Potency data for probe GNE-2256 and control GNE-6689
In vitro potency
| Target name | Target information | Species | Assay description | GNE-2256 | GNE-6689 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| IRAK4 | recombinant protein purified from insect cells | Homo sapiens | IRAK4 biochemical assay: Measured the fluorescence polarization of ADP2-antibody::TRACER complex formed | Ki = 1.4 nM ± 0.320 nM (n=30) | WO2017108723A2 |
In cell potency
| Target name | Target information | Species | Assay description | GNE-2256 | GNE-6689 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| IRAK4 | Homo sapiens | NanoBRET assay (IRAK4, SGC Frankfurt) | EC50 = 3 nM ± 0.300 nM (n=3) | EC50 = 9.5 µM ± 0.540 µM (n=3) | ||
| Homo sapiens | R848-induced IL-6 production in human whole blood | IC50 = 190 nM ± 79.000 nM (n=10) | PMID: 32184965 | |||
| Homo sapiens | IFNalpha human whole blood assay: Blood was stimulated with gardiquimod (5 µg/ml) for 4 hours. | IC50 = 290 nM | PMID: 32487715 | |||
| LRRK2 | Homo sapiens | NanoBRET assay (LRRK2, SGC Frankfurt) | EC50 = 5.2 µM ± 0.740 µM (n=3) | EC50 > 50 µM (n=3) | ||
| NTRK2 | Homo sapiens | NanoBRET assay (NTRK2, SGC Frankfurt) | EC50 = 5.6 µM ± 1.200 µM (n=3) | EC50 > 50 µM (n=3) | ||
| NTRK1 | Homo sapiens | NanoBRET assay (NTRK1v2, SGC Frankfurt) | EC50 = 11 µM ± 0.990 µM (n=3) | EC50 > 50 µM (n=3) | ||
| FLT3 | Homo sapiens | NanoBRET assay (FLT3, SGC Frankfurt) | EC50 > 50 µM (n=3) | EC50 = 3.6 µM ± 0.740 µM (n=3) | ||
| JAK1 | Homo sapiens | NanoBRET assay (JAK1, SGC Frankfurt) | EC50 > 50 µM (n=3) | EC50 > 50 µM (n=3) | ||
| JAK2 | Homo sapiens | NanoBRET assay (JAK2, SGC Frankfurt) | EC50 > 50 µM (n=3) | EC50 > 50 µM (n=3) |