Matches in SemOpenAlex for { <https://semopenalex.org/work/W2134161156> ?p ?o ?g. }
- W2134161156 endingPage "410" @default.
- W2134161156 startingPage "396" @default.
- W2134161156 abstract "Abstract The objective of the present study was to transfer the concept of library screening by MS binding assays, so far applied to pseudostatic hydrazine libraries, to static oxime libraries to screen for new potent inhibitors of mGAT1, the most abundant GABA transporter in the central nervous system that represents a validated drug target for the treatment of epilepsy. Library generation was performed by reaction of guvacine derivatives possessing a hydroxylamine functionality with various sets of four aldehydes. After dilution, the libraries were screened by competitive MS binding assays. Deconvolution experiments allowed hits in the most active libraries to be identified, and they were resynthesized for biological evaluation. That way a series of compounds was identified that displayed binding affinities ≥8.00 (p K i ) at mGAT1, one of which was found to be the most potent mGAT1 inhibitor known to date in a functional GABA uptake assay with a pIC 50 value of 8.27±0.03." @default.
- W2134161156 created "2016-06-24" @default.
- W2134161156 creator A5002115527 @default.
- W2134161156 creator A5039007961 @default.
- W2134161156 date "2014-11-04" @default.
- W2134161156 modified "2023-10-16" @default.
- W2134161156 title "Generation and Screening of Oxime Libraries Addressing the Neuronal GABA Transporter GAT1" @default.
- W2134161156 cites W1566384403 @default.
- W2134161156 cites W1576980256 @default.
- W2134161156 cites W1970124769 @default.
- W2134161156 cites W1978181170 @default.
- W2134161156 cites W1979276942 @default.
- W2134161156 cites W1985038609 @default.
- W2134161156 cites W1985637710 @default.
- W2134161156 cites W1991449748 @default.
- W2134161156 cites W1998667379 @default.
- W2134161156 cites W2002729353 @default.
- W2134161156 cites W2007164248 @default.
- W2134161156 cites W2007580188 @default.
- W2134161156 cites W2010621614 @default.
- W2134161156 cites W2011563038 @default.
- W2134161156 cites W2016499962 @default.
- W2134161156 cites W2022200746 @default.
- W2134161156 cites W2030857678 @default.
- W2134161156 cites W2034342600 @default.
- W2134161156 cites W2037671541 @default.
- W2134161156 cites W2039923977 @default.
- W2134161156 cites W2039991333 @default.
- W2134161156 cites W2040498799 @default.
- W2134161156 cites W2044470761 @default.
- W2134161156 cites W2044951200 @default.
- W2134161156 cites W2049190709 @default.
- W2134161156 cites W2049568654 @default.
- W2134161156 cites W2055611087 @default.
- W2134161156 cites W2057392629 @default.
- W2134161156 cites W2063792905 @default.
- W2134161156 cites W2073680518 @default.
- W2134161156 cites W2074631079 @default.
- W2134161156 cites W2074957611 @default.
- W2134161156 cites W2079613778 @default.
- W2134161156 cites W2084902496 @default.
- W2134161156 cites W2085387776 @default.
- W2134161156 cites W2085886216 @default.
- W2134161156 cites W2094916309 @default.
- W2134161156 cites W2115120433 @default.
- W2134161156 cites W2125655640 @default.
- W2134161156 cites W2126143811 @default.
- W2134161156 cites W2137976898 @default.
- W2134161156 cites W2157771225 @default.
- W2134161156 cites W2158381930 @default.
- W2134161156 cites W2167162307 @default.
- W2134161156 cites W2332091544 @default.
- W2134161156 cites W2896860430 @default.
- W2134161156 cites W4206270724 @default.
- W2134161156 cites W4242773223 @default.
- W2134161156 doi "https://doi.org/10.1002/cmdc.201402376" @default.
- W2134161156 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25369775" @default.
- W2134161156 hasPublicationYear "2014" @default.
- W2134161156 type Work @default.
- W2134161156 sameAs 2134161156 @default.
- W2134161156 citedByCount "28" @default.
- W2134161156 countsByYear W21341611562016 @default.
- W2134161156 countsByYear W21341611562017 @default.
- W2134161156 countsByYear W21341611562018 @default.
- W2134161156 countsByYear W21341611562019 @default.
- W2134161156 countsByYear W21341611562020 @default.
- W2134161156 countsByYear W21341611562021 @default.
- W2134161156 countsByYear W21341611562022 @default.
- W2134161156 countsByYear W21341611562023 @default.
- W2134161156 crossrefType "journal-article" @default.
- W2134161156 hasAuthorship W2134161156A5002115527 @default.
- W2134161156 hasAuthorship W2134161156A5039007961 @default.
- W2134161156 hasConcept C104317684 @default.
- W2134161156 hasConcept C149011108 @default.
- W2134161156 hasConcept C161624437 @default.
- W2134161156 hasConcept C185592680 @default.
- W2134161156 hasConcept C21951064 @default.
- W2134161156 hasConcept C2775999725 @default.
- W2134161156 hasConcept C2779046065 @default.
- W2134161156 hasConcept C2779057010 @default.
- W2134161156 hasConcept C2779648554 @default.
- W2134161156 hasConcept C55493867 @default.
- W2134161156 hasConcept C71240020 @default.
- W2134161156 hasConcept C86803240 @default.
- W2134161156 hasConcept C98274493 @default.
- W2134161156 hasConceptScore W2134161156C104317684 @default.
- W2134161156 hasConceptScore W2134161156C149011108 @default.
- W2134161156 hasConceptScore W2134161156C161624437 @default.
- W2134161156 hasConceptScore W2134161156C185592680 @default.
- W2134161156 hasConceptScore W2134161156C21951064 @default.
- W2134161156 hasConceptScore W2134161156C2775999725 @default.
- W2134161156 hasConceptScore W2134161156C2779046065 @default.
- W2134161156 hasConceptScore W2134161156C2779057010 @default.
- W2134161156 hasConceptScore W2134161156C2779648554 @default.
- W2134161156 hasConceptScore W2134161156C55493867 @default.
- W2134161156 hasConceptScore W2134161156C71240020 @default.
- W2134161156 hasConceptScore W2134161156C86803240 @default.
- W2134161156 hasConceptScore W2134161156C98274493 @default.