| Year |
Citation |
Score |
| 2024 |
Balıkçı E, Marques AMC, Bauer LG, Seupel R, Bennett J, Raux B, Buchan K, Simelis K, Singh U, Rogers C, Ward J, Cheng C, Szommer T, Schützenhofer K, Elkins JM, ... ... Brennan PE, et al. Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist. Journal of Medicinal Chemistry. PMID 38635563 DOI: 10.1021/acs.jmedchem.4c00072 |
0.667 |
|
| 2023 |
O'Brien DP, Jones HB, Guenther F, Murphy EJ, England KS, Vendrell I, Anderson M, Brennan P, Davis JB, Pinto-Fernández A, Turnbull AP, Kessler BM. Structural Premise of Selective Deubiquitinase USP30 Inhibition by Small-Molecule Benzosulfonamides. Molecular & Cellular Proteomics : McP. 100609. PMID 37385347 DOI: 10.1016/j.mcpro.2023.100609 |
0.312 |
|
| 2023 |
Fowkes MM, Troeberg L, Brennan PE, Vincent TL, Meldal M, Lim NH. Development of Selective ADAMTS-5 Peptide Substrates to Monitor Proteinase Activity. Journal of Medicinal Chemistry. 66: 3522-3539. PMID 36891740 DOI: 10.1021/acs.jmedchem.2c02090 |
0.738 |
|
| 2022 |
Frank N, Nugent J, Shire BR, Pickford HD, Rabe P, Sterling AJ, Zarganes-Tzitzikas T, Grimes T, Thompson AL, Smith RC, Schofield CJ, Brennan PE, Duarte F, Anderson EA. Synthesis of meta-substituted arene bioisosteres from [3.1.1]propellane. Nature. PMID 36108675 DOI: 10.1038/s41586-022-05290-z |
0.513 |
|
| 2022 |
Fowkes MM, Das Neves Borges P, Cacho-Nerin F, Brennan PE, Vincent TL, Lim NH. Imaging articular cartilage in osteoarthritis using targeted peptide radiocontrast agents. Plos One. 17: e0268223. PMID 35536857 DOI: 10.1371/journal.pone.0268223 |
0.738 |
|
| 2020 |
De Cesco S, Davis JB, Brennan PE. TargetDB: A target information aggregation tool and tractability predictor. Plos One. 15: e0232644. PMID 32877430 DOI: 10.1371/Journal.Pone.0232644 |
0.344 |
|
| 2020 |
Cottone L, Cribbs AP, Khandelwal G, Wells G, Ligammari L, Philpott M, Tumber A, Lombard P, Hookway ES, Szommer T, Johansson C, Brennan PE, Pillay N, Jenner RG, Oppermann U, et al. Inhibition of histone H3K27 demethylases inactivates brachyury (TBXT) and promotes chordoma cell death. Cancer Research. PMID 32855205 DOI: 10.1158/0008-5472.Can-20-1387 |
0.348 |
|
| 2020 |
Kahn Tareque R, Hassell-Hart S, Krojer T, Bradley A, Velupillai S, Talon R, Fairhead M, Day IJ, Bala K, Felix R, Kemmitt P, Brennan P, von Delft F, Díaz Sáez L, Spencer J, et al. Deliberately Losing Control of C-H Activation Processes in the Design of Small Molecule Fragment Arrays Targeting Peroxisomal Metabolism. Chemmedchem. PMID 32812371 DOI: 10.1002/Cmdc.202000543 |
0.319 |
|
| 2019 |
Ni X, Heidenreich D, Christott T, Bennett J, Moustakim M, Brennan PE, Fedorov O, Knapp S, Chaikuad A. Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1. Acs Medicinal Chemistry Letters. 10: 1661-1666. PMID 31857843 DOI: 10.1021/Acsmedchemlett.9B00460 |
0.794 |
|
| 2019 |
Fagan V, Johansson C, Gileadi C, Monteiro O, Dunford JE, Nibhani R, Philpott M, Malzahn J, Wells G, Farham R, Cribbs A, Halidi N, Li F, Chau I, Greschik H, ... ... Brennan PE, et al. A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function. Journal of Medicinal Chemistry. PMID 31550156 DOI: 10.1021/Acs.Jmedchem.9B00562 |
0.368 |
|
| 2019 |
Xiong Y, Greschik H, Johansson C, Seifert L, Bacher J, Park KS, Babault N, Martini ML, Fagan V, Li F, Chau I, Christott T, Dilworth D, Barsyte-Lovejoy D, Vedadi M, ... ... Brennan PE, et al. Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). Journal of Medicinal Chemistry. PMID 31260300 DOI: 10.1021/Acs.Jmedchem.9B00522 |
0.356 |
|
| 2019 |
Fang H, De Wolf H, Knezevic B, Burnham KL, Osgood J, Sanniti A, Lledó Lara A, Kasela S, De Cesco S, Wegner JK, Handunnetthi L, McCann FE, Chen L, Sekine T, ... Brennan PE, et al. A genetics-led approach defines the drug target landscape of 30 immune-related traits. Nature Genetics. PMID 31253980 DOI: 10.1038/S41588-019-0456-1 |
