Potency data for probe ERKi and control ERKi-NC
In vitro potency
| Target name | Target information | Species | Assay description | ERKi | ERKi-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MAPK1 | Homo sapiens | ERK Biochemical Assay | IC50 = 1.8 nM (n=7) | IC50 = 1780 nM | ||
| MAPK1 | Homo sapiens | Invitrogen kinase screen (MAPK1) | IC50 = 4 nM | |||
| GSK3A | Homo sapiens | Invitrogen kinase screen (GSK3A) | IC50 = 0.21 µM | |||
| SGK | Homo sapiens | Invitrogen kinase screen (SGK) | IC50 = 0.27 µM | |||
| GSK3B | Homo sapiens | Invitrogen kinase screen (GSK3B) | IC50 = 0.54 µM | |||
| GRK2 | Homo sapiens | Invitrogen kinase screen (GRK2) | IC50 = 0.59 µM | |||
| TBK1 | Homo sapiens | Invitrogen kinase screen (TBK1) | IC50 = 0.77 µM | |||
| CDK2 | Homo sapiens | Invitrogen kinase screen (CDK2) | IC50 = 0.79 µM | |||
| STK26 | Homo sapiens | Invitrogen kinase screen (STK26) | IC50 = 0.88 µM | |||
| CLK2 | Homo sapiens | Invitrogen kinase screen (CLK2) | IC50 = 0.94 µM | |||
| PRKG2 | Homo sapiens | Invitrogen kinase screen (PRKG2) | IC50 = 0.95 µM | |||
| CDK5 | Homo sapiens | Invitrogen kinase screen (CDK5) | IC50 = 1.2 µM | |||
| ROCK1 | Homo sapiens | Invitrogen kinase screen (ROCK1) | IC50 = 1.2 µM | |||
| ROCK2 | Homo sapiens | Invitrogen kinase screen (ROCK2) | IC50 = 1.4 µM | |||
| MARK2 | Homo sapiens | Invitrogen kinase screen (MARK2) | IC50 = 1.4 µM | |||
| GSK3A | Homo sapiens | NanoBRET (GSK3A, SGC Frankfurt) | EC50 = 13 µM ± 1.000 µM (n=3) | EC50 > 50 µM (n=3) |
In cell potency
| Target name | Target information | Species | Assay description | ERKi | ERKi-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MAPK1 | Homo sapiens | Cell Assay: Inhibition of RSK phosphorylation (pRSK A375SM) | IC50 = 280 nM (n=6) | IC50 > 10 µM | ||
| MAPK1 | Homo sapiens | Cell Assay: Inhibition of RSK phosphorylation (pRSK with 40% mouse serum ) | IC50 = 788 nM (n=6) | |||
| MAPK1 | Mus musculus | Cell Assay: Inhibition of RSK phosphorylation (pRSK with 40% human serum) | IC50 = 225 nM (n=6) | |||
| MAPK1 | Homo sapiens | Anti-Proliferation assay: A375SM | IC50 = 214 nM (n=4) | IC50 > 10 µM | ||
| MAPK1 | Homo sapiens | Anti-Proliferation assay: SK-MEL 30 | IC50 = 305 nM (n=6) | |||
| MAPK1 | Homo sapiens | Anti-Proliferation assay: Colo 205 | IC50 = 91 nM (n=6) | |||
| MAPK1 | Homo sapiens | Anti-Proliferation assay: Lovo | IC50 = 201 nM (n=6) | |||
| MAPK1 | Homo sapiens | NanoBRET (MAPK1, SGC Frankfurt) | EC50 = 95 nM ± 19.000 nM (n=3) | EC50 = 18 µM ± 2.700 µM (n=3) | ||
| MAPK3 | Homo sapiens | NanoBRET (MAPK3, SGC Frankfurt) | EC50 = 32 nM ± 11.000 nM (n=3) | EC50 = 6.7 µM ± 1.000 µM (n=3) | ||
| SGK1 | Homo sapiens | NanoBRET (SGK1, SGC Frankfurt) | EC50 > 50 µM (n=3) | EC50 > 50 µM (n=3) | ||
| GSK3B | Homo sapiens | NanoBRET (GSK3B, SGC Frankfurt) | EC50 = 5.2 µM ± 1.900 µM (n=3) | EC50 > 50 µM (n=3) | ||
| TBK1 | Homo sapiens | NanoBRET (TBK1, SGC Frankfurt) | EC50 = 22 µM ± 4.800 µM (n=3) | EC50 > 50 µM (n=3) | ||
| GRK2, PTK2B | Homo sapiens | NanoBRET (GRK2) | IC50 > 20 µM (n=3) |