Detalhe da pesquisa
1.
Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry.
Anal Chem
; 95(11): 4834-4839, 2023 03 21.
Artigo
em Inglês
| MEDLINE | ID: mdl-36876898
2.
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Bioorg Med Chem Lett
; 26(2): 534-539, 2016 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26639762
3.
Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.
Bioorg Med Chem Lett
; 26(15): 3518-24, 2016 08 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27346791
4.
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.
Bioorg Med Chem Lett
; 26(18): 4455-4461, 2016 09 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27524313
5.
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Bioorg Med Chem Lett
; 25(19): 4109-13, 2015 Oct 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26321361
6.
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Bioorg Med Chem Lett
; 25(15): 2907-12, 2015 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26048793
7.
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Bioorg Med Chem Lett
; 24(16): 3891-7, 2014 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-25017032
8.
A reversed sulfonamide series of selective RORc inverse agonists.
Bioorg Med Chem Lett
; 24(24): 5769-5776, 2014 Dec 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-25453817
9.
Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-in-Class Therapy for Respiratory Disease.
J Med Chem
; 67(5): 3287-3306, 2024 Mar 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-38431835
10.
Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist.
Drug Metab Dispos
; 41(12): 2104-13, 2013 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-24041744
11.
Systemic concentrations can limit the oral absorption of poorly soluble drugs: an investigation of non-sink permeation using physiologically based pharmacokinetic modeling.
Mol Pharm
; 10(11): 3980-8, 2013 Nov 04.
Artigo
em Inglês
| MEDLINE | ID: mdl-23611122
12.
Novel nanoparticles formulation for cassette dosing via intravenous injection in rats for high throughput pharmacokinetic screening and potential applications.
J Nanosci Nanotechnol
; 12(10): 7993-8000, 2012 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-23421169
13.
Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor.
Drug Metab Dispos
; 39(10): 1840-9, 2011 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-21742900
14.
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
ACS Med Chem Lett
; 12(5): 791-797, 2021 May 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-34055227
15.
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
J Med Chem
; 64(7): 3940-3955, 2021 04 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-33780623
16.
Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.
J Med Chem
; 64(7): 3843-3869, 2021 04 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-33749283
17.
Interplay of dissolution, solubility, and nonsink permeation determines the oral absorption of the Hedgehog pathway inhibitor GDC-0449 in dogs: an investigation using preclinical studies and physiologically based pharmacokinetic modeling.
Drug Metab Dispos
; 38(7): 1029-38, 2010 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-20406853
18.
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.
ACS Med Chem Lett
; 11(4): 541-549, 2020 Apr 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-32292562
19.
GDC-0449-a potent inhibitor of the hedgehog pathway.
Bioorg Med Chem Lett
; 19(19): 5576-81, 2009 Oct 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19716296
20.
Cyclodextrin Reduces Intravenous Toxicity of a Model Compound.
J Pharm Sci
; 108(6): 1934-1943, 2019 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-30639736