Potency data for probe SR-302 and control SR-301
In vitro potency
| Target name | Target information | Species | Assay description | SR-302 | SR-301 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| DDR1 | Homo sapiens | Enzyme kinetic assay (Reaction Biology) (DDR1): Compound tested in a 10-point dose response IC50 with 3-fold serial dilution starting at 10 µM as highest assay concentration. ATP concentration higher Km(ATP) was chosen. ATP conc. : 100 µM Control compound: Staurosporine (IC50 = 6.5 nM) | IC50 = 53.3 nM | |||
| DDR2 | Homo sapiens | Enzyme kinetic assay (Reaction Biology) (DDR2): Compound tested in a 10-point dose response IC50 with 3-fold serial dilution starting at 10 µM as highest assay concentration. ATP concentration higher Km(ATP) was chosen. ATP conc. : 5 µM Control compound: Staurosporine (IC50 = 0.38 nM) | IC50 = 0.75 nM | |||
| MAPK11 | Homo sapiens | Enzyme kinetic assay (Reaction Biology) (MAPK11): Compound tested in a 10-point dose response IC50 with 3-fold serial dilution starting at 10 µM as highest assay concentration. ATP concentration higher Km(ATP) was chosen. ATP conc. : 50 µM, Control compound: SB202190 (IC50 = 67.9 nM) | IC50 = 45.1 nM | |||
| MAPK14 | Homo sapiens | Enzyme kinetic assay (Reaction Biology) (MAPK14): Compound tested in a 10-point dose response IC50 with 3-fold serial dilution starting at 10 μM as highest assay concentration. ATP concentration higher Km(ATP) was chosen. ATP conc. : 2.5 µM Control compound: SB202190 (IC50 = 11.8 nM) | IC50 = 6.2 nM |
In cell potency
| Target name | Target information | Species | Assay description | SR-302 | SR-301 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| DDR1 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (DDR1) | IC50 = 23 nM ± 2.000 nM | IC50 = 21.9 µM ± 5.440 µM (n=3) | |
| DDR2 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (DDR2) | IC50 = 18 nM ± 2.000 nM | IC50 = 15.5 µM ± 5.080 µM (n=3) | |
| MAPK11 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (MAPK11) | IC50 = 196 nM ± 8.000 nM | IC50 = 1.63 µM | |
| MAPK14 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (MAPK14) | IC50 = 125 nM ± 11.000 nM | IC50 = 5.39 µM ± 3.100 µM (n=3) | |
| ABL1 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (ABL1) | IC50 > 25 µM | ||
| RIPK2 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (RIPK2) | IC50 > 25 µM | ||
| RPS6KA5 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (RPS6KA5) | IC50 > 25 µM | ||
| CHEK2 | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (CHEK2) | IC50 > 25 µM | ||
| BRAF | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (BRAF) | IC50 > 25 µM | ||
| STK38L | HEK293T cells; full-length | Homo sapiens | NanoBRET (SGC-Frankfurt) (STK38L) | IC50 > 25 µM |