Detalhe da pesquisa
1.
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Bioorg Med Chem Lett;
50: 128335, 2021 10 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-34425201
2.
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Bioorg Med Chem Lett;
29(16): 2090-2093, 2019 08 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-31311734
3.
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Bioorg Med Chem Lett;
29(7): 905-911, 2019 04 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-30732944
4.
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Bioorg Med Chem Lett;
28(1): 15-23, 2018 01 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-29169673
5.
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Bioorg Med Chem Lett;
27(13): 2974-2981, 2017 07 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28512031
6.
Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Bioorg Med Chem Lett;
26(16): 4036-41, 2016 08 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27406798
7.
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
J Med Chem;
64(16): 11841-11856, 2021 08 26.
Artigo
em Inglês
| MEDLINE
| ID: mdl-34251202
8.
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
ACS Med Chem Lett;
11(6): 1342-1347, 2020 Jun 11.
Artigo
em Inglês
| MEDLINE
| ID: mdl-32551022
9.
Investigation on the interaction between a heterocyclic aminal derivative, SBDC, and human serum albumin.
Colloids Surf B Biointerfaces;
61(1): 75-80, 2008 Jan 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17768036
10.
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
J Med Chem;
60(24): 10151-10171, 2017 12 28.
Artigo
em Inglês
| MEDLINE
| ID: mdl-29155580
11.
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
J Med Chem;
60(22): 9162-9183, 2017 11 22.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28892380
12.
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
J Med Chem;
59(23): 10549-10563, 2016 12 08.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27682507
13.
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
ACS Med Chem Lett;
7(5): 531-6, 2016 May 12.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27190605
14.
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
J Med Chem;
57(23): 10112-29, 2014 Dec 11.
Artigo
em Inglês
| MEDLINE
| ID: mdl-25411915
15.
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
J Med Chem;
56(11): 4764-85, 2013 Jun 13.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23659214
16.
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
J Med Chem;
55(13): 6176-93, 2012 Jul 12.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22698084