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| Compound | K d a [nM] |
|---|---|
| Nilotinib (1) | 3.9 ± 0.3 |
| Nilotinib-SH (1a) | 881 ± 151 |
| Ponatinib (2) | 0.9 ± 0.5 |
| Ponatinib-SH (2a) | 0.6 ± 0.1 |
| Ponatinib-BT (2b) | 8.4 ± 2.3 |
| GZD824 (3) | 0.6 ± 0.3 |
| GZD824-SH (3a) | 0.9 ± 0.4 |
The determination of the dissociation constants (Kd) was performed with non-phosphorylated Abl1 kinase using the KdELECT assay (DiscoverX). The Kd values were calculated from quadruplicates.
