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Items: 11


Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Zak M, Hanan EJ, Lupardus P, Brown DG, Robinson C, Siu M, Lyssikatos JP, Romero FA, Zhao G, Kellar T, Mendonca R, Ray NC, Goodacre SC, Crackett PH, McLean N, Hurley CA, Yuen PW, Cheng YX, Liu X, Liimatta M, Kohli PB, Nonomiya J, Salmon G, Buckley G, Lloyd J, Gibbons P, Ghilardi N, Kenny JR, Johnson A.

Bioorg Med Chem Lett. 2019 Jun 15;29(12):1522-1531. doi: 10.1016/j.bmcl.2019.04.008. Epub 2019 Apr 4.


Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.

Dengler HS, Wu X, Peng I, Rinderknecht CH, Kwon Y, Suto E, Kohli PB, Liimatta M, Barrett K, Lloyd J, Cain G, Briggs M, Addo S, Salmon G, Ubhayakar S, Deshmukh G, Shahidi-Latham SK, Quiason-Huynh CM, Jackman J, Liu J, Ray NC, Goodacre SC, Johnson A, McKenzie BS, Lee WP, Zak M, Kenny JR, Ghilardi N.

Sci Transl Med. 2018 Nov 21;10(468). pii: eaao2151. doi: 10.1126/scitranslmed.aao2151.


Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

Blackaby WP, Lewis RT, Thomson JL, Jennings AS, Goodacre SC, Street LJ, MacLeod AM, Pike A, Wood S, Thomas S, Brown TA, Smith A, Pillai G, Almond S, Guscott MR, Burns HD, Eng W, Ryan C, Cook J, Hamill TG.

ACS Med Chem Lett. 2010 Jun 25;1(7):350-4. doi: 10.1021/ml1001085. eCollection 2010 Oct 14.


Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.

Thomson JL, Blackaby WP, Jennings AS, Goodacre SC, Pike A, Thomas S, Brown TA, Smith A, Pillai G, Street LJ, Lewis RT.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2235-9. doi: 10.1016/j.bmcl.2009.02.102. Epub 2009 Feb 28.


Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands.

Fradley RL, Guscott MR, Bull S, Hallett DJ, Goodacre SC, Wafford KA, Garrett EM, Newman RJ, O'Meara GF, Whiting PJ, Rosahl TW, Dawson GR, Reynolds DS, Atack JR.

J Psychopharmacol. 2007 Jun;21(4):384-91. Epub 2006 Nov 8.


The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone.

Atack JR, Pike A, Marshall G, Stanley J, Lincoln R, Cook SM, Lewis RT, Blackaby WP, Goodacre SC, McKernan RM, Dawson GR, Wafford KA, Reynolds DS.

Neuropharmacology. 2006 May;50(6):677-89. Epub 2006 Jan 20.


Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.

Blackaby WP, Atack JR, Bromidge F, Castro JL, Goodacre SC, Hallett DJ, Lewis RT, Marshall GR, Pike A, Smith AJ, Street LJ, Tattersall DF, Wafford KA.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1175-9. Epub 2006 Jan 6.


Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.

Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR.

J Med Chem. 2006 Jan 12;49(1):35-8.


Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Goodacre SC, Hallett DJ, Carling RW, Castro JL, Reynolds DS, Pike A, Wafford KA, Newman R, Atack JR, Street LJ.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1582-5. Epub 2005 Dec 27.


Neighboring group participation of the indole nucleus: An unusual DAST-mediated rearrangement reaction

Hallett DJ, Gerhard U, Goodacre SC, Hitzel L, Sparey TJ, Thomas S, Rowley M, Ball RG.

J Org Chem. 2000 Aug 11;65(16):4984-93.


Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.

van Niel MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, Sohal B, Stanton JA, Thomas S, Verrier H, Watt AP, Castro JL.

J Med Chem. 1999 Jun 17;42(12):2087-104.


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