774214-05-0Relevant articles and documents
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4)inhibitors, compound profiling in cell-based target engagement assays
Le Bihan, Yann-Va?,Lanigan, Rachel M.,Atrash, Butrus,McLaughlin, Mark G.,Velupillai, Srikannathasan,Malcolm, Andrew G.,England, Katherine S.,Ruda, Gian Filippo,Mok, N. Yi,Tumber, Anthony,Tomlin, Kathy,Saville, Harry,Shehu, Erald,McAndrew, Craig,Carmichael, LeAnne,Bennett, James M.,Jeganathan, Fiona,Eve, Paul,Donovan, Adam,Hayes, Angela,Wood, Francesca,Raynaud, Florence I.,Fedorov, Oleg,Brennan, Paul E.,Burke, Rosemary,van Montfort, Rob L.M.,Rossanese, Olivia W.,Blagg, Julian,Bavetsias, Vassilios
supporting information, p. 316 - 337 (2019/06/05)
Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between
Water-soluble phosphinothiol reagents
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, (2013/04/13)
Water soluble reagents and methods for the formation of an amide bond between a phosphinothioester and an azide in an aqueous medium. The phosphinothioester is generated using a water-soluble phosphinothiol reagent. This reaction allows formation of an amide bond between a wide variety of chemical species including amino acids, peptides or protein fragments in an aqueous solution. Of particular interest, this reaction allows for the formation of an amide bond in a physiological setting. In a specific embodiment, this invention provides reagents and methods for peptide ligation in an aqueous medium. The reaction eliminates the need for a cysteine residue and is traceless leaving no residual atoms in the ligated peptide product.
Coulombic effects on the traceless Staudinger ligation in water
Tam, Annie,Raines, Ronald T.
experimental part, p. 1055 - 1063 (2009/09/06)
The traceless Staudinger ligation can be mediated by phosphinothiols under physiological conditions. Proximal positive charges are necessary to achieve that transformation, presumably because those charges discourage protonation of the key iminophosphoran
Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments
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Page/Page column 35; 36, (2008/12/06)
The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I) wherein K-L-M-N, Z and R1, R2, R3, R4 are described in the claims, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatments of humans or animals.
Combination of a 5-HT7 receptor ligand and an opioid receptor ligand
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Page/Page column 29, (2009/01/20)
The present invention refers to a combination of a 5HT7 receptor ligand and an opioid recptor ligand, especially of a 5HT7 receptor agonist and an opioid recptor agonist, a medicament comprising this combination, or the use of this combination for the treatment of the symptoms of pain, the prevention or the prophylaxis of the symptoms of pain.
Structure-activity correlations for β-phenethylamines at human trace amine receptor 1
Lewin, Anita H.,Navarro, Hernan A.,Wayne Mascarella
, p. 7415 - 7423 (2008/12/22)
A cell line in which RD-HGA16 cells were stably transfected with the hTAAR 1 receptor was created and utilized to carry out a systematic evaluation of a series of β-phenethylamines. Fair agreement was observed with data obtained for aryl and ethylene chain substituted analogs in an AV12-664 cell line in which hemagglutinin-tagged hTAAR 1 was stably co-expressed with rat Gαs. Analogs with multiple substituents as well as analogs with bulky groups were found to be partial agonists. Analogs in which the primary amino group was converted to a secondary or a tertiary amino group by N-methylation were also partial agonists. Comparative Molecular Field Analysis (CoMFA) using the potency data yielded a regression coefficient r2 of 0.824. The steric field contribution to the model was 61% with the balance (39%) contributed by the electrostatic field. The collective results suggest that increasing steric bulk both at the amino nitrogen, particularly by N-dimethylation, and at the 4-position of the aromatic ring leads to low efficacy ligands.
Novel aminoethylbiphenyls as 5-HT7 receptor ligands
Paillet-Loilier, Magalie,Fabis, Frederic,Lepailleur, Alban,Bureau, Ronan,Butt-Gueulle, Sabrina,Dauphin, Francois,Lesnard, Aurelien,Delarue, Catherine,Vaudry, Hubert,Rault, Sylvain
, p. 3018 - 3022 (2008/02/07)
The synthesis of a series of aminoethylbiphenyls as novel 5-HT7 receptor ligands is described. The novel derivatives exhibit high affinity for the 5-HT7 receptor with selectivity toward 5-HT1A receptor.