Detalles de la búsqueda
1.
Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Bioorg Med Chem
; 26(3): 721-736, 2018 02 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29342416
2.
Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.
Bioorg Med Chem
; 26(3): 647-660, 2018 02 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29291937
3.
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Bioorg Med Chem
; 26(2): 483-500, 2018 01 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-29262987
4.
Biochemical Properties of TAK-828F, a Potent and Selective Retinoid-Related Orphan Receptor Gamma t Inverse Agonist.
Pharmacology
; 102(5-6): 244-252, 2018.
Artículo
en Inglés
| MEDLINE | ID: mdl-30134246
5.
Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKCθ inhibitors.
Bioorg Med Chem
; 24(11): 2466-75, 2016 06 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27117263
6.
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.
J Biol Chem
; 286(21): 18756-65, 2011 May 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-21454582
7.
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Bioorg Med Chem
; 20(18): 5600-15, 2012 Sep 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22883026
8.
A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR) γ agonists: design and synthesis of benzylpyrazole acylsulfonamides.
Bioorg Med Chem
; 20(2): 714-33, 2012 Jan 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22209730
9.
Structure-activity relationships and key structural feature of pyridyloxybenzene-acylsulfonamides as new, potent, and selective peroxisome proliferator-activated receptor (PPAR) γ Agonists.
Bioorg Med Chem
; 20(10): 3332-58, 2012 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22503460
10.
Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors.
Bioorg Med Chem Lett
; 21(21): 6314-8, 2011 Nov 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-21944854
11.
Structure-Based Design, Synthesis, and Biological Evaluation of Imidazo[4,5-b]Pyridin-2-one-Based p38 MAP Kinase Inhibitors: Partâ 2.
ChemMedChem
; 14(24): 2093-2101, 2019 12 17.
Artículo
en Inglés
| MEDLINE | ID: mdl-31697454
12.
Structure-Based Design, Synthesis, and Biological Evaluation of Imidazo[4,5-b]pyridin-2-one-Based p38 MAP Kinase Inhibitors: Part 1.
ChemMedChem
; 14(10): 1022-1030, 2019 05 17.
Artículo
en Inglés
| MEDLINE | ID: mdl-30945818
13.
Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists.
ChemMedChem
; 14(22): 1917-1932, 2019 11 20.
Artículo
en Inglés
| MEDLINE | ID: mdl-31659845
14.
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
J Med Chem
; 62(3): 1167-1179, 2019 02 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-30652849
15.
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
ACS Med Chem Lett
; 10(10): 1498-1503, 2019 Oct 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-31620240
16.
Cholesterol Unbound RORγt Protein Enables a Sensitive Inverse Agonist Screening.
Assay Drug Dev Technol
; 16(4): 194-204, 2018.
Artículo
en Inglés
| MEDLINE | ID: mdl-29874096
17.
Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
J Med Chem
; 61(7): 2973-2988, 2018 04 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-29510038
18.
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
J Med Chem
; 60(16): 6942-6990, 2017 08 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-28699740
19.
Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography.
Structure
; 10(12): 1659-67, 2002 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-12467573
20.
Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases.
Structure
; 12(7): 1325-34, 2004 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-15242608