TABLE 3.
ELQ | Substituent at position: |
IC50 value (nM) or ratio fora: |
||||
---|---|---|---|---|---|---|
3 | 6 | 7 | Dd2 | C2B/Dd2 | D1/Dd2 | |
271 | DAEb | H | H | 12 | 2.8 | 0.2 |
298 | DAE | H | OCH3 | 5.5 | 0.7 | 0.8 |
314 | DAE | F | H | 33 | 1.3 | 3.4 |
316 | DAE | F | OCH3 | 3.1 | 1.1 | 3.6 |
296 | DAE | Cl | H | 29 | 0.9 | 16 |
300 | DAE | Cl | OCH3 | 6.6 | 0.7 | 24 |
339 | DAE | Br | H | 170 | 1.1 | 14 |
340 | DAE | Br | OCH3 | 25 | 0.4 | 65 |
IC50 values were averaged from ≥3 independent experiments run in triplicate. The standard deviations were <10%.
DAE, para-OCF3 diaryl ether side chain, as present in ELQ-300.