0.309 |
|
| 2019 |
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, ... ... Brennan PE, et al. 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. European Journal of Medicinal Chemistry. 177: 316-337. PMID 31158747 DOI: 10.1016/J.Ejmech.2019.05.041 |
0.745 |
|
| 2019 |
Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, ... ... Brennan PE, et al. Rapid covalent-probe discovery by electrophile-fragment screening. Journal of the American Chemical Society. PMID 31060360 DOI: 10.1021/Jacs.9B02822 |
0.379 |
|
| 2019 |
Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, et al. A chemical toolbox for the study of bromodomains and epigenetic signaling. Nature Communications. 10: 1915. PMID 31015424 DOI: 10.1038/S41467-019-09672-2 |
0.408 |
|
| 2019 |
Huang LY, Li H, Li LL, Niu L, Seupel R, Wu C, Cheng W, Chen C, Ding B, Brennan PE, Yang S. Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell Active Inhibitors of P300/CBP-Associated Factor Bromodomain. Journal of Medicinal Chemistry. PMID 30998845 DOI: 10.1021/Acs.Jmedchem.9B00096 |
0.384 |
|
| 2019 |
Gray JL, von Delft F, Brennan P. Targeting the Small GTPase Superfamily through their Regulatory Proteins. Angewandte Chemie (International Ed. in English). PMID 30869179 DOI: 10.1002/Anie.201900585 |
0.374 |
|
| 2019 |
Hassell-Hart S, Runcie A, Krojer T, Doyle J, Lineham E, Ocasio CA, Neto BAD, Fedorov O, Marsh G, Maple H, Felix R, Banks R, Ciulli A, Picaud S, Filippakopoulos P, ... ... Brennan P, et al. Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor Organometallics. 39: 408-416. DOI: 10.1021/Acs.Organomet.9B00750 |
0.407 |
|
| 2018 |
D'Ascenzio M, Pugh KM, Konietzny R, Berridge G, Tallant C, Hashem S, Monteiro O, Thomas JR, Schirle M, Knapp S, Marsden B, Fedorov O, Bountra C, Kessler BM, Brennan PE. An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains. Angewandte Chemie (International Ed. in English). PMID 30589164 DOI: 10.1002/Anie.201807825 |
0.43 |
|
| 2018 |
Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs A, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, ... ... Brennan P, et al. Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. Angewandte Chemie (International Ed. in English). PMID 30431220 DOI: 10.1002/Anie.201810179 |
0.796 |
|
| 2018 |
Heidenreich D, Moustakim M, Schmidt J, Merk D, Brennan PE, Fedorov O, Chaikuad A, Knapp S. A structure-based approach towards identification of inhibitory fragments for eleven-nineteen-leukemia protein (ENL). Journal of Medicinal Chemistry. PMID 30407816 DOI: 10.1021/Acs.Jmedchem.8B01457 |
0.797 |
|
| 2018 |
Moustakim M, Felce SL, Zaarour N, Farnie G, McCann FE, Brennan PE. Target Identification Using Chemical Probes. Methods in Enzymology. 610: 27-58. PMID 30390803 DOI: 10.1016/Bs.Mie.2018.09.013 |
0.787 |
|
| 2018 |
Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Saez LD, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, ... ... Brennan P, et al. Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Angewandte Chemie (International Ed. in English). PMID 30288907 DOI: 10.1002/Anie.201810617 |
0.802 |
|
| 2018 |
Wright M, Martinez-Lamenca C, Leenaerts JE, Brennan PE, Trabanco AA, Oehlrich D. A Bench-Stable Transfer Reagent for the Synthesis of Trifluoromethyl-sulfonimidamides from Sulfinamides. The Journal of Organic Chemistry. PMID 29932332 DOI: 10.1021/Acs.Joc.8B01244 |
0.754 |
|
| 2018 |
Heroven C, Georgi V, Ganotra GK, Brennan PE, Wolfreys F, Wade RC, Fernández-Montalván AE, Chaikuad A, Knapp S. Halogen-aromatic π-interactions modulate inhibitor residence time. Angewandte Chemie (International Ed. in English). PMID 29601130 DOI: 10.1002/Anie.201801666 |
