Detalles de la búsqueda
1.
Optimization of a Series of RIPK2 PROTACs.
J Med Chem
; 64(17): 12978-13003, 2021 09 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-34432979
2.
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.
Bioorg Med Chem Lett
; 20(1): 371-4, 2010 Jan 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19926282
3.
Understanding Pharmacokinetic Disconnect in Preclinical Species for 4-Aminoquinolines: Consequences of Low Permeability and High P-glycoprotein Efflux Ratio on Rat and Dog Oral Pharmacokinetics.
J Pharm Sci
; 109(10): 3160-3171, 2020 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-32565354
4.
Correction to Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
ACS Med Chem Lett
; 11(6): 1353, 2020 Jun 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-32551024
5.
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.
Bioorg Med Chem Lett
; 19(10): 2637-41, 2009 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19376703
6.
Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.
Bioorg Med Chem Lett
; 19(15): 4292-5, 2009 Aug 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19487124
7.
Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.
Bioorg Med Chem Lett
; 19(15): 4441-5, 2009 Aug 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19497745
8.
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.
Bioorg Med Chem Lett
; 19(16): 4664-8, 2009 Aug 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19616429
9.
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
ACS Med Chem Lett
; 10(6): 857-862, 2019 Jun 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-31223438
10.
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.
J Med Chem
; 62(14): 6482-6494, 2019 07 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-31265286
11.
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
J Med Chem
; 62(10): 5096-5110, 2019 05 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-31013427
12.
Development of potent and selective small-molecule human Urotensin-II antagonists.
Bioorg Med Chem Lett
; 18(12): 3500-3, 2008 Jun 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-18502123
13.
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Bioorg Med Chem Lett
; 18(13): 3716-9, 2008 Jul 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-18524591
14.
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.
ACS Med Chem Lett
; 9(10): 1039-1044, 2018 Oct 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-30344914
15.
Identification of an antibody-based immunoassay for measuring direct target binding of RIPK1 inhibitors in cells and tissues.
Pharmacol Res Perspect
; 5(6)2017 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-29226625
16.
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.
J Med Chem
; 60(4): 1247-1261, 2017 02 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-28151659
17.
Investigation of the utility of published in vitro intrinsic clearance data for prediction of in vivo clearance.
J Pharmacol Toxicol Methods
; 53(2): 106-16, 2006.
Artículo
en Inglés
| MEDLINE | ID: mdl-16188462
18.
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
J Med Chem
; 59(5): 2163-78, 2016 Mar 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-26854747
19.
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
J Med Chem
; 59(10): 4867-80, 2016 05 26.
Artículo
en Inglés
| MEDLINE | ID: mdl-27109867
20.
A comprehensive analysis of the role of correction factors in the allometric predictivity of clearance from rat, dog, and monkey to humans.
J Pharm Sci
; 93(10): 2522-34, 2004 Oct.
Artículo
en Inglés
| MEDLINE | ID: mdl-15349961