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Permeability and microsomal stability data on Leu-to-Ser substitutions in compound 3.
| ||||||||
|---|---|---|---|---|---|---|---|---|
| cpd | R1 | R3 | R4 | PAMPA (%T) | RRCK pH 7.4 (× 106cm/s) | HLM Clint (μg/min/mg) | RLM Clint (μg/min/mg) | Human plasma stab (t1/2, min) |
| 3 L1S | −OH | i-Pr | i-Pr | < 0.08 | 1.9 | 54 | 98 | > 360 |
| 3 L3S | i-Pr | −OH | i-Pr | < 0.08 | 1.6 | 85 | 53 | > 360 |
| 3 L4S | i-Pr | i-Pr | −OH | < 0.08 | 0.76 | 271 | 507 | >360 |
