Table 2.
compd | R | X | Y | EC50 (nM) | EC90 (nM) | CC50 (nM) | therapeutic index | HLM (t1/2) (min) |
---|---|---|---|---|---|---|---|---|
2 | CN | H | O | 5 | 470 | >300 000 | >60 000 | 84.4 |
44 | CN | Br | O | 0.5 | 2.0 | >20 000 | >40 000 | 15 |
45 | CN | Cl | O | 0.7 | 1.3 | >20 000 | >28 571 | 16.8 |
46 | CN | F | O | >250 | >250 | 15 710 | >62 | 37.9 |
47 | CN | Br | SO2 | 3.1 | 10.4 | >20 000 | >6451 | 150.7 |
48 | SO2Me | Br | O | 8.3 | 18.2 | >20 000 | >2409 | 22.4 |
49 | CF3 | Br | O | 2.5 | 15.3 | >20 000 | >8000 | 3.6 |
51 | CH2OH | Br | O | 1.3 | 52.2 | >20 000 | >15 385 | 19.2 |
BMS-433771 | 34.5 | >2000 | >300 000 | >8695 | 64.2 | |||
JNJ-53718678 | 0.9 | 1.1 | 16 056 | 17 840 | 52.9 |