Table 1.
IC50 data for hits from the LYP/PTP-PEST screen in µM.
| Cmpd # | Phosphine | LYP (DiFMUP) |
LYP (peptide 1) |
PEST (DiFMUP) |
PEST (peptide 1) |
HePTP (DiFMUP) |
CD45 (DiFMUP) |
|---|---|---|---|---|---|---|---|
| 12 | P(Ph)2(m-SO3H-Ph) | 2.0±0.1 | 1.9±0.2 | 70±2 | 4.0±0.2 | 40±1 | > 70 |
| 13 | P(Me)2(Ph) | 3.5±0.3 | 2.0±0.3 | 70±2 | 30±2 | > 50 | > 100 |
| 17 | P(Ph)2(2-pyridine) | 5.0±0.2 | 1.5±0.3 | 76±3 | 43±3 | 35±2 | > 150 |
| 18 | P(p-SO3H-Ph)2(Ph) | 2.0±0.1 | 0.85±0.05 | 39±1 | 10±2 | 16±2 | 26±1 |
| 25 | P(cy)3 | 25±1 | 61±1 | 45±1 | > 80 | 20±2 | > 70 |
| 28 | P(EtCN)2(Ph) | 3.5±0.1 | 2.5±0.6 | > 80 | 33±1 | > 50 | > 70 |
| 34 | P(p-SO3H-Ph)3 | 1.5±0.1 | 0.75±0.15 | 15±1 | 3.2±0.2 | 13±3 | 23±1 |
| 39 | P(Et)3 | 33±3 | 26±2 | >150 | 93±9 | 120±5 | 33±3 |