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. Author manuscript; available in PMC: 2020 Jul 1.
Published in final edited form as: Bioorg Med Chem. 2019 May 9;27(13):2972–2977. doi: 10.1016/j.bmc.2019.05.009

Table 1:

Binding constants measured by SPR for compounds binding the HIV-1 FSS. Binding constants represent the average of the constants obtained from individually fitting four SPR curves, at two different concentrations. Competition binding experiments with tRNA were conducted with HIV-1 FSS on-chip and a 5 fold excess (relative to compound) concentration of tRNA in solution. All dissociation constants KD are reported ± standard error.

Compound cLogP ka
(1/M·s)		 kd (1/s) KD for FSS RNA
(nM)		 KD with tRNA Competition
(nM)
3 2.63 1.9*105 3.0*10−3 16 ± 2 130 ± 10
4 0.31 6.49*104 2.37*10−2 497 ± 157 132 ± 34.5
5 −1.52 1.49*104 6.80*10−3 583 ± 202 441 ± 121
6 −1.6 5.66*104 2.26*10−3 62.2 ± 21.3 124 ± 37.4
7 −3.44 6.74*104 5.42*10−3 110 ± 34.2 183 ± 32.5
8 3.94 1.69*103 2.07*10−2 19,300 ± 5,170 16,800 ± 7,020
9 2.11 ND ND ND ND
10 0.19 4.09*103 5.41*10−3 1,470 ± 237 ND
11 2.02 ND ND ND ND