Table 1.
| ||||
---|---|---|---|---|
IC50(nM)a | ||||
Compd | R | Human | Murine | logP (±0.5)b |
2 | 2.8 | 1.2 | 3.1 | |
3 | 3.9 | 0.9 | 2.3 | |
4 | 12 | 3.5 | 1.8 | |
5 | 3.2 | 0.4 | 3.5 | |
6 | 2.7 | 7.4 | 1.8 | |
7 | 130 | 49 | 1.3 | |
8 | 3.0 | 4.2 | 2.4 | |
9 | 3,800 | >5,000 | ndc |
IC50 values were determined with a fluorescent assay using homogenous recombinant murine and human enzymes (see methods).
Confidence refers to logP value. See supplementary material for full explaination.
The HPLC method used is limited to logP values greater than zero.