Table 1.
Bfl-1 targeting agents and biochemical assays data.
| Compd ID | Sequences | DELFIA IC50 (nM)* | |
|---|---|---|---|
| hBfl-1 | hBcl-xL | ||
| hBIM-BH3 | Ac-IWIAQELRRIGDEFNAYYARR-CONH2 | 18 ± 2 | 5.0 ± 1 |
| 135P1 | Ac-λIAAALRRIGDAFNAAY-CONH2 | 3.0 ± 0.1 | 280 ± 180 |
| 138C5 | [NH-λIAE]ALRRIGDAFNAAY-CONH2 | 2.9 ± 0.1 | 1750 ± 500 |
| 138C7 | [NH-λI-Aib-E]ALRRIGDAFNAAY-CONH2 | 1.1 ± 0.1 | 1500 ± 200 |
| 138C8 | [NH-λI-Aib-E]-Aib-LRRIGD-Aib-FNA-Aib-Y-CONH2 | 3.1 ± 0.1 | >10 μM |
λ = L-Dap-2-chloroacetamide, Aib = 2-aminobutyric acid,
2 h incubation, see methods.