Table 1. Antagonistic and Spectroscopic Properties of RU486 and Its Fluorescent Derivatives.
IC50a | RBAb | log Pc | λexd | λemd | Φfl | |
---|---|---|---|---|---|---|
RU486 | 1.70 ± 0.24 | 1 | (4.72) | |||
RU486-BODIPY | 1.10 ± 0.22 | 1.5 | 3.51 ± 0.24 | 495 | 505 | 0.04–0.29 |
RU486-TAMRA | 7.55 ± 1.34 | 0.2 | 0.95 ± 0.14 | 550 | 578 | 0.04–0.08 |
Determined from dose–response curve of progesterone-induced alkaline phosphatase activity inhibition. Units are in nM.
Relative biological activity as determined by ratio of IC50(RU486) to IC50 of tested compound.
Measured using shake flask method. In parentheses: from DrugBank [DB00834].
Units are in nm.