0.359 |
|
| 2018 |
Brennan P, Bowkett D, Talon R, Tallant C, Schofield C, Bruton G, von Delft F, Knapp S. Identifying small molecule binding sites for epigenetic proteins at domain-domain interfaces. Chemmedchem. PMID 29578648 DOI: 10.1002/Cmdc.201800030 |
0.73 |
|
| 2018 |
Moustakim M, Riedel K, Schuller M, Gehring AP, Monteiro OP, Martin SP, Fedorov O, Heer J, Dixon DJ, Elkins JM, Knapp S, Bracher F, Brennan PE. Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Bioorganic & Medicinal Chemistry. PMID 29567296 DOI: 10.1016/J.Bmc.2018.03.020 |
0.781 |
|
| 2018 |
Kiely-Collins HJ, Sechi I, Brennan PE, McLaughlin MG. Mild, calcium catalysed Beckmann rearrangements. Chemical Communications (Cambridge, England). 54: 654-657. PMID 29300400 DOI: 10.1039/C7Cc09491D |
0.572 |
|
| 2018 |
Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Díaz-Sáez L, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, ... ... Brennan PE, et al. Entdeckung einer chemischen Sonde für MLLT1/3-YEATS-Domänen Angewandte Chemie. 130: 16540-16545. DOI: 10.1002/Ange.201810617 |
0.735 |
|
| 2017 |
Bradley AR, Echalier A, Fairhead M, Strain-Damerell C, Brennan P, Bullock AN, Burgess-Brown NA, Carpenter EP, Gileadi O, Marsden BD, Lee WH, Yue W, Bountra C, von Delft F. The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery. Essays in Biochemistry. 61: 495-503. PMID 29118096 DOI: 10.1042/Ebc20170051 |
0.352 |
|
| 2017 |
Gerken P, Wolstenhulme J, Tumber A, Hatch S, Zhang Y, Müller S, Chandler S, Mair B, Li F, Nijman S, Konietzny R, Szommer T, Yapp C, Fedorov O, Benesch J, ... ... Brennan P, et al. Discovery of a highly selective cell-active inhibitor of KDM2/7. Angewandte Chemie (International Ed. in English). PMID 28976073 DOI: 10.1002/Anie.201706788 |
0.55 |
|
| 2017 |
Meier JC, Tallant C, Fedorov O, Witwicka H, Hwang SY, van Stiphout RG, Lambert JP, Rogers C, Yapp C, Gerstenberger BS, Fedele V, Savitsky P, Heidenreich D, Daniels DL, Owen DR, ... ... Brennan PE, et al. Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation. Acs Chemical Biology. PMID 28849908 DOI: 10.1021/Acschembio.7B00481 |
0.36 |
|
| 2017 |
Roberts TC, Etxaniz U, Dall'Agnese A, Wu SY, Chiang CM, Brennan PE, Wood MJA, Puri PL. BRD3 and BRD4 BET Bromodomain Proteins Differentially Regulate Skeletal Myogenesis. Scientific Reports. 7: 6153. PMID 28733670 DOI: 10.1038/S41598-017-06483-7 |
0.36 |
|
| 2017 |
Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, et al. Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins. Journal of Medicinal Chemistry. PMID 28714688 DOI: 10.1021/Acs.Jmedchem.7B00611 |
0.408 |
|
| 2017 |
Kawamura A, Münzel M, Kojima T, Yapp C, Bhushan B, Goto Y, Tumber A, Katoh T, King ON, Passioura T, Walport LJ, Hatch SB, Madden S, Müller S, Brennan PE, et al. Highly selective inhibition of histone demethylases by de novo macrocyclic peptides. Nature Communications. 8: 14773. PMID 28382930 DOI: 10.1038/Ncomms14773 |
0.418 |
|
| 2017 |
Denny RA, Flick AC, Coe JW, Langille J, Basak A, Liu S, Stock IA, Sahasrabudhe P, Bonin PD, Hay DA, Brennan PE, Pletcher MT, Jones LH, Chekler EL. Structure-based design of highly selective inhibitors of the CREB binding protein bromodomain. Journal of Medicinal Chemistry. PMID 28375629 DOI: 10.1021/Acs.Jmedchem.6B01839 |
0.418 |
|
| 2017 |
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, ... ... Brennan PE, et al. Assessing histone demethylase inhibitors in cells: lessons learned. Epigenetics & Chromatin. 10: 9. PMID 28265301 DOI: 10.1186/S13072-017-0116-6 |
0.641 |
|
| 2017 |
