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Doc ID CHEMBL1131846
Journal Bioorg. Med. Chem. Lett. (1999) 9:2413-2418
Title Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.
Authors Campbell RM, Cartwright C, Chen W, Chen Y, Duzic E, Fu JM, Loveland M, Manning R, McKibben B, Pleiman CM, Silverman L, Trueheart J, Webb DR, Wilkinson V, Witter DJ, Xie X, Castelhano AL.
Abstract Evaluation of a biased "library" of pyrrolo[2,3-d]pyrimidines using yeast-based functional assays expressing human A1- and A2a-adenosine receptors, led to the A1 selective antagonist 4b. A direct correlation between yeast functional activity and binding data was established. Practical compounds with polar residues at C-4 of the pyrrolopyrimidine system required H-bond donor functionality for high potency.
CiteXplore 10476879
DOI 10.1016/s0960-894x(99)00398-4

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