Table 3. The ten fragments obtained from fragment screening that showed affinities better than 1 mM: structures, molecular weights, response levels from the initial fragment screening and respective KD values.
| Compound name | Structure | Molecular weight [Da] | SPR response a [%] | K D b [mM] |
| MB605 |
|
140.1 | 215 | 0.31 ± 0.04 |
| MB1261 |
|
134.1 | 95 | 0.35 ± 0.04 |
| MB1318 |
|
170.6 | 61 | 0.36 ± 0.04 |
| MB1082 |
|
146.2 | 53 | 0.37 ± 0.04 |
| MB417 |
|
180.2 | 87 | 0.42 ± 0.04 |
| MB895 |
|
157.2 | 53 | 0.43 ± 0.05 |
| AT0381 |
|
118.1 | 53 | 0.74 ± 0.06 |
| CA023 |
|
95.1 | 52 | 0.77 ± 0.06 |
| MB1284 |
|
149.2 | 90 | 0.86 ± 0.07 |
| MB1315 |
|
162.2 | 52 | 0.94 ± 0.09 |
aNormalised relative value against NK1.
bSteady-state binding constant from SPR.