Tumber A, Nuzzi A, Hookway ES, Hatch SB, Velupillai S, Johansson C, Kawamura A, Savitsky P, Yapp C, Szykowska A, Wu N, Bountra C, Strain-Damerell C, Burgess-Brown NA, Ruda GF, ... ... Brennan PE, et al. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chemical Biology. PMID 28262558 DOI: 10.1016/J.Chembiol.2017.02.006 |
0.368 |
|
| 2017 |
Igoe N, Bayle ED, Fedorov O, Tallant C, Savitsky P, Rogers C, Owen DR, Deb G, Somervaille TC, Andrews DM, Jones N, Cheasty A, Ryder H, Brennan PE, Müller S, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. Journal of Medicinal Chemistry. PMID 28068087 DOI: 10.1021/Acs.Jmedchem.6B01583 |
0.378 |
|
| 2016 |
Cox OB, Krojer T, Collins P, Monteiro O, Talon R, Bradley A, Fedorov O, Amin J, Marsden BD, Spencer J, von Delft F, Brennan PE. A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain. Chemical Science. 7: 2322-2330. PMID 29910922 DOI: 10.1039/C5Sc03115J |
0.704 |
|
| 2016 |
Moustakim M, Clark PGK, Hay DA, Dixon DJ, Brennan PE. Chemical probes and inhibitors of bromodomains outside the BET family. Medchemcomm. 7: 2246-2264. PMID 29170712 DOI: 10.1039/C6Md00373G |
0.798 |
|
| 2016 |
Moustakim M, Clark PG, Trulli L, Fuentes de Arriba AL, Ehebauer MT, Chaikuad A, Murphy EJ, Mendez-Johnson J, Daniels D, Hou CD, Lin YH, Walker JR, Hui R, Yang H, Dorrell L, ... ... Brennan PE, et al. Discovery of a PCAF Bromodomain Chemical Probe. Angewandte Chemie (International Ed. in English). PMID 27966810 DOI: 10.1002/Anie.201610816 |
0.771 |
|
| 2016 |
Clark PG, Dixon DJ, Brennan PE. Development of chemical probes for the bromodomains of BRD7 and BRD9. Drug Discovery Today. Technologies. 19: 73-80. PMID 27769361 DOI: 10.1016/J.Ddtec.2016.05.002 |
0.572 |
|
| 2016 |
Picaud S, Leonards K, Lambert JP, Dovey O, Wells C, Fedorov O, Monteiro O, Fujisawa T, Wang CY, Lingard H, Tallant C, Nikbin N, Guetzoyan L, Ingham R, Ley SV, ... Brennan P, et al. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. Science Advances. 2: e1600760. PMID 27757418 DOI: 10.1126/Sciadv.1600760 |
0.519 |
|
| 2016 |
Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. Journal of Medicinal Chemistry. PMID 27673482 DOI: 10.1021/Acs.Jmedchem.6B00774 |
0.424 |
|
| 2016 |
Nowak RP, Tumber A, Johansson C, Che KH, Brennan P, Owen D, Oppermann U. Advances and challenges in understanding histone demethylase biology. Current Opinion in Chemical Biology. 33: 151-159. PMID 27371875 DOI: 10.1016/J.Cbpa.2016.06.021 |
0.343 |
|
| 2016 |
Vukovic S, Brennan PE, Huggins DJ. Exploring the role of water in molecular recognition: predicting protein ligandability using a combinatorial search of surface hydration sites. Journal of Physics. Condensed Matter : An Institute of Physics Journal. 28: 344007. PMID 27367338 DOI: 10.1088/0953-8984/28/34/344007 |
0.337 |
|
| 2016 |
Montenegro RC, Clark PG, Howarth A, Wan X, Ceroni A, Siejka P, Nunez-Alonso GA, Monteiro O, Rogers C, Gamble V, Burbano R, Brennan PE, Tallant C, Ebner D, Fedorov O, et al. BET inhibition as a new strategy for the treatment of gastric cancer. Oncotarget. PMID 27259267 DOI: 10.18632/Oncotarget.9766 |
0.522 |
|
| 2016 |
Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway ES, Nowak RP, Strain-Damerell C, Gileadi C, Philpott M, Burgess-Brown N, Wu N, Kopec J, Nuzzi A, Steuber H, Egner U, ... ... Brennan PE, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nature Chemical Biology. PMID 27214403 DOI: 10.1038/Nchembio.2087 |
0.409 |
|
| 2016 |
Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV. Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the Switch/Sucrose Non-Fermenting complex. Journal of Medicinal Chemistry. PMID 27119626 DOI: 10.1021/Acs.Jmedchem.5B01997 |
0.502 |
|
| 2016 |
