Table 4.
New Inhibitors Synthesized and Assayed as a Result of Predictiona
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---|---|---|---|---|---|
Comp’d | Predicted Log[PDE4D IC50] | Experimental Log[PDE4D IC50] | PDE4D* | PDE4B* | Selectivity |
IC50 (nM) | IC50 (nM) | B/D | |||
48 | 1.62 | 1.11 | 13 | 2130 | 165 |
49 | 0.59 | 0.26 | 1.8 | 665 | 364 |
50 | −0.39 | −0.44 | 0.36 | 91 | 254 |
51 | −0.90 | −0.52 | 0.30 | 81 | 270 |
52 | 0.11 | 0.57 | 3.7 | 198 | 54 |
See Table 1 for assay definitions.