Table 3.
R1 | R2 | R3 | R4 | R5 | X | hkinact/Ki (M−1 s−1) | rkinact/Ki (M−1 s−1) | |
---|---|---|---|---|---|---|---|---|
19 | H | H | H | H | H | N | 695 | 174 |
6a | Me | H | H | H | H | N | 2401 | 1083 |
20 | Me | H | H | H | H | C | 5129 | 2613 |
21 | Et | H | H | H | H | N | 1402 | 774 |
22 | Et | H | H | H | H | C | 1668 | 1013 |
6b | Me | H | H | H | Me | N | 1481 | 390 |
23 | Cl | H | H | H | Me | N | 900 | 133 |
24 | Me | F | H | H | H | N | 3321 | 1203 |
25 | Me | F | H | H | H | C | 4147 | 1547 |
26 | Me | F | H | H | Me | N | 1980 | 758 |
27 | Me | H | F | H | H | N | 3134 | 779 |
13 | Me | H | F | H | H | C | 4474 | 729 |
28 | Me | H | Me | H | H | N | 2635 | 557 |
29 | Me | H | Me | H | H | C | 3024 | 482 |
30 | Me | H | Cl | H | H | N | 2822 | 1133 |
31 | Me | H | CF3 | H | H | N | 1389 | 219 |
32 | Me | H | OMe | H | H | N | 1381 | 500 |
33 | Et | H | F | H | H | N | 1808 | 617 |
34 | Et | H | F | H | H | C | 2292 | 1141 |
35 | Me | H | F | H | Me | N | 1871 | 260 |
36 | Me | H | Me | H | Me | N | 1169 | 183 |
37 | Me | H | H | OMe | H | N | 73 | 113 |
38 | Me | H | H | OEt | H | N | 14 | <10 |
39 | Cl | H | H | Me | Me | N | 73 | 14 |