| Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation O Gilan, I Rioja, K Knezevic, MJ Bell, MM Yeung, NR Harker, EYN Lam, ... Science 368 (6489), 387-394, 2020 | 353 | 2020 |
| Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy S Picaud, O Fedorov, A Thanasopoulou, K Leonards, K Jones, J Meier, ... Cancer research 75 (23), 5106-5119, 2015 | 255 | 2015 |
| The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor R Gosmini, VL Nguyen, J Toum, C Simon, JMG Brusq, G Krysa, O Mirguet, ... Journal of medicinal chemistry 57 (19), 8111-8131, 2014 | 212 | 2014 |
| Protein arginine deiminase 4 inhibition is sufficient for the amelioration of collagen-induced arthritis VC Willis, NK Banda, KN Cordova, PE Chandra, WH Robinson, ... Clinical & Experimental Immunology 188 (2), 263-274, 2017 | 108 | 2017 |
| Modification of the ultrafiltration technique to overcome solubility and non-specific binding challenges associated with the measurement of plasma protein binding of … S Taylor, A Harker Journal of pharmaceutical and biomedical analysis 41 (1), 299-303, 2006 | 94 | 2006 |
| Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor K Biggadike, RK Bledsoe, DM Coe, TWJ Cooper, D House, MA Iannone, ... Proceedings of the National Academy of Sciences 106 (43), 18114-18119, 2009 | 84 | 2009 |
| The optimization of a novel, weak bromo and extra terminal domain (BET) bromodomain fragment ligand to a potent and selective second bromodomain (BD2) inhibitor JT Seal, SJ Atkinson, H Aylott, P Bamborough, C Chung, RCB Copley, ... Journal of Medicinal Chemistry 63 (17), 9093-9126, 2020 | 52 | 2020 |
| Small-molecule inhibition of the acyl-lysine reader ENL as a strategy against acute myeloid leukemia Y Liu, Q Li, F Alikarami, DR Barrett, L Mahdavi, H Li, S Tang, TA Khan, ... Cancer discovery 12 (11), 2684-2709, 2022 | 45 | 2022 |
| Structure-based design of a bromodomain and extraterminal domain (BET) inhibitor selective for the N-terminal bromodomains that retains an anti-inflammatory and … CR Wellaway, P Bamborough, SG Bernard, C Chung, PD Craggs, ... Journal of Medicinal Chemistry 63 (17), 9020-9044, 2020 | 42 | 2020 |
| Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of … A Preston, S Atkinson, P Bamborough, C Chung, PD Craggs, L Gordon, ... Journal of Medicinal Chemistry 63 (17), 9070-9092, 2020 | 42 | 2020 |
| Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose EH Demont, S Arpino, RA Bit, CA Campbell, N Deeks, S Desai, SJ Dowell, ... Journal of medicinal chemistry 54 (19), 6724-6733, 2011 | 34 | 2011 |
| Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists CM Yates, PJ Brown, EL Stewart, C Patten, RJH Austin, JA Holt, ... Journal of medicinal chemistry 53 (11), 4531-4544, 2010 | 33 | 2010 |
| Discovery of a novel bromodomain and extra terminal domain (BET) protein inhibitor, I-BET282E, suitable for clinical progression KL Jones, DM Beaumont, SG Bernard, RA Bit, SP Campbell, C Chung, ... Journal of Medicinal Chemistry 64 (16), 12200-12227, 2021 | 29 | 2021 |
| Discovery of a highly selective BET BD2 inhibitor from a DNA-encoded library technology screening hit F Rianjongdee, SJ Atkinson, C Chung, P Grandi, JRJ Gray, ... Journal of Medicinal Chemistry 64 (15), 10806-10833, 2021 | 29 | 2021 |
| Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists HA Barnett, DM Coe, TWJ Cooper, TI Jack, HT Jones, SJF Macdonald, ... Bioorganic & Medicinal Chemistry Letters 19 (1), 158-162, 2009 | 29 | 2009 |
| Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate EH Demont, BI Andrews, RA Bit, CA Campbell, JWB Cooke, N Deeks, ... ACS Medicinal Chemistry Letters 2 (6), 444-449, 2011 | 27 | 2011 |
| GSK973 is an inhibitor of the second bromodomains (BD2s) of the bromodomain and extra-terminal (BET) family A Preston, SJ Atkinson, P Bamborough, C Chung, LJ Gordon, P Grandi, ... ACS Medicinal Chemistry Letters 11 (8), 1581-1587, 2020 | 25 | 2020 |
| BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo MA Morse, KK Balogh, SA Brendle, CA Campbell, MX Chen, RC Furze, ... Antiviral research 154, 158-165, 2018 | 24 | 2018 |
| Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles J Skidmore, J Heer, CN Johnson, D Norton, S Redshaw, J Sweeting, ... Journal of Medicinal Chemistry 57 (24), 10424-10442, 2014 | 21 | 2014 |
| Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra … LA Harrison, SJ Atkinson, A Bassil, C Chung, P Grandi, JRJ Gray, ... Journal of Medicinal Chemistry 64 (15), 10742-10771, 2021 | 18 | 2021 |
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