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Page 1
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
Walton MI, Eve PD, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Boxall KJ, Tall M, Swales K, Matthews TP, McHardy T, Lainchbury M, Osborne J, Hunter JE, Perkins ND, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Collins I, Garrett MD. Walton MI, et al. Among authors: aherne gw. Oncotarget. 2016 Jan 19;7(3):2329-42. doi: 10.18632/oncotarget.4919. Oncotarget. 2016. PMID: 26295308 Free PMC article.
CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs.
Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD. Walton MI, et al. Among authors: aherne gw. Clin Cancer Res. 2012 Oct 15;18(20):5650-61. doi: 10.1158/1078-0432.CCR-12-1322. Epub 2012 Aug 28. Clin Cancer Res. 2012. PMID: 22929806 Free PMC article.
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, Hayes A, Valenti MR, de Haven Brandon AK, Box G, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Garrett MD, Collins I. Lainchbury M, et al. Among authors: aherne gw. J Med Chem. 2012 Nov 26;55(22):10229-40. doi: 10.1021/jm3012933. Epub 2012 Oct 19. J Med Chem. 2012. PMID: 23082860 Free PMC article.
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KM, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Jamin Y, Robinson SP, Westwood IM, van Montfort RL, Leonard PM, Lamers MB, Reader JC, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I. Osborne JD, et al. Among authors: aherne gw. J Med Chem. 2016 Jun 9;59(11):5221-37. doi: 10.1021/acs.jmedchem.5b01938. Epub 2016 May 23. J Med Chem. 2016. PMID: 27167172 Free article.
The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106.
Walton MI, Eve PD, Hayes A, Valenti M, De Haven Brandon A, Box G, Boxall KJ, Aherne GW, Eccles SA, Raynaud FI, Williams DH, Reader JC, Collins I, Garrett MD. Walton MI, et al. Among authors: aherne gw. Mol Cancer Ther. 2010 Jan;9(1):89-100. doi: 10.1158/1535-7163.MCT-09-0938. Epub 2010 Jan 6. Mol Cancer Ther. 2010. PMID: 20053762 Free article.
Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.
Silva-Santisteban MC, Westwood IM, Boxall K, Brown N, Peacock S, McAndrew C, Barrie E, Richards M, Mirza A, Oliver AW, Burke R, Hoelder S, Jones K, Aherne GW, Blagg J, Collins I, Garrett MD, van Montfort RL. Silva-Santisteban MC, et al. Among authors: aherne gw. PLoS One. 2013 Jun 12;8(6):e65689. doi: 10.1371/journal.pone.0065689. Print 2013. PLoS One. 2013. PMID: 23776527 Free PMC article.
The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.
Couty S, Westwood IM, Kalusa A, Cano C, Travers J, Boxall K, Chow CL, Burns S, Schmitt J, Pickard L, Barillari C, McAndrew PC, Clarke PA, Linardopoulos S, Griffin RJ, Aherne GW, Raynaud FI, Workman P, Jones K, van Montfort RL. Couty S, et al. Among authors: aherne gw. Oncotarget. 2013 Oct;4(10):1647-61. doi: 10.18632/oncotarget.1255. Oncotarget. 2013. PMID: 24072592 Free PMC article.
Identification of inhibitors of checkpoint kinase 1 through template screening.
Matthews TP, Klair S, Burns S, Boxall K, Cherry M, Fisher M, Westwood IM, Walton MI, McHardy T, Cheung KM, Van Montfort R, Williams D, Aherne GW, Garrett MD, Reader J, Collins I. Matthews TP, et al. Among authors: aherne gw. J Med Chem. 2009 Aug 13;52(15):4810-9. doi: 10.1021/jm900314j. J Med Chem. 2009. PMID: 19572549
Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).
McHardy T, Caldwell JJ, Cheung KM, Hunter LJ, Taylor K, Rowlands M, Ruddle R, Henley A, de Haven Brandon A, Valenti M, Davies TG, Fazal L, Seavers L, Raynaud FI, Eccles SA, Aherne GW, Garrett MD, Collins I. McHardy T, et al. Among authors: aherne gw. J Med Chem. 2010 Mar 11;53(5):2239-49. doi: 10.1021/jm901788j. J Med Chem. 2010. PMID: 20151677 Free PMC article.
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
Matthews TP, McHardy T, Klair S, Boxall K, Fisher M, Cherry M, Allen CE, Addison GJ, Ellard J, Aherne GW, Westwood IM, van Montfort R, Garrett MD, Reader JC, Collins I. Matthews TP, et al. Among authors: aherne gw. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4045-9. doi: 10.1016/j.bmcl.2010.05.096. Epub 2010 May 27. Bioorg Med Chem Lett. 2010. PMID: 20561787
136 results