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| compound | R | pAKT AlphaLISA IC50 (nM)a | Clint human hepatocytes (mL/min/kg)b | |
|---|---|---|---|---|
| T47D | SKBR3 | |||
| 7 | –H | 78 | 5894 | 181 |
| 8 | –Me | 3 | 1465 | 340 |
| 11 | –F | 0.3 | >10,000 | 862 |
| 12 | –CN | 1 | 4739 | 79 |
| 13 | –CF3 | 28 | >10,000 | N.D. |
| 14 | –CONH2 | >10,000 | >10,000 | N.D. |
Measured inhibition of pAKT formation using alphaLISA after 24 h of treatment.
Intrinsic clearance obtained from scaling in vitro half-lives from pooled hepatocytes.
