| Year |
Citation |
Score |
| 2022 |
Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, ... ... Tsui V, et al. GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. Journal of Medicinal Chemistry. PMID 35930799 DOI: 10.1021/acs.jmedchem.2c00662 |
0.334 |
|
| 2019 |
Nittinger E, Gibbons P, Eigenbrot C, Davies DR, Maurer B, Yu CL, Kiefer JR, Kuglstatter A, Murray J, Ortwine DF, Tang Y, Tsui V. Water molecules in protein-ligand interfaces. Evaluation of software tools and SAR comparison. Journal of Computer-Aided Molecular Design. PMID 30756207 DOI: 10.1007/S10822-019-00187-Y |
0.364 |
|
| 2019 |
Wang X, Blackaby WP, Allen V, Chan GKY, Chang JH, Chiang PC, Diene C, Drummond J, Do S, Fan E, Harstad E, Hodges A, Hu H, Jia W, Kofie W, ... ... Tsui V, et al. Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma. Journal of Medicinal Chemistry. PMID 30715878 DOI: 10.1021/Acs.Jmedchem.8B01857 |
0.413 |
|
| 2018 |
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, et al. GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like. Journal of Medicinal Chemistry. PMID 30289257 DOI: 10.1021/acs.jmedchem.8b01225 |
0.428 |
|
| 2018 |
Wertz I, Kategaya L, Lello PD, Rouge L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton J, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, ... ... Tsui V, et al. Abstract SY23-03: Development and mechanistic characterization of USP7 deubiquitinase inhibitors Cancer Research. 78. DOI: 10.1158/1538-7445.Am2018-Sy23-03 |
0.468 |
|
| 2017 |
Lai KW, Romero FA, Tsui V, Beresini MH, de Leon Boenig G, Bronner SM, Chen K, Chen Z, Choo EF, Crawford TD, Cyr P, Kaufman S, Li Y, Liao J, Liu W, et al. Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. Bioorganic & Medicinal Chemistry Letters. PMID 29169673 DOI: 10.1016/J.Bmcl.2017.11.025 |
0.438 |
|
| 2017 |
Di Lello P, Pastor R, Murray JM, Blake RA, Cohen F, Crawford TD, Drobnick J, Drummond J, Kategaya L, Kleinheinz T, Maurer T, Rouge L, Zhao X, Wertz I, Ndubaku C, ... Tsui V, et al. Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and In-Silico Techniques. Journal of Medicinal Chemistry. PMID 29166018 DOI: 10.1021/Acs.Jmedchem.7B01293 |
0.453 |
|
| 2017 |
Bronner SM, Murray JM, Romero FA, Lai KW, Tsui V, Cyr P, Beresini MH, de Leon Boenig G, Chen Z, Choo EF, Clark KR, Crawford TD, Jayaram H, Kaufman S, Li R, et al. A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors. Journal of Medicinal Chemistry. PMID 29155580 DOI: 10.1021/acs.jmedchem.7b01372 |
0.444 |
|
| 2017 |
Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, ... ... Tsui V, et al. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. PMID 29045385 DOI: 10.1038/Nature24006 |
0.461 |
|
| 2017 |
Romero FA, Murray JM, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). Journal of Medicinal Chemistry. PMID 28892380 DOI: 10.1021/Acs.Jmedchem.7B00796 |
0.461 |
|
| 2017 |
Liang J, Van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair WS, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Goodacre S, Ghilardi N, MacLeod C, Johnson A, ... ... Tsui V, et al. Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model. Bioorganic & Medicinal Chemistry Letters. PMID 28830649 DOI: 10.1016/J.Bmcl.2017.08.022 |
0.413 |
|
| 2017 |
