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The ActiTarg-G Collection is a plated screening set of molecules that contain chemical lattices present in compounds reported in the technical or patent literature to possess GPCR-ligand properties. From our collection of over 7000 compounds in more than 15 different chemical series we have assembled a pre-filtered diversity collection of 2300 compounds that should provide a high value screening library of drug-like molecules for identifying synthesis direction for the development of new GPCR ligands. Structural constraints and novel pendants within these lattices provide the structural variability to identify new chemical directions for hit optimization.
Compounds are available for cherry-picking and/or as a collection in 96, 384-well plates and in vials.
Contact us for structural info, formatting options and pricing. About GPCR Ligands
G-protein coupled receptors are a ubiquitous super family of proteins with hundreds of members having been identified and cloned. These receptors generally have a seven-membrane spanning alpha-helical topography, and while these receptors are similar in overall structure and function, they differ in key amino acid residues. The potential for this super family of receptors to reveal small molecule modulators of a significant biological function has been responsible the focus of intense drug discovery efforts.
Compounds with structural features and molecular lattices that are present in a large number molecules described in both the patent and technical literature that possess GPCR activity have been identified, and assembled as indicated below. | GPCR | Lattice type | | Contact us if you are interested in a chemical diversity selection of structures from the different GPCR libraries assembled as 5, 10 and 20 plate sets | | CRF / NPY | Ar-X-Ar | | CRF | 4-Ar-2-aminothiazole | | 5HT
5HT | Indolines
gamma-Carbolines | | 5HT | 5-Substituted indoles | | 5HT | 4-ArylpiperazinesNH | | 5HT | Aminoethylbenzamides | | 5HT | Aminopropylbenzamides | | BDZ-like | Fused 6,7 ring systems | | Various | Spiro systems | | Various | Aryl/Heteroarylpiperazines | | Various | Benzylpiperazines | | Various | 4-Aryl/heteroarylpiperidines | | Various | 4-OH-4Phe-piperidines | | Various | Tetrahydroisoquinolines | | Chemokine | Diarylureas | Lefkowitz RJ: Seven transmembrane receptors: something old, something new. Acta Physiol (oxf) 2007;190:9-19 Lander ES, Linton LM, Birren B, Nusbaum C, Zody MC, Baldwin J, et al: Initial Sequencing and analysis of the human genome. Nature 2001;409:860-921 Venter JC, Adams MD, Myers EQ, Li PW, Mural RJ, Sutton GG, et al: The sequence of the human genome. Science 2001;291:1304-1354 Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov 2006;5:993-996 Xiao SH, Reagan JD, Lee PH, Fu A, Schwandner R, Zhao X, et al: High throughput screening for orphan and liganded GPCRs. Comb Chem High Throughput Screen 2008;11:195-215
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