Detalles de la búsqueda
1.
The Absolute Bioavailability and Absorption, Metabolism, and Excretion of Ipatasertib, a Potent and Highly Selective Protein Kinase B (Akt) Inhibitor.
Drug Metab Dispos
; 51(10): 1332-1341, 2023 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-37524543
2.
Evaluation of Ipatasertib Interactions with Itraconazole and Coproporphyrin I and III in a Single Drug Interaction Study in Healthy Subjects.
J Pharmacol Exp Ther
; 378(2): 87-95, 2021 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-34049965
3.
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Bioorg Med Chem Lett
; 29(12): 1497-1501, 2019 06 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-31000154
4.
Preclinical assessment of the ADME, efficacy and drug-drug interaction potential of a novel NAMPT inhibitor.
Xenobiotica
; 49(9): 1063-1077, 2019 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-30257601
5.
Use of Subcutaneous and Intraperitoneal Administration Methods to Facilitate Cassette Dosing in Microdialysis Studies in Rats.
Drug Metab Dispos
; 46(7): 964-969, 2018 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-29700231
6.
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Bioorg Med Chem Lett
; 27(13): 2974-2981, 2017 07 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28512031
7.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-27406798
8.
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.
Bioorg Med Chem Lett
; 26(18): 4492-4496, 2016 09 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27499454
9.
Use of cassette dosing to enhance the throughput of rat brain microdialysis studies.
Drug Metab Dispos
; 43(7): 1123-8, 2015 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-25943358
10.
Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
Bioorg Med Chem Lett
; 25(3): 529-41, 2015 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25556090
11.
Pharmacokinetic drivers of toxicity for basic molecules: strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor.
Toxicol Appl Pharmacol
; 266(1): 86-94, 2013 Jan 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23142475
12.
High-throughput liquid chromatography/mass spectrometry method for the quantitation of small molecules using accurate mass technologies in supporting discovery drug screening.
Rapid Commun Mass Spectrom
; 27(3): 401-8, 2013 Feb 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-23280971
13.
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Bioorg Med Chem Lett
; 23(17): 4875-85, 2013 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23899614
14.
Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Bioorg Med Chem Lett
; 23(12): 3531-8, 2013 Jun 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-23668988
15.
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Bioorg Med Chem Lett
; 23(20): 5488-97, 2013 Oct 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-24021463
16.
Use of the cassette-dosing approach to assess brain penetration in drug discovery.
Drug Metab Dispos
; 40(5): 963-9, 2012 May.
Artículo
en Inglés
| MEDLINE | ID: mdl-22328585
17.
Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors.
Xenobiotica
; 42(5): 456-65, 2012 May.
Artículo
en Inglés
| MEDLINE | ID: mdl-22122353
18.
Preclinical absorption, distribution, metabolism, excretion, and pharmacokinetic-pharmacodynamic modelling of N-(4-(3-((3S,4R)-1-ethyl-3-fluoropiperidine-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-4-yloxy)-3-fluorophenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide, a novel MET kinase inhibitor.
Xenobiotica
; 41(4): 327-39, 2011 Apr.
Artículo
en Inglés
| MEDLINE | ID: mdl-21182395
19.
Translational and pharmacokinetic-pharmacodynamic application for the clinical development of GDC-0334, a novel TRPA1 inhibitor.
Clin Transl Sci
; 14(5): 1945-1954, 2021 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-34058071
20.
A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment.
J Exp Med
; 218(4)2021 04 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-33620419