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1.
A Chemical Probe for the ATAD2 Bromodomain.
Angew Chem Int Ed Engl
; 55(38): 11382-6, 2016 09 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-27530368
2.
Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.
J Med Chem
; 2024 Jun 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-38866424
3.
Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors.
ACS Med Chem Lett
; 14(9): 1231-1236, 2023 Sep 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-37736196
4.
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
J Med Chem
; 66(23): 15728-15749, 2023 12 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-37967462
5.
Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
ACS Med Chem Lett
; 12(8): 1308-1317, 2021 Aug 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-34413961
6.
Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
J Med Chem
; 64(15): 10711-10741, 2021 08 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-34260229
7.
Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
J Med Chem
; 64(15): 10742-10771, 2021 08 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-34232650
8.
Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.
J Med Chem
; 64(15): 10806-10833, 2021 08 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-34251219
9.
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J Med Chem
; 64(6): 3249-3281, 2021 03 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-33662213
10.
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
J Med Chem
; 64(15): 10772-10805, 2021 08 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-34255512
11.
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
J Med Chem
; 64(16): 12200-12227, 2021 08 26.
Artículo
en Inglés
| MEDLINE | ID: mdl-34387088
12.
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Bioorg Med Chem Lett
; 20(10): 3161-4, 2010 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-20399651
13.
Domain-selective targeting of BET proteins in cancer and immunological diseases.
Curr Opin Chem Biol
; 57: 184-193, 2020 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-32741705
14.
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.
J Med Chem
; 63(17): 9045-9069, 2020 09 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-32691589
15.
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
J Med Chem
; 63(10): 5212-5241, 2020 05 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-32321240
16.
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 Proteins.
J Med Chem
; 63(17): 9070-9092, 2020 09 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-32691591
17.
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
ACS Med Chem Lett
; 11(8): 1581-1587, 2020 Aug 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-32832027
18.
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
J Med Chem
; 63(17): 9020-9044, 2020 09 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-32787145
19.
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
J Med Chem
; 63(17): 9093-9126, 2020 09 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-32702236
20.
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
Science
; 368(6489): 387-394, 2020 04 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-32193360