Table 3.
Phenotypic screening of R1 analogs in CML cell lines.
| |||||
|---|---|---|---|---|---|
| Compound ID | R1 | IC50 AR230 (μm) | IC50 AR230R (μm) | Fold Difference | LogP[a] |
| PSL-3-115 | H | 5.2 | 2.3 | 2.26 | 3.39 |
| PSL-3-122 | F | 6.1 | 3 | 2.03 | 3.36 |
| DR-4-003 | Cl | 4.1 | 1.7 | 2.41 | 3.68 |
| DR-3-186 | CF3 | 1.4 | 0.72 | 1.94 | 3.95 |
| PSL-3-132 | c-Pr | 4.2 | 2.4 | 1.75 | 3.86 |
| DR-4-020 | c-Bu | 8.6 | 4.2 | 2.05 | 4.05 |
| DR-3-162 | t-Bu | 3.2 | 0.8 | 4 | 4.24 |
| DR-3-093 | c-Pent | 3.3 | 1.2 | 2.75 | 4.23 |
| DR-3-165 | c-Hept | 2.7 | 1.1 | 2.45 | 4.8 |
| DR-3-119 |
|
5.8 | 3.2 | 1.81 | 4.84 |
| PSL-3-089 |
|
7.4 | 5.2 | 1.42 | 3.29 |
| DR-4-042 |
|
4.7 | 4.2 | 1.12 | 3.29 |
Values calculated by StarDrop.