Table 1.
Comp. | TPSA | LogP /LogD | Phospho-Tyr | PTPRZ1 inhibition at 1.0 μM |
---|---|---|---|---|
1 | 94.27 | 5.35 | X | - |
4a | 79.70 | 7.26 | √ | X |
4b | 79.70 | 7.37 | √ | X |
4c | 79.70 | 6.99 | √ | √ |
4d | 79.70 | 6.88 | √ | √ |
5a | 114.14 | 4.88 | X | - |
5b | 114.14 | 5.00 | √ | √ |
5c | 114.14 | 4.62 | √ | X |
10a | 59.83 | 7.73 | √ | √ |
10b | 51.75 | 6.54 | X | - |
10c | 47.42 | 4.34 | √ | X |
12a | 62.63 | 7.55 | √ | X |
12b | 62.63 | 7.50/6.64 | √ | √ |
12c | 41.91 | 5.43/4.41 | X | |
12d | 37.33 | 5.48 | √ | √ |
12e | 37.33 | 5.99 | X | |
13 | 79.14 | 11.72/11.56 | √ | X |