Table 5. Viability of MM.1S Cells Treated with Compounds.
compound | R | X | Y | BRD4-D1 IC50 (μM)a | MM.1S EC50 (μM)b |
---|---|---|---|---|---|
22 | C(NH)NH2 | O | N | 9.7 ± 1.8 | >50 |
5 | C(NH)NH2 | O | CH | 3.6 ± 0.05, 1.7 ± 0.30c | >50 |
27 | C(NH)NH2 | NH | CH | 4.5 ± 0.35 | >50 |
28 | H | O | N | 11 ± 2.5 | 6.6 ± 1.9 |
29 | H | O | CH | 2.9 ± 0.07, 1.3 ± 0.25c | 2.9 ± 0.6 |
30 | H | NH | CH | 3.9 ± 0.35 | 6.3 ± 1.1 |
IC50 values were determined by fluorescence anisotropy. Data represents the mean and standard deviation of three independent trials.
Data reported are mean ± SEM of three biological replicates, with three technical replicates each. EC50 values were determined using the Nonlinear fit algorithm on GraphPad Prism.
IC50 values were determined by AlphaScreen by Reaction Biology.