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1.
Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
ACS Med Chem Lett
; 13(10): 1591-1597, 2022 Oct 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-36262388
2.
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
J Med Chem
; 64(16): 12286-12303, 2021 08 26.
Artículo
en Inglés
| MEDLINE | ID: mdl-34387469
3.
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein-Protein Interaction.
J Med Chem
; 64(7): 4071-4088, 2021 04 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-33761253
4.
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
J Med Chem
; 61(16): 7314-7329, 2018 08 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-30091600
5.
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
J Med Chem
; 61(11): 4978-4992, 2018 06 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-29775310
6.
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
J Med Chem
; 50(13): 3101-12, 2007 Jun 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-17536796
7.
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.
J Med Chem
; 50(20): 4789-92, 2007 Oct 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-17850061
8.
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
J Med Chem
; 60(11): 4611-4625, 2017 06 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-28492317
9.
Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.
J Med Chem
; 49(7): 2253-61, 2006 Apr 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-16570921
10.
Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.
J Med Chem
; 48(22): 6790-802, 2005 Nov 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-16250638
11.
Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.
J Med Chem
; 48(22): 6803-12, 2005 Nov 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-16250639
12.
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.
ACS Med Chem Lett
; 6(7): 798-803, 2015 Jul 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-26191369
13.
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.
J Med Chem
; 58(16): 6574-88, 2015 Aug 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-26218264
14.
CCK(2) receptor antagonists containing the conformationally constrained phenylalanine derivatives, including the new amino acid Xic.
Eur J Med Chem
; 37(5): 379-89, 2002 May.
Artículo
en Inglés
| MEDLINE | ID: mdl-12008052
15.
omega-(Imidazol-4-yl)alkane-1-sulfonamides: a new series of potent histamine H(3) receptor antagonists.
Bioorg Med Chem
; 10(2): 425-32, 2002 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-11741790
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