Table 3.
Comparison of assay results for compounds 4–6
| Compound | Binding site | SPR K d (mM) | MSA IC50 (mM) | FLT IC50 (mM) | MST K d (mM) |
|---|---|---|---|---|---|
| 4 | ATP | 0.78 | 0.41 | 0.52 | 0.89 |
| 5 | ATP | 1.59 | 2.6 | n.a.b | 1.15 |
| 6 | Distal site | 1.38 | 3.24 | n.a. | >0.3a |
| Neg. control | – | TRmax 25.4% (0.2 mM) | 2.2% inh. (1 mM) | Not tested | >2 |
aConcentration dependent binding for compound 6 has been detected by MST, but the K d could not be exactly determined due to a high Hill slope; an estimated K d for 6 is within the range of those determined for compounds 4 and 5
bDose response curves were started at 1.5 mM maximal concentration and IC50 values are not applicable