Table 1. . Thermostabilization and dissociation constants of carbazole-based Y220C binders.
 | |||||||
|---|---|---|---|---|---|---|---|
| Compound ID | R1† | DSF ΔTM [°C]‡ |
ITC KD [μM] | Compound ID | R1† | DSF ΔTM [°C]‡ |
ITC KD [μM] |
| PK083 | H | 1.0 ± 0.1 | 125 ± 10§ | PK9321 |  |
3.2 ± 0.1 | 5.6 ± 1.1¶ |
| PK9284 | Br | 3.0 ± 0.1 | 14.2 ± 2.0¶ | PK9322 |  |
3.0 ± 0.1 | 8.3 ± 2.6¶ |
| PK9295 |  |
1.3 ± 0.3 | 62 ± 6.5¶ | PK9323 |  |
3.4 ± 0.2 | 5.3 ± 1.4# |
| PK9296 |  |
1.9 ± 0.0 | - | PK9324 |  |
1.8 ± 0.1 | - |
| PK9304 |  |
-0.6 ± 0.0 | - | PK9326 |  |
0.8 ± 0.1 | - |
| PK9305 |  |
0.6 ± 0.0 | - | PK9331 |  |
1.7 ± 0.1 | - |
| PK9318 |  |
3.6 ± 0.2 | 2.6 ± 0.4# | PK9327 |  |
3.1 ± 0.2 | - |
| PK9319 |  |
0.5 ± 0.1 | - | PK9328 |  |
3.3 ± 0.0 | 1.7 ± 0.2# |
| PK9320 |  |
3.7 ± 0.0 | 4.1 ± 0.2# | PK9329 |  |
0.1 ± 0.0 | - |
†
All compounds were synthesized as the amine-hydrochloride salt to aid aqueous solubility.
‡
Measured at a compound concentration of 250 μM. Mean values of quadruplicate measurements are shown.
§
Value taken from reference [22].
¶
Single measurement with ITC fit error.
#
Mean value of at least three independent measurements with SEM.