Crawford TD, Audia JE, Bellon S, Burdick DJ, Bommi-Reddy A, Côté A, Cummings RT, Duplessis M, Flynn EM, Hewitt M, Huang HR, Jayaram H, Jiang Y, Joshi S, Kiefer JR, ... ... Tsui V, et al. GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2). Acs Medicinal Chemistry Letters. 8: 737-741. PMID 28740608 DOI: 10.1021/Acsmedchemlett.7B00132 |
0.422 |
|
| 2017 |
Crawford TD, Vartanian S, Côté A, Bellon S, Duplessis M, Flynn EM, Hewitt M, Huang HR, Kiefer JR, Murray J, Nasveschuk CG, Pardo E, Romero FA, Sandy P, Tang Y, ... ... Tsui V, et al. Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance. Bioorganic & Medicinal Chemistry Letters. PMID 28606761 DOI: 10.1016/J.Bmcl.2017.05.063 |
0.428 |
|
| 2017 |
Wang X, Kolesnikov A, Tay S, Chan G, Chao Q, Do S, Drummond J, Ebens AJ, Liu N, Ly JQ, Harstad E, Hu H, Moffat JG, Munugalavadla V, Murray JM, ... ... Tsui V, et al. Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability. Journal of Medicinal Chemistry. PMID 28445037 DOI: 10.1021/Acs.Jmedchem.7B00418 |
0.427 |
|
| 2017 |
Kategaya L, Cuellar T, Haley B, Liu J, Tran A, Cao Y, Stokoe D, McCleland M, Blackwood B, Yee S, Drobnick J, Drummond J, Ernst J, Kwok M, Ly C, ... ... Tsui V, et al. Abstract B23: Crucial deubiquitinases in cancer cell survival Clinical Cancer Research. 23. DOI: 10.1158/1557-3265.Pmccavuln16-B23 |
0.325 |
|
| 2016 |
Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. Journal of Medicinal Chemistry. PMID 27682507 DOI: 10.1021/Acs.Jmedchem.6B01022 |
0.421 |
|
| 2016 |
Crawford TD, Tsui V, Flynn EM, Wang S, Taylor AM, Côté A, Audia JE, Beresini MH, Burdick DJ, Cummings RT, Dakin LA, Duplessis M, Good AC, Hewitt MC, Huang HR, et al. Diving into the water: Inducible binding conformations for BRD4, TAF1(2), BRD9, and CECR2 bromodomains. Journal of Medicinal Chemistry. PMID 27219867 DOI: 10.1021/Acs.Jmedchem.6B00264 |
0.438 |
|
| 2016 |
Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, ... ... Tsui V, et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). Acs Medicinal Chemistry Letters. 7: 531-536. PMID 27190605 DOI: 10.1021/Acsmedchemlett.6B00075 |
0.447 |
|
| 2016 |
Ghosh S, Taylor A, Chin M, Huang HR, Conery AR, Mertz JA, Salmeron A, Dakle PJ, Mele D, Cote A, Jayaram H, Setser JW, Poy F, Hatzivassiliou G, DeAlmeida-Nagata D, ... ... Tsui V, et al. Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition. The Journal of Biological Chemistry. PMID 27056325 DOI: 10.1074/Jbc.M115.708560 |
0.361 |
|
| 2016 |
Heffron TP, Heald RA, Ndubaku CO, Wei B, Augustin M, Do S, Edgar K, Eigenbrot C, Lori F, Gancia E, Jackson P, Jones G, Kolesnikov A, Lee L, Lesnick J, ... ... Tsui V, et al. The Rational Design of Selective Benzoxazepin Inhibitors of the -Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). Journal of Medicinal Chemistry. PMID 26741947 DOI: 10.1021/Acs.Jmedchem.5B01483 |
0.48 |
|
| 2015 |
Romero FA, Taylor AM, Crawford TD, Tsui V, Cote A, Magnuson S. Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors. Journal of Medicinal Chemistry. PMID 26572217 DOI: 10.1021/Acs.Jmedchem.5B01514 |
0.423 |
|
| 2015 |
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, et al. Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors. Bioorganic & Medicinal Chemistry Letters. 25: 5258-64. PMID 26459208 DOI: 10.1016/J.Bmcl.2015.09.052 |
0.478 |
|
| 2015 |
