Table 1 Physicochemical Properties of sCLU Enhancer Analogs
Compound | MW (Da) | Kinetic Solubility [μM] | Microsomal Stability [t1/2(min)] | Plasma Binding [% bound] | Brain Tissue Binding [% bound] | PAMPA [Pm] | EC50 for sCLU increase [nM] |
|---|---|---|---|---|---|---|---|
( + )-JQ1 | 456.99 | 86.5 | 27 | 85 | 87 | 1.44 | 313 |
DDL-351 | 469.00 | 57.5 | 3 | 99 | 94 | 1.35 | 117 |
DDL-352 | 453.99 | >100 | 62 | 96 | 64 | 0.98 | 1445 |
DDL-353 | 468.02 | >100 | 8 | 93 | 79 | 1.08 | 977 |
DDL-354 | 500.01 | 91.1 | 12 | 91 | 67 | 0.76 | 676 |
DDL-355 | 454.97 | 63.7 | 27 | 86 | 88 | 1.42 | 99 |
DDL-356 | 456.95 | >100 | 75 | 79 | 57 | 0.96 | 178 |
DDL-357 | 440.95 | 80.0 | 61 | 88 | 75 | 1.66 | 223 |
DDL-358 | 456.99 | 59.3 | 14 | 98 | 93 | 1.42 | 446 |
DDL-359 | 514.04 | >100 | 13 | 94 | 44 | 0.71 | 2344 |
DDL-360 | 415.90 | >100 | >120 | 88 | 59 | 1.09 | 631 |
