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1.
Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation.
J Biol Chem
; 294(23): 9029-9036, 2019 06 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-31018963
2.
Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors.
Proc Natl Acad Sci U S A
; 109(45): 18281-9, 2012 Nov 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-22988103
3.
Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
J Med Chem
; 67(3): 1734-1746, 2024 Feb 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-38267212
4.
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
J Med Chem
; 67(3): 1747-1757, 2024 Feb 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-38230963
5.
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.
Bioorg Med Chem Lett
; 23(9): 2787-92, 2013 May 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23506825
6.
Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1.
J Med Chem
; 66(7): 4888-4909, 2023 04 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-36940470
7.
Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction.
Bioorg Med Chem Lett
; 22(24): 7605-9, 2012 Dec 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-23116892
8.
Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone.
Bioorg Med Chem Lett
; 21(12): 3557-62, 2011 Jun 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-21612924
9.
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).
J Med Chem
; 64(1): 644-661, 2021 01 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-33356246
10.
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
J Med Chem
; 63(21): 12725-12747, 2020 11 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-33054210
11.
Characterizing the effects of the juxtamembrane domain on vascular endothelial growth factor receptor-2 enzymatic activity, autophosphorylation, and inhibition by axitinib.
Biochemistry
; 48(29): 7019-31, 2009 Jul 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-19526984
12.
Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3.
Clin Cancer Res
; 14(22): 7272-83, 2008 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19010843
13.
Subtypes in patients with opioid misuse: A prognostic enrichment strategy using electronic health record data in hospitalized patients.
PLoS One
; 14(7): e0219717, 2019.
Artículo
en Inglés
| MEDLINE | ID: mdl-31310611
14.
Small molecule inhibitors reveal PTK6 kinase is not an oncogenic driver in breast cancers.
PLoS One
; 13(6): e0198374, 2018.
Artículo
en Inglés
| MEDLINE | ID: mdl-29879184
15.
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
J Med Chem
; 61(3): 650-665, 2018 02 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-29211475
16.
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors.
J Med Chem
; 50(22): 5253-6, 2007 Nov 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-17887663
17.
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
J Med Chem
; 60(7): 3002-3019, 2017 04 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-28287730
18.
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
J Med Chem
; 59(5): 2005-24, 2016 Mar 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-26756222
19.
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
J Med Chem
; 57(11): 4720-44, 2014 Jun 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-24819116
20.
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
J Med Chem
; 57(4): 1170-87, 2014 Feb 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-24432909