Feng JA, Aliagas I, Bergeron P, Blaney JM, Bradley EK, Koehler MF, Lee ML, Ortwine DF, Tsui V, Wu J, Gobbi A. An integrated suite of modeling tools that empower scientists in structure- and property-based drug design. Journal of Computer-Aided Molecular Design. 29: 511-23. PMID 25921252 DOI: 10.1007/S10822-015-9845-4 |
0.371 |
|
| 2015 |
Sharpe HJ, Pau G, Dijkgraaf GJ, Basset-Seguin N, Modrusan Z, Januario T, Tsui V, Durham AB, Dlugosz AA, Haverty PM, Bourgon R, Tang JY, Sarin KY, Dirix L, Fisher DC, et al. Genomic analysis of smoothened inhibitor resistance in basal cell carcinoma. Cancer Cell. 27: 327-41. PMID 25759019 DOI: 10.1016/J.Ccell.2015.02.001 |
0.311 |
|
| 2015 |
Ndubaku C, Tsui V. Inhibiting the deubiquitinating enzymes (DUBs). Journal of Medicinal Chemistry. 58: 1581-95. PMID 25364867 DOI: 10.1021/Jm501061A |
0.384 |
|
| 2013 |
Siu M, Pastor R, Liu W, Barrett K, Berry M, Blair WS, Chang C, Chen JZ, Eigenbrot C, Ghilardi N, Gibbons P, He H, Hurley CA, Kenny JR, Cyrus Khojasteh S, ... ... Tsui V, et al. 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 5014-21. PMID 23870430 DOI: 10.1016/J.Bmcl.2013.06.008 |
0.389 |
|
| 2013 |
Liang J, Tsui V, Van Abbema A, Bao L, Barrett K, Beresini M, Berezhkovskiy L, Blair WS, Chang C, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, et al. Lead identification of novel and selective TYK2 inhibitors. European Journal of Medicinal Chemistry. 67: 175-87. PMID 23867602 DOI: 10.1016/J.Ejmech.2013.03.070 |
0.455 |
|
| 2013 |
Liang J, van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair W, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, ... ... Tsui V, et al. Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. Journal of Medicinal Chemistry. 56: 4521-36. PMID 23668484 DOI: 10.1021/Jm400266T |
0.418 |
|
| 2013 |
Wang X, Magnuson S, Pastor R, Fan E, Hu H, Tsui V, Deng W, Murray J, Steffek M, Wallweber H, Moffat J, Drummond J, Chan G, Harstad E, Ebens AJ. Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design. Bioorganic & Medicinal Chemistry Letters. 23: 3149-53. PMID 23623490 DOI: 10.1016/J.Bmcl.2013.04.020 |
0.477 |
|
| 2013 |
Staben ST, Blaquiere N, Tsui V, Kolesnikov A, Do S, Bradley EK, Dotson J, Goldsmith R, Heffron TP, Lesnick J, Lewis C, Murray J, Nonomiya J, Olivero AG, Pang J, et al. Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase. Bioorganic & Medicinal Chemistry Letters. 23: 897-901. PMID 23265894 DOI: 10.1016/J.Bmcl.2012.10.121 |
0.409 |
|
| 2012 |
Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, ... ... Tsui V, et al. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). Journal of Medicinal Chemistry. 55: 4101-13. PMID 22413863 DOI: 10.1021/Jm300060K |
0.388 |
|
| 2012 |
Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ. Erratum to “Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres” [Bioorg. Med. Chem. Lett. 20 (2010) 2229–2233] Bioorganic & Medicinal Chemistry Letters. 22: 753-754. DOI: 10.1016/J.Bmcl.2011.11.056 |
0.36 |
|
| 2011 |
Heffron TP, Wei B, Olivero A, Staben ST, Tsui V, Do S, Dotson J, Folkes AJ, Goldsmith P, Goldsmith R, Gunzner J, Lesnick J, Lewis C, Mathieu S, Nonomiya J, et al. Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform. Journal of Medicinal Chemistry. 54: 7815-33. PMID 21985639 DOI: 10.1021/Jm2007084 |
0.446 |
|
| 2011 |
