In vitro affinity in binding to three subtypes of hARs of diverse heterocyclic derivatives identified through their high ranks in the <i>in silico</i> screen (structures are shown in Chart 2).
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aBinding in membranes of CHO (A1 and A3ARs) or HEK293 (A2AAR) cells stably expressing a hAR subtype. Total and nonspecific binding at the A1AR determined using [3H]DPCPX in the absence and presence of 10 µM CGS15943 (N-[9-chloro-2-(2-furanyl) [1], [2], [4]triazolo[1,5-c]quinazolin-5-amine), respectively. bECFP4 Tanimoto similarity for the most structurally similar known AR ligand (Table S3). *percent inhibition at 10 µM compound concentration. **n = 1.
创建时间：
2012-11-21
