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. Author manuscript; available in PMC: 2011 Jun 7.
Published in final edited form as: J Med Chem. 2009 Dec 10;52(23):7580–7592. doi: 10.1021/jm900426g

Figure 2.

Figure 2

Functional agonism by the tested in an assay of adenylate cyclase in membranes of CHO cells expressing the hA3AR. Each experiment was repeated three times. (A) Activity of the 5′-N-methyluronamide (N)-methanocarba analogues 17a and 18. The EC50 values of 17a and 18 were 2.50 ±0.42 and 1.09 ±0.28 nM, respectively. (B) Activity of the truncated (N)-methanocarba analogues 2b and 2c at the hA3AR. The full agonist 51 was included for comparison (representing 100% efficacy). The percent relative efficacy of 2b and 2c was 46 ± 4% and 44 ± 6%, respectively. The EC50 values of 2b and 2c were 4.2± 0.6 and 12± 1 nM, respectively.