Detalhe da pesquisa
1.
Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70.
Molecules
; 27(3)2022 Jan 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-35164081
2.
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.
Bioorg Med Chem
; 26(11): 3021-3029, 2018 07 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29764757
3.
Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy.
Br J Cancer
; 116(9): 1166-1176, 2017 Apr 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-28334731
4.
Scaffold-focused virtual screening: prospective application to the discovery of TTK inhibitors.
J Chem Inf Model
; 53(5): 1100-12, 2013 May 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-23672464
5.
Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.
Bioorg Med Chem
; 21(18): 5707-24, 2013 Sep 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23920481
6.
Benzimidazole inhibitors of the protein kinase CHK2: clarification of the binding mode by flexible side chain docking and protein-ligand crystallography.
Bioorg Med Chem
; 20(22): 6630-9, 2012 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23058106
7.
Analysis of water patterns in protein kinase binding sites.
Proteins
; 79(7): 2109-21, 2011 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-21557316
8.
Small molecule colorimetric probes for specific detection of human arylamine N-acetyltransferase 1, a potential breast cancer biomarker.
J Am Chem Soc
; 132(10): 3238-9, 2010 Mar 17.
Artigo
em Inglês
| MEDLINE | ID: mdl-20170182
9.
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases.
Bioorg Med Chem Lett
; 20(14): 4045-9, 2010 Jul 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20561787
10.
Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2.
Bioorg Med Chem
; 17(2): 905-18, 2009 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19059786
11.
High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers.
Mol Cancer Ther
; 18(10): 1696-1707, 2019 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-31575759
12.
Structure of HsaD, a steroid-degrading hydrolase, from Mycobacterium tuberculosis.
Acta Crystallogr Sect F Struct Biol Cryst Commun
; 64(Pt 1): 2-7, 2008 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18097091
13.
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
J Med Chem
; 61(18): 8226-8240, 2018 09 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-30199249
14.
Kinetic characterisation of arylamine N-acetyltransferase from Pseudomonas aeruginosa.
BMC Biochem
; 8: 3, 2007 Mar 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-17374145
15.
Expression, purification, characterization and structure of Pseudomonas aeruginosa arylamine N-acetyltransferase.
Biochem J
; 385(Pt 2): 605-12, 2005 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-15447630
16.
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.
J Med Chem
; 59(10): 4625-36, 2016 05 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-27119979
17.
A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.
Sci Rep
; 6: 34701, 2016 10 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-27708405
18.
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
J Med Chem
; 59(8): 3671-88, 2016 04 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-27055065
19.
Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
J Med Chem
; 59(11): 5221-37, 2016 06 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-27167172
20.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
J Med Chem
; 59(4): 1388-409, 2016 Feb 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-26741168