89951-56-4Relevant articles and documents
Selective Triazenation Reaction (STaR) of Secondary Amines for Tagging Monomethyl Lysine Post-Translational Modifications
Nwajiobi, Ogonna,Mahesh, Sriram,Streety, Xavier,Raj, Monika
supporting information, p. 7344 - 7352 (2021/03/01)
Lysine monomethylation (Kme) is an impactful post-translational modification (PTM) responsible for regulating biological processes and implicated in diseases, thus there is great interest in identifying these methylation marks globally. However, the progr
KINASE INHIBITORS
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Paragraph 0503; 0504, (2015/01/06)
Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract
New hits as antagonists of GPR103 identified by HTS
Nordqvist, Anneli,Kristensson, Lisbeth,Johansson, Kjell E.,Isaksson Da Silva, Krystle,Fex, Tomas,Tyrchan, Christian,Svensson Henriksson, Anette,Nilsson, Kristina
supporting information, p. 527 - 532 (2014/06/09)
Preclinical data indicate that GPR103 receptor and its endogenous neuropeptides QRFP26 and QRFP43 are involved in appetite regulation. A high throughput screening (HTS) for small molecule GPR103 antagonists was performed with the clinical goal to target weight management by modulation of appetite. A high hit rate from the HTS and initial low confirmation with respect to functional versus affinity data challenged us to revise the established screening cascade. To secure high quality data while increasing throughput, the binding assay was optimized on quality to run at single concentration. This strategy enabled evaluation of a larger fraction of chemical clusters and singletons delivering 17 new compound classes for GPR103 antagonism. Representative compounds from three clusters are presented. One of the identified clusters was further investigated, and an initial structure-activity relationship study is reported. The most potent compound identified had a pIC50 of 7.9 with an improved ligand lipophilic efficiency.