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ADME parameters for CRFBP-CRF2 NAMs.
| Parameter | MLS-0046818 | MLS-0219419 |
|---|---|---|
| Plasma Stability at 1 h (rat) | 98.6% | 71.5% |
| Microsomal Stability at 1 h | 0.5% (rat), 6.6% (human) | 0.1% (rat), 0.1% (human) |
| Plasma Protein Binding (rat) | 4.6% free | 0.1% free |
| Brain Homogenate Binding (rat) | 2.3% free | 0.0% free |
| CYP3A4 Inhibition at 10 μM | 91% | 76% |
| CYP2C9 Inhibition at 10 μM | 86% | 102% |
| CYP1A2 Inhibition at 10 μM | 46% | 65% |
| CYP2D6 Inhibition at 10 μM | −21% | −128% |
| hERG Binding Inhibition at 10 μM | 48% | 86% |
