Table 1. Elaboration of the quinazoline-carbocycle scaffold.
| Compound | R= | R′= | Kd (mM) WT HSC70-NBD | Kd (mM) S275W HSC70-NBDa | LEb |
|---|---|---|---|---|---|
| 27 | 3,4-dichlorophenyl | H | 0.85 (±0.26) | 5 | 0.14 |
| 28 | phenyl | H | 0.37 (±0.03) | No binding | 0.17 |
| 29 | phenyl | 4-cyanobenzyl | 2.0 (±0.0) | 2 | 0.10 |
| 30 | 2-pyridine | H | 0.075 (±0.13) | No binding | 0.20 |
SPR measurements on WT HSC70-NBD were carried out in triplicate. SPR Kd values are expressed as a mean ± standard deviation unless otherwise stated. aSingle measurement. bLigand efficiency is calculated using the SPR Kd.