Search details
1.
Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140.
BMC Biol
; 20(1): 182, 2022 08 19.
Article
in English
| MEDLINE | ID: mdl-35986286
2.
A Chemical Probe for the ATAD2 Bromodomain.
Angew Chem Int Ed Engl
; 55(38): 11382-6, 2016 09 12.
Article
in English
| MEDLINE | ID: mdl-27530368
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.
Article
in English
| 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.
Article
in English
| MEDLINE | ID: mdl-37967462
5.
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.
Article
in English
| MEDLINE | ID: mdl-34232650
6.
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.
Article
in English
| MEDLINE | ID: mdl-34387088
7.
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
J Med Chem
; 63(10): 5212-5241, 2020 05 28.
Article
in English
| MEDLINE | ID: mdl-32321240
8.
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.
Article
in English
| MEDLINE | ID: mdl-32691591
9.
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.
Article
in English
| MEDLINE | ID: mdl-32832027
10.
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.
Article
in English
| MEDLINE | ID: mdl-32787145
11.
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
J Med Chem
; 63(2): 714-746, 2020 01 23.
Article
in English
| MEDLINE | ID: mdl-31904959
12.
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
J Med Chem
; 62(16): 7506-7525, 2019 08 22.
Article
in English
| MEDLINE | ID: mdl-31398032
13.
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Bioorg Med Chem Lett
; 18(20): 5609-13, 2008 Oct 15.
Article
in English
| MEDLINE | ID: mdl-18809327
14.
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Bioorg Med Chem Lett
; 18(24): 6429-36, 2008 Dec 15.
Article
in English
| MEDLINE | ID: mdl-19006669
15.
Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors.
J Med Chem
; 61(18): 8321-8336, 2018 09 27.
Article
in English
| MEDLINE | ID: mdl-30226378
16.
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
ACS Med Chem Lett
; 7(6): 552-7, 2016 Jun 09.
Article
in English
| MEDLINE | ID: mdl-27326325
17.
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
J Med Chem
; 58(15): 6151-78, 2015 Aug 13.
Article
in English
| MEDLINE | ID: mdl-26230603
18.
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.
J Med Chem
; 58(14): 5649-73, 2015 Jul 23.
Article
in English
| MEDLINE | ID: mdl-26155854
19.
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
ACS Med Chem Lett
; 5(11): 1190-5, 2014 Nov 13.
Article
in English
| MEDLINE | ID: mdl-25408830
20.
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
J Med Chem
; 52(4): 1180-9, 2009 Feb 26.
Article
in English
| MEDLINE | ID: mdl-19191554