Table 2.
TAK1 affinity of current TAK1 inhibitors.
name | IC50 [nM] | PDB crystal structure | binding mode | reference |
---|---|---|---|---|
5Z-7-Oxozeaenol | 9 | 4GS6 | covalent | [60] |
hypothemycin | 100 | n.a. | covalent | [61] |
epoxyquinol | 20000 | n.a. | covalent | [62] |
AZ-TAK1 | 8 | unpublished | Type I | [63] |
ABC-FP | 28 | 4L53 | Type I | [64,65] |
PF-04358168 | 1640 | 2YIY | Type II | [66] |
PF-05381941 | 156 | N/A | Type II | [66] |
NG-25 | 4 | 4O91 | Type II | [67] |
LYTAK1 | N/A | n.a. | N/A | [68] |
takinib | 9.5 | 5V5N | Type 1.5 | [13] |