TABLE 4.
Cmpd | R | hATX IC50 [nM] | LogD (pH 7.4) | Solubility [µg/mL], pH 6.5 | Permeability Pe [10–6 * cm/s] | Mic CL h/m/r [µL/m/mg prot] | GSH adducts |
---|---|---|---|---|---|---|---|
11 | 1 | 2.3 | <1 | Na | 10/10/na | Neg | |
12 | 137 | 3.2 | 8 | 1.8 | 10/na/10 | Neg | |
13 | 6 | 3.2 | 28 | 4.5 | 10/10/10 | Neg | |
14 | 6 | 2.5 | 46 | 2.7 | 10/27/40 | Neg | |
15 | 8 | 2.0 | 190 | 0.4 | 10/10/na | Neg |
Na = not available.