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Assessment of brain permeability, tissue binding and partitioning of TP compounds.
| Compound ID | BTB (%) | MDR1-MDCK | Efflux Ratio | B/P Ratio | ||
|---|---|---|---|---|---|---|
| A–B | B–A | B–A/A–B | 5 min | 60 min | ||
| GNF3849 | >99 | 4.5 | 14.1 | 3.2 | 0.22 | 0.28 |
| GNF6702 | 94.7 | 8.3 | 22.1 | 2.7 | 0.13 | 0.17 |
| NITD689 | 96.5 | 32.6 | 29.2 | 0.9 | 0.12 | 0.12 |
Note: BTB: rat brain tissue binding; MDR1-MDCK = Multi Drug Resistant 1 overexpressing Madin–Darby canine kidney cells; A–B = Apical to Basolateral; B–A = Basolateral to Apical; B/P ratio = brain-to-plasma ratio.
