Table 2.
Assessment of key ADME properties of G28, CHI3L1-IN-1, K284, and G721–0282.
| Compound | Kinetic Solubility 1% DMSO/PBS [μM]a | PAMPA permeability (cm/s) | LogD7.4b | IC50 against hERG [μM] | PPB human [%] |
|---|---|---|---|---|---|
| G28 | 251 | 7.1 × 10−6 | 1.8 | >100 | 79.5 |
| CHI3L1-IN-1 | 53 | 2.2 × 10−6 | 2.7 | 16 ± 2.5 | 96.1 |
| K284 | 89 | 3.1 × 10−6 | 2.1 | 22 ± 3.1 | 91.5 |
| G721–0282 | 12 | 1.5 × 10−6 | 3.3 | 5.3 ± 0.8 | 98.3 |
a
Kinetic solubility measured in 1% DMSO/PBS (pH 7.4) by UV−vis spectrophotometry (n=3).
b
LogD (pH = 7.4) the distribution coefficient at physiological pH 7.4.