Compound inhibition in the NanoBRET target engagement assay against Abl1 and Ba/F3 Abl, Ba/F3 T315I Abl, and K562 cell lines. IC50 is the concentration at which 50% inhibition is observed, GI50 is the concentration at which 50% inhibition of cell growth is observed, SD is the standard deviation of the mean values.
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| Cmpd. | ABL1 WT | Ba/F3 ABL | Ba/F3 AblT315I | K562 | Cmpd. | ABL1 WT | Ba/F3 ABL | Ba/F3 ABLT315I | K562 | |
| IC50 ± SD (nM) | GI50 ± SD (nM) | GI50 ± SD (nM) | GI50 ± SD (nM) | IC50 ± SD (nM) | GI50 ± SD (nM) | GI50 ± SD (nM) | GI50 ± SD (nM) | |||
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1 (h1–t1) | 15.7 ± 0.3 | 83 ± 63 | 117 ± 64 | 2.3 ± 1.6 | 2 (h1–t2) | 64.7 ± 4.2 | 66 ± 34 | 269 ± 112 | 4 ± 2.5 |
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3 (h2–t1) | 38.3 ± 11.5 | 36 ± 15 | 162 ± 79 | 6.9 ± 1.5 | 4 (h2–t2) | 345 ± 109 | 164 ± 138 | 801 ± 419 | 13 ± 3 |
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5 (h3–t1) | 637 ± 72 | >10 000 | >10 000 | 451 ± 6 | 6 (h3–t2) | 719 ± 43 | >5000 | >10 000 | 239 ± 53 |