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers CM, Parikh MD, Taylor A, Samas BM, O'Mahony A, Berg EL, et al. Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. Journal of Medicinal Chemistry. PMID 27115555 DOI: 10.1021/Acs.Jmedchem.6B00012 |
0.401 |
|
| 2016 |
Mathea S, Abdul Azeez KR, Salah E, Tallant C, Wolfreys F, Konietzny R, Fischer R, Lou HJ, Brennan PE, Schnapp G, Pautsch A, Kessler BM, Turk BE, Knapp S. Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib. Acs Chemical Biology. PMID 26999302 DOI: 10.1021/Acschembio.6B00043 |
0.383 |
|
| 2016 |
Brennan PE. Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma Cell Death and Disease. 7. PMID 26821065 DOI: 10.1038/Cddis.2015.384 |
0.37 |
|
| 2016 |
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, ... ... Brennan PE, et al. 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26741168 DOI: 10.1021/Acs.Jmedchem.5B01635 |
0.734 |
|
| 2016 |
Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Müller S, Siegal G, Knapp S. Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain. Journal of Medicinal Chemistry. PMID 26731131 DOI: 10.1021/Acs.Jmedchem.5B01719 |
0.395 |
|
| 2015 |
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angewandte Chemie (Weinheim An Der Bergstrasse, Germany). 127: 6315-6319. PMID 27346896 DOI: 10.1002/ange.201501394 |
0.541 |
|
| 2015 |
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. Recent Progress in Histone Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26710088 DOI: 10.1021/Acs.Jmedchem.5B01758 |
0.389 |
|
| 2015 |
Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, ... ... Brennan PE, et al. Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance. Science Advances. 1: e1500723. PMID 26702435 DOI: 10.1126/Sciadv.1500723 |
0.353 |
|
| 2015 |
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Hing Che K, ... ... Brennan P, et al. Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy. Cancer Research. PMID 26552700 DOI: 10.1158/0008-5472.Can-15-0236 |
0.386 |
|
| 2015 |
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, et al. Corrigendum: The promise and peril of chemical probes. Nature Chemical Biology. 11: 887. PMID 26485080 DOI: 10.1038/Nchembio1115-887C |
0.566 |
|
| 2015 |
Thinnes CC, Tumber A, Yapp C, Scozzafava G, Yeh T, Chan MC, Tran TA, Hsu K, Tarhonskaya H, Walport LJ, Wilkins SE, Martinez ED, Müller S, Pugh CW, Ratcliffe PJ, ... Brennan PE, et al. Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases. Chemical Communications (Cambridge, England). 51: 15458-61. PMID 26345662 DOI: 10.1039/C5Cc06095H |
0.407 |
|
| 2015 |
Canning P, Ruan Q, Schwerd T, Hrdinka M, Maki JL, Saleh D, Suebsuwong C, Ray S, Brennan PE, Cuny GD, Uhlig HH, Gyrd-Hansen M, Degterev A, Bullock AN. Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors. Chemistry & Biology. 22: 1174-84. PMID 26320862 DOI: 10.1016/J.Chembiol.2015.07.017 |
0.351 |
|
| 2015 |
Hammitzsch A, Tallant C, Fedorov O, O'Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proceedings of the National Academy of Sciences of the United States of America. 112: 10768-73. PMID 26261308 DOI: 10.1073/Pnas.1501956112 |
0.329 |
|
| 2015 |
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, et al. The promise and peril of chemical probes. Nature Chemical Biology. 11: 536-41. PMID 26196764 DOI: 10.1038/Nchembio.1867 |
0.542 |
|
| 2015 |
Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. Journal of Medicinal Chemistry. PMID 25974391 DOI: 10.1021/Acs.Jmedchem.5B00458 |
0.43 |
|
| 2015 |
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angewandte Chemie (International Ed. in English). 54: 6217-21. PMID 25864491 DOI: 10.1002/Anie.201501394 |
0.59 |
|
| 2015 |
