Table 4.
Phenotypic screening of R1 analogs in CML cell lines.
![]() | |||||
---|---|---|---|---|---|
Compound ID | R | R1 | IC50 AR230 (μm) | IC50 AR230R (μm) | LogP[a] |
RG1-066 | 3-pyridyl | c-Pent | >32 | >32 | 3.61 |
RG1-085 | 2-pyridyl | c-Pent | >32 | >32 | 3.61 |
AM1-116 | 4-fluoro-3-pyridyl | c-Pent | >32 | >32 | 3.74 |
AM1-117 | 4-fluoro-2-pyridyl | c-Pent | >32 | >32 | 3.74 |
AM1-020 | 2,3,5,6-tetrafluoro-phenyl | c-Pent | >32 | 13.1 | 4.28 |
AM1-112 | 4-chloro-2,3,5,6-tetrafluorophenyl | c-Pent | >32 | 30.7 | 4.6 |
AM1-077 | 4-bromo-2,3,5,6-tetrafluorophenyl | c-Pent | 25.07 | 20.3 | 4.74 |
AM1-066 | 4-trifluoromethyl-2,3,5,6-tetrafluorophenyl | c-Pent | 20.4 | 21.6 | 4.84 |
AM1-030 | 4-methyl-2,3,5,6-tetrafluorophenyl | c-Pent | >32 | 18.6 | 4.54 |
AES1-094 | 4-fluorophenyl | t-Bu | >32 | 10.6 | 1.96 |
Values calculated by StarDrop.