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Developing predictive assays: the phenotypic screening "rule of 3".
Vincent F, Loria P, Pregel M, Stanton R, Kitching L, Nocka K, Doyonnas R, Steppan C, Gilbert A, Schroeter T, Peakman MC. Vincent F, et al. Sci Transl Med. 2015 Jun 24;7(293):293ps15. doi: 10.1126/scitranslmed.aab1201. Sci Transl Med. 2015. PMID: 26109101 Review.
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: vincent f. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Human amyotrophic lateral sclerosis excitability phenotype screen: Target discovery and validation.
Huang X, Roet KCD, Zhang L, Brault A, Berg AP, Jefferson AB, Klug-McLeod J, Leach KL, Vincent F, Yang H, Coyle AJ, Jones LH, Frost D, Wiskow O, Chen K, Maeda R, Grantham A, Dornon MK, Klim JR, Siekmann MT, Zhao D, Lee S, Eggan K, Woolf CJ. Huang X, et al. Among authors: vincent f. Cell Rep. 2021 Jun 8;35(10):109224. doi: 10.1016/j.celrep.2021.109224. Cell Rep. 2021. PMID: 34107252 Free PMC article.
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization.
Thorarensen A, Balbo P, Banker ME, Czerwinski RM, Kuhn M, Maurer TS, Telliez JB, Vincent F, Wittwer AJ. Thorarensen A, et al. Among authors: vincent f. Bioorg Med Chem. 2021 Jan 1;29:115865. doi: 10.1016/j.bmc.2020.115865. Epub 2020 Nov 18. Bioorg Med Chem. 2021. PMID: 33285410
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
Hall J, Brault A, Vincent F, Weng S, Wang H, Dumlao D, Aulabaugh A, Aivazian D, Castro D, Chen M, Culp J, Dower K, Gardner J, Hawrylik S, Golenbock D, Hepworth D, Horn M, Jones L, Jones P, Latz E, Li J, Lin LL, Lin W, Lin D, Lovering F, Niljanskul N, Nistler R, Pierce B, Plotnikova O, Schmitt D, Shanker S, Smith J, Snyder W, Subashi T, Trujillo J, Tyminski E, Wang G, Wong J, Lefker B, Dakin L, Leach K. Hall J, et al. Among authors: vincent f. PLoS One. 2017 Sep 21;12(9):e0184843. doi: 10.1371/journal.pone.0184843. eCollection 2017. PLoS One. 2017. PMID: 28934246 Free PMC article.
662 results