Sutherlin DP, Bao L, Berry M, Castanedo G, Chuckowree I, Dotson J, Folks A, Friedman L, Goldsmith R, Gunzner J, Heffron T, Lesnick J, Lewis C, Mathieu S, Murray J, ... ... Tsui V, et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. Journal of Medicinal Chemistry. 54: 7579-87. PMID 21981714 DOI: 10.1021/Jm2009327 |
0.478 |
|
| 2011 |
Staben ST, Siu M, Goldsmith R, Olivero AG, Do S, Burdick DJ, Heffron TP, Dotson J, Sutherlin DP, Zhu BY, Tsui V, Le H, Lee L, Lesnick J, Lewis C, et al. Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. Bioorganic & Medicinal Chemistry Letters. 21: 4054-8. PMID 21636270 DOI: 10.1016/J.Bmcl.2011.04.124 |
0.421 |
|
| 2011 |
Tsui V, Gibbons P, Ultsch M, Mortara K, Chang C, Blair W, Pulk R, Stanley M, Starovasnik M, Williams D, Lamers M, Leonard P, Magnuson S, Liang J, Eigenbrot C. A new regulatory switch in a JAK protein kinase. Proteins. 79: 393-401. PMID 21117080 DOI: 10.1002/Prot.22889 |
0.39 |
|
| 2011 |
Sutherlin DP, Belvin M, Bao L, Berry L, Berry M, Castanedo G, Edgar K, Folkes A, Friedman L, Heffron T, Patel S, Olivero A, Lesnick J, Lewis C, Marsters J, ... ... Tsui V, et al. Abstract 2787: Discovery of GDC-0980, a selective PI3K/mTOR inhibitor in clinical trials Cancer Research. 71: 2787-2787. DOI: 10.1158/1538-7445.Am2011-2787 |
0.485 |
|
| 2010 |
Staben ST, Heffron TP, Sutherlin DP, Bhat SR, Castanedo GM, Chuckowree IS, Dotson J, Folkes AJ, Friedman LS, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Olivero AG, ... ... Tsui V, et al. Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase. Bioorganic & Medicinal Chemistry Letters. 20: 6048-51. PMID 20822905 DOI: 10.1016/J.Bmcl.2010.08.067 |
0.429 |
|
| 2010 |
Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, ... ... Tsui V, et al. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor. Bioorganic & Medicinal Chemistry Letters. 20: 2408-11. PMID 20346656 DOI: 10.1016/J.Bmcl.2010.03.046 |
0.465 |
|
| 2010 |
Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ. Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres. Bioorganic & Medicinal Chemistry Letters. 20: 2229-33. PMID 20189383 DOI: 10.1016/J.Bmcl.2010.02.021 |
0.38 |
|
| 2010 |
Sutherlin DP, Sampath D, Berry M, Castanedo G, Chang Z, Chuckowree I, Dotson J, Folkes A, Friedman L, Goldsmith R, Heffron T, Lee L, Lesnick J, Lewis C, Mathieu S, ... ... Tsui V, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. Journal of Medicinal Chemistry. 53: 1086-97. PMID 20050669 DOI: 10.1021/Jm901284W |
0.481 |
|
| 2009 |
Ndubaku C, Varfolomeev E, Wang L, Zobel K, Lau K, Elliott LO, Maurer B, Fedorova AV, Dynek JN, Koehler M, Hymowitz SG, Tsui V, Deshayes K, Fairbrother WJ, Flygare JA, et al. Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists. Acs Chemical Biology. 4: 557-66. PMID 19492850 DOI: 10.1021/Cb900083M |
0.358 |
|
| 2009 |
Cohen F, Alicke B, Elliott LO, Flygare JA, Goncharov T, Keteltas SF, Franklin MC, Frankovitz S, Stephan JP, Tsui V, Vucic D, Wong H, Fairbrother WJ. Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold. Journal of Medicinal Chemistry. 52: 1723-30. PMID 19228017 DOI: 10.1021/Jm801450C |
0.382 |
|
| 2006 |
Castanedo G, Clark K, Wang S, Tsui V, Wong M, Nicholas J, Wickramasinghe D, Marsters JC, Sutherlin D. CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads. Bioorganic & Medicinal Chemistry Letters. 16: 1716-20. PMID 16384702 DOI: 10.1016/J.Bmcl.2005.12.004 |
0.385 |
|
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