedchem.1c00343. Epub 2021 May 24. J Med Chem. 2021. PMID: 34028270
2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.
Walpole C, Ko SY, Brown M, Beattie D, Campbell E, Dickenson F, Ewan S, Hughes GA, Lemaire M, Lerpiniere J, Patel S, Urban L. Walpole C, et al. Among authors: hughes ga. J Med Chem. 1998 Aug 13;41(17):3159-73. doi: 10.1021/jm970499g. J Med Chem. 1998. PMID: 9703462
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
Culshaw AJ, Bevan S, Christiansen M, Copp P, Davis A, Davis C, Dyson A, Dziadulewicz EK, Edwards L, Eggelte H, Fox A, Gentry C, Groarke A, Hallett A, Hart TW, Hughes GA, Knights S, Kotsonis P, Lee W, Lyothier I, McBryde A, McIntyre P, Paloumbis G, Panesar M, Patel S, Seiler MP, Yaqoob M, Zimmermann K. Culshaw AJ, et al. Among authors: hughes ga. J Med Chem. 2006 Jan 26;49(2):471-4. doi: 10.1021/jm051058x. J Med Chem. 2006. PMID: 16420034
3,000 results