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14 results

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Page 1
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: eve pd. 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.
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I. Reader JC, et al. J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22111927 Free PMC 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: eve pd. 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.
Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.
Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD. Yap TA, et al. Among authors: eve pd. Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29. Mol Cancer Ther. 2011. PMID: 21191045 Free PMC article.
AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity.
Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD. Yap TA, et al. Among authors: eve pd. Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10. Clin Cancer Res. 2012. PMID: 22781553
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: eve pd. 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.
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: eve pd. Oncotarget. 2016 Jan 19;7(3):2329-42. doi: 10.18632/oncotarget.4919. Oncotarget. 2016. PMID: 26295308 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: eve pd. 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.
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V. Le Bihan YV, et al. Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17. Eur J Med Chem. 2019. PMID: 31158747 Free PMC article.
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
Davis OA, Cheung KJ, Brennan A, Lloyd MG, Rodrigues MJ, Pierrat OA, Collie GW, Le Bihan YV, Huckvale R, Harnden AC, Varela A, Bright MD, Eve P, Hayes A, Henley AT, Carter MD, McAndrew PC, Talbot R, Burke R, van Montfort RLM, Raynaud FI, Rossanese OW, Meniconi M, Bellenie BR, Hoelder S. Davis OA, et al. J Med Chem. 2022 Jun 23;65(12):8169-8190. doi: 10.1021/acs.jmedchem.1c02174. Epub 2022 Jun 3. J Med Chem. 2022. PMID: 35657291 Free PMC article.
14 results