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. 2022 Oct 7;65(21):14337–14347. doi: 10.1021/acs.jmedchem.2c00065

Table 6. Profiles of Hit Bicycle 10 Versus Partially Optimized Lead 45 and Final Optimized Bicycle 58.

      in vitro plasma stability (t 1/2, h)
 
Bicycle number affinity Ki (nM) solubility phosphate buffer pH 7.4 (mg/mL) mouse human CHIlogP
10 17.6 0.16 1.9 >24 4.07
45 8.9 0.50 >24 >24 2.12
58 2.8 4.6 >24 >24 1.50