Potency data for probe MLi-2 and control MLi-2-NC
In vitro potency
| Target name | Target information | Species | Assay description | MLi-2 | MLi-2-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| LRRK2 | GST-tagged truncated human mutant G2019S LRRK2 | Homo sapiens | LRRK2 Biochemical Assay: LanthaScreen | IC50 = 1.8 nM | IC50 = 6480 nM | PMID: 26407721 |
| LRRK2 | GST-tagged truncated human mutant G2019S LRRK2 | Homo sapiens | LRRK2 Biochemical Assay with 5mM ATP: LanthaScreen | IC50 = 6.3 nM | PMID: 26407721 |
In cell potency
| Target name | Target information | Species | Assay description | MLi-2 | MLi-2-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| LRRK2 | LRRK2 G2019S SH-SY5Y human neuroblastoma cell line | Homo sapiens | Cellular assay monitoring dephosphorylation of pSer935 LRRK2 | IC50 = 3.5 nM | PMID: 26407721 | |
| LRRK2 | Homo sapiens | NanoBRET (LRRK2, SGC Frankfurt) | EC50 = 2.5 nM ± 0.130 nM (n=3) | EC50 > 50 µM (n=3) | ||
| MAP3K5 | Homo sapiens | NanoBRET (MAP3K5, SGC Frankfurt) | EC50 = 12 µM ± 3.100 µM (n=3) | EC50 = 4.1 µM ± 1.700 µM (n=3) | ||
| CLK4 | Homo sapiens | NanoBRET (CLK4, SGC Frankfurt) | EC50 = 24 µM ± 8.800 µM (n=3) | EC50 = 6.2 µM ± 1.200 µM (n=3) | ||
| CLK2 | Homo sapiens | NanoBRET (CLK2, SGC Frankfurt) | EC50 = 2 µM ± 0.630 µM (n=3) | EC50 = 11 µM ± 1.700 µM (n=3) | ||
| MAP3K14 | Homo sapiens | NanoBRET (MAP3K14, SGC Frankfurt) | EC50 > 50 µM (n=3) | EC50 > 50 µM (n=3) | ||
| TTK | Homo sapiens | NanoBRET (TTK, SGC Frankfurt) | EC50 > 50 µM (n=3) | EC50 > 50 µM (n=3) | ||
| LRRK2 | LRRK2 G2019S SH-SY5Y human neuroblastoma cell line | Homo sapiens | Cellular assay monitoring dephosphorylation of pSer935 LRRK2 | IC50 = 5439 nM |