Table 2.
Solubility data for selected [b]-annulated indoles.
Compound | Sexp., therm., pH 7.4 [µM] a | Sexp., kin., pH 7.4 [µM] b |
---|---|---|
KuFal194 (10) | <5 | 5.28 (4.99–5.57) |
11 | <5 | 26.1 (25.6–26.5) |
16 | 13,650 (11,100–16,200) | 2310 * |
a Thermodynamic solubility (phosphate buffer pH 7.4) using the shake-flask method. In two independent experiments vials were incubated at 25 °C and quantified by HPLC. Signals lower than the limit of quantification are indicated as <5 µM (lowest concentration used for calibration). Mean value and range are given. b Kinetic solubility using nephelometry. Mean value and range are given. * Singlicate measurement.