Table 1. Hit Profile of Pyrazine Sulfonamide 1.
biological assay/test procedure | compound 1 |
---|---|
hCCR4 binding (pIC50) | 7.2 ± 0.2 |
hPPB (%) | >99.9 |
calcd WBP (pIC50)a | <4.2 |
logD | 1.1 |
solubility (mg/mL) | 0.34 |
human hepatocytes (μL/mL/106 cells) | <0.2 |
rat/mouse in vivo PK | |
Cl (mL/min/kg) | 0.1/0.1 |
Vss (L/kg) | 0.1/0.1 |
T1/2 (h) | 16/10 |
bioavailability (%) | 45/86 |
rat/mouse CCR4 binding (pIC50) | 8.3/8.3 |
rat/mouse PPB (%) | 99.85/96.7 |
Calculated from the hCCR4 binding and % age PPB.