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165 results

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Page 1
Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.
Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, Cheung KJ, Drouin L, Innocenti P, Woodward H, Davis OA, Lloyd MG, Varela A, Huckvale R, Broccatelli F, Carter M, Galiwango D, Hayes A, Raynaud FI, Bryant C, Whittaker S, Rossanese OW, Hoelder S, Burke R, van Montfort RLM. Pierrat OA, et al. Among authors: raynaud fi. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.
Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity.
Stimson L, Rowlands MG, Newbatt YM, Smith NF, Raynaud FI, Rogers P, Bavetsias V, Gorsuch S, Jarman M, Bannister A, Kouzarides T, McDonald E, Workman P, Aherne GW. Stimson L, et al. Among authors: raynaud fi. Mol Cancer Ther. 2005 Oct;4(10):1521-32. doi: 10.1158/1535-7163.MCT-05-0135. Mol Cancer Ther. 2005. PMID: 16227401
In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.
Sharp SY, Boxall K, Rowlands M, Prodromou C, Roe SM, Maloney A, Powers M, Clarke PA, Box G, Sanderson S, Patterson L, Matthews TP, Cheung KM, Ball K, Hayes A, Raynaud F, Marais R, Pearl L, Eccles S, Aherne W, McDonald E, Workman P. Sharp SY, et al. Cancer Res. 2007 Mar 1;67(5):2206-16. doi: 10.1158/0008-5472.CAN-06-3473. Cancer Res. 2007. PMID: 17332351 Free article.
Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.
Caldwell JJ, Davies TG, Donald A, McHardy T, Rowlands MG, Aherne GW, Hunter LK, Taylor K, Ruddle R, Raynaud FI, Verdonk M, Workman P, Garrett MD, Collins I. Caldwell JJ, et al. Among authors: raynaud fi. J Med Chem. 2008 Apr 10;51(7):2147-57. doi: 10.1021/jm701437d. Epub 2008 Mar 18. J Med Chem. 2008. PMID: 18345609
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).
Niculescu-Duvaz D, Gaulon C, Dijkstra HP, Niculescu-Duvaz I, Zambon A, Ménard D, Suijkerbuijk BM, Nourry A, Davies L, Manne H, Friedlos F, Ogilvie L, Hedley D, Whittaker S, Kirk R, Gill A, Taylor RD, Raynaud FI, Moreno-Farre J, Marais R, Springer CJ. Niculescu-Duvaz D, et al. Among authors: raynaud fi. J Med Chem. 2009 Apr 23;52(8):2255-64. doi: 10.1021/jm801509w. J Med Chem. 2009. PMID: 19323560
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: raynaud fi. J Med Chem. 2010 Mar 11;53(5):2239-49. doi: 10.1021/jm901788j. J Med Chem. 2010. PMID: 20151677 Free PMC article.
Drugging the PI3 kinome: from chemical tools to drugs in the clinic.
Workman P, Clarke PA, Raynaud FI, van Montfort RL. Workman P, et al. Among authors: raynaud fi. Cancer Res. 2010 Mar 15;70(6):2146-57. doi: 10.1158/0008-5472.CAN-09-4355. Epub 2010 Feb 23. Cancer Res. 2010. PMID: 20179189 Free PMC article. Review.
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
Suijkerbuijk BM, Niculescu-Duvaz I, Gaulon C, Dijkstra HP, Niculescu-Duvaz D, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie LM, Hedley D, Lopes F, Preece NP, Moreno-Farre J, Raynaud FI, Kirk R, Whittaker S, Marais R, Springer CJ. Suijkerbuijk BM, et al. Among authors: raynaud fi. J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f. J Med Chem. 2010. PMID: 20199087
165 results