Johannes Brussee

Author PubWeight™ 22.33‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem 2008 1.87
2 New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine. J Med Chem 2004 1.12
3 Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action. J Med Chem 2005 1.02
4 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem 2004 1.02
5 Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands. Mol Cell Endocrinol 2012 0.97
6 Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor. J Med Chem 2006 0.94
7 False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase. J Med Chem 2008 0.91
8 Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics. J Biomol Screen 2012 0.90
9 Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. J Med Chem 2010 0.90
10 Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor. J Med Chem 2009 0.87
11 Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. J Med Chem 2013 0.87
12 A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. J Med Chem 2009 0.86
13 Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers. Bioorg Med Chem 2005 0.84
14 Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines. J Med Chem 2014 0.83
15 A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor. J Med Chem 2005 0.82
16 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem 2006 0.82
17 A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem 2008 0.81
18 Synthesis and biological evaluation of disubstituted N6-cyclopentyladenine analogues: the search for a neutral antagonist with high affinity for the adenosine A1 receptor. Bioorg Med Chem 2004 0.80
19 Understanding of molecular substructures that contribute to hERG K+ channel blockade: synthesis and biological evaluation of E-4031 analogues. ChemMedChem 2011 0.80
20 Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide. J Med Chem 2013 0.79
21 Binding kinetics of ZM241385 derivatives at the human adenosine A2A receptor. ChemMedChem 2014 0.79
22 Exploring chemical substructures essential for HERG k(+) channel blockade by synthesis and biological evaluation of dofetilide analogues. ChemMedChem 2009 0.79
23 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem 2007 0.78
24 Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues. J Med Chem 2013 0.77
25 Synthesis of L-altro-1-deoxynojirimycin, D-allo-1-deoxynojirimycin, and D-galacto-1-deoxynojirimycin from a single chiral cyanohydrin. Org Lett 2010 0.76
26 Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A). J Med Chem 2012 0.75
27 Designing active template molecules by combining computational de novo design and human chemist's expertise. J Med Chem 2007 0.75
28 Non-xanthine antagonists for the adenosine A1 receptor. Chem Biodivers 2004 0.75
29 Stereochemistry of intramolecular Diels-Alder furan (IMDAF) reactions of furyl-substituted chiral ethanolamides. Org Biomol Chem 2003 0.75
30 Multi-objective evolutionary design of adenosine receptor ligands. J Chem Inf Model 2012 0.75
31 Development of a process model to describe the synthesis of (R)-mandelonitrile by Prunus amygdalus hydroxynitrile lyase in an aqueous-organic biphasic reactor. Biotechnol Bioeng 2002 0.75