Compound | IC50 | Selectivity Ratio | ||||||
---|---|---|---|---|---|---|---|---|
AKR1C2 | AKR1C2 | AKR1C3 | COX-1 | COX-2 | AKR1C1 vs AKR1C2 | AKR1C1 vs AKR1C3 | AKR1C2 vs AKR1C3 | |
μM | ||||||||
9 | 14.0 ± 2.80 | 0.04 ± 0.00 | 1.02 ± 0.10 | ≫250 | ≫250 | 63 | 3.5 | 18 |
KI = 1.30 | KI = 0.021 | KI = 0.37 | ||||||
10 | 22.2 ± 2.50 | 0.05 ± 0.00 | 10.5 ± 2.70 | ≫1000 | ≫1000 | 483 | 1.2 | 578 |
KI = 8.30 | KI = 0.017 | KI = 10.0 | ||||||
11 | 9.20 ± 0.60 | 0.09 ± 0.00 | 1.57 ± 0.18 | ≫500 | ≫500 | 110 | 2.3 | 48 |
KI = 3.45 | KI = 0.032 | KI = 1.50 | ||||||
12 | 13.1 ± 1.10 | 0.03 ± 0.00 | 1.38 ± 0.13 | ≫1000 | N.D. | 450 | 3.7 | 120 |
KI = 4.90 | KI = 0.011 | KI = 1.30 | ||||||
13 | 177 ± 27.0 | 2.00 ± 0.30 | 216 ± 40.0 | ≫1000 | ≫1000 | 92 | 3.1 | 287 |
KI = 66.0 | KI = 0.72 | KI = 206 | ||||||
14 | 61.2 ± 5.90 | 0.56 ± 0.06 | 104 ± 19.0 | ≫1000 | ≫1000 | 114 | 4.3 | 493 |
KI = 23.0 | KI = 0.20 | KI = 9.0 | ||||||
15 | ≫100 | 2.50 ± 0.25 | > 100 | ≫250 | N.D. | 42 | 2.5 | 106 |
KI = 0.90 |
N.D., not determined.