Hay DA, Rogers CM, Fedorov O, Tallant C, Martin S, Monteiro OP, Müller S, Knapp S, Schofield CJ, Brennan PE. Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains Medchemcomm. 6: 1381-1386. DOI: 10.1039/C5Md00152H |
0.405 |
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| 2014 |
England KS, Tumber A, Krojer T, Scozzafava G, Ng SS, Daniel M, Szykowska A, Che K, von Delft F, Burgess-Brown NA, Kawamura A, Schofield CJ, Brennan PE. Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. Medchemcomm. 5: 1879-1886. PMID 26682034 DOI: 10.1039/C4Md00291A |
0.409 |
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| 2014 |
Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, ... ... Brennan PE, et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. Journal of the American Chemical Society. 136: 9308-19. PMID 24946055 DOI: 10.1021/Ja412434F |
0.402 |
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| 2014 |
Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, et al. Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HTâ‚‚C) receptor agonists with exquisite functional selectivity over 5-HTâ‚‚A and 5-HTâ‚‚B receptors. Journal of Medicinal Chemistry. 57: 5258-69. PMID 24878222 DOI: 10.1021/Jm5003292 |
0.327 |
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| 2014 |
Rooney TP, Filippakopoulos P, Fedorov O, Picaud S, Cortopassi WA, Hay DA, Martin S, Tumber A, Rogers CM, Philpott M, Wang M, Thompson AL, Heightman TD, Pryde DC, Cook A, ... ... Brennan PE, et al. A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction. Angewandte Chemie (International Ed. in English). 53: 6126-30. PMID 24821300 DOI: 10.1002/Anie.201402750 |
0.349 |
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| 2014 |
Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I, Marsden BD, Filippakopoulos P, Müller S, Knapp S, Brennan PE. [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. Journal of Medicinal Chemistry. 57: 462-76. PMID 24313754 DOI: 10.1021/Jm401568S |
0.408 |
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| 2014 |
Yue WW, Froese DS, Brennan PE. The role of protein structural analysis in the next generation sequencing era. Topics in Current Chemistry. 336: 67-98. PMID 22610134 DOI: 10.1007/128_2012_326 |
0.323 |
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| 2014 |
Guetzoyan L, Ingham RJ, Nikbin N, Rossignol J, Wolling M, Baumert M, Burgess-Brown NA, Strain-Damerell CM, Shrestha L, Brennan PE, Fedorov O, Knapp S, Ley SV. Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography Medchemcomm. 5: 540-546. DOI: 10.1039/C4Md00007B |
0.477 |
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| 2013 |
Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JB, King ON, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, ... ... Brennan PE, et al. 5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation. Chemical Science (Royal Society of Chemistry : 2010). 4: 3110-3117. PMID 26682036 DOI: 10.1039/C3Sc51122G |
0.347 |
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| 2013 |
Hay D, Fedorov O, Filippakopoulos P, Martin S, Philpott M, Picaud S, Hewings DS, Uttakar S, Heightman TD, Conway SJ, Knapp S, Brennan PE. The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains. Medchemcomm. 4: 140-144. PMID 26682033 DOI: 10.1039/C2Md20189E |
0.374 |
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| 2013 |
Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proceedings of the National Academy of Sciences of the United States of America. 110: 19754-9. PMID 24248379 DOI: 10.1073/Pnas.1310658110 |
0.397 |
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| 2013 |
Morley AD, Pugliese A, Birchall K, Bower J, Brennan P, Brown N, Chapman T, Drysdale M, Gilbert IH, Hoelder S, Jordan A, Ley SV, Merritt A, Miller D, Swarbrick ME, et al. Fragment-based hit identification: thinking in 3D. Drug Discovery Today. 18: 1221-7. PMID 23906694 DOI: 10.1016/J.Drudis.2013.07.011 |
0.398 |
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| 2013 |
Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, et al. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Research. 73: 3336-46. PMID 23576556 DOI: 10.1158/0008-5472.Can-12-3292 |
0.409 |
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| 2013 |
Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, ... Brennan PE, et al. Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. Journal of Medicinal Chemistry. 56: 3217-27. PMID 23517011 DOI: 10.1021/Jm301588R |
0.412 |
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| 2012 |
Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. Journal of Medicinal Chemistry. 55: 9831-7. PMID 23095041 DOI: 10.1021/Jm3010515 |
0.426 |
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| 2012 |
Hewings DS, Rooney TP, Jennings LE, Hay DA, Schofield CJ, Brennan PE, Knapp S, Conway SJ. Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. Journal of Medicinal Chemistry. 55: 9393-413. PMID 22924434 DOI: 10.1021/Jm300915B |
0.44 |
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| 2012 |
Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, ... ... Brennan PE, et al. Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. Journal of Medicinal Chemistry. 55: 6639-43. PMID 22724510 DOI: 10.1021/Jm300677J |
0.348 |
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| 2012 |
Brennan P, Filippakopoulos P, Knapp S. The therapeutic potential of acetyl-lysine and methyl-lysine effector domains Drug Discovery Today: Therapeutic Strategies. 9: e101-e110. DOI: 10.1016/J.Ddstr.2012.04.001 |
0.406 |
|
| 2011 |
Andrews MD, Fish PV, Blagg J, Brabham TK, Brennan PE, Bridgeland A, Brown AD, Bungay PJ, Conlon KM, Edmunds NJ, af Forselles K, Gibbons CP, Green MP, Hanton G, Holbrook M, et al. Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Bioorganic & Medicinal Chemistry Letters. 21: 2715-20. PMID 21195614 DOI: 10.1016/J.Bmcl.2010.11.120 |
0.549 |
|
| 2009 |
Ley SV, Tackett MN, Maddess ML, Anderson JC, Brennan PE, Cappi MW, Heer JP, Helgen C, Kori M, Kouklovsky C, Marsden SP, Norman J, Osborn DP, Palomero MA, Pavey JB, et al. Total synthesis of rapamycin. Chemistry (Weinheim An Der Bergstrasse, Germany). 15: 2874-914. PMID 19204960 DOI: 10.1002/Chem.200801656 |
0.664 |
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| 2007 |
Maddess ML, Tackett MN, Watanabe H, Brennan PE, Spilling CD, Scott JS, Osborn DP, Ley SV. Total synthesis of rapamycin. Angewandte Chemie (International Ed. in English). 46: 591-7. PMID 17154218 DOI: 10.1002/Anie.200604053 |
0.391 |
|
| 2003 |
Smith MD, Stepan AF, Ramarao C, Brennan PE, Ley SV. Palladium-containing perovskites: recoverable and reuseable catalysts for Suzuki couplings. Chemical Communications (Cambridge, England). 2652-3. PMID 14649794 DOI: 10.1039/B308465E |
0.491 |
|
| 2003 |
MacCoss RN, Brennan PE, Ley SV. Synthesis of carbohydrate derivatives using solid-phase work-up and scavenging techniques. Organic & Biomolecular Chemistry. 1: 2029-31. PMID 12945889 DOI: 10.1039/B303951J |
0.725 |
|
| 2002 |
Spaller MR, Thielemann WT, Brennan PE, Bartlett PA. Combinatorial synthetic design. Solution and polymer-supported synthesis of heterocycles via intramolecular aza Diels-Alder and imino alcohol cyclizations. Journal of Combinatorial Chemistry. 4: 516-22. PMID 12217025 DOI: 10.1021/Cc020027+ |
0.509 |
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