Potency data for probe SR-318 and control SR-321
In vitro potency
| Target name | Target information | Species | Assay description | Compound conc. | SR-318 | SR-321 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| MAPK14 | Homo sapiens | Radiometric activity assay, ProQinase (MAPK14) | IC50 = 5 nM | PMID: 31702918 | |||
| MAPK11 | Homo sapiens | Radiometric activity assay, ProQinase (MAPK11) | IC50 = 32 nM | PMID: 31702918 | |||
| MAPK14 | Homo sapiens | Binding based DSF (Differencial Scanning Fluorimetry) assay | 10 µM | deltaTm = 15.4 °C ± 0.400 °C (n=4) | PMID: 31702918 |
In cell potency
| Target name | Target information | Species | Assay description | Compound conc. | SR-318 | SR-321 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| MAPK14, MAPK14 | HEK cells; full length | Homo sapiens | NanoBRET (MAPK14) | IC50 = 3.7 nM ± 0.200 nM (n=2) | IC50 = 13 µM ± 3.900 µM (n=2) | PMID: 31702918 | |
| MAPK11, MAPK11 | HEK cells | Homo sapiens | NanoBRET (MAPK11) | IC50 = 10 nM ± 2.300 nM (n=2) | IC50 = 11 µM ± 3.300 µM (n=2) | PMID: 31702918 | |
| HSPB1 | Homo sapiens | Inhibition of HSP27 (Ser82) (Western blot) | IC50 < 1 µM | ||||
| TNF | Homo sapiens | TNF-α release ( LPS stim., WB) | 10 µM | IC50 = 283 nM | PMID: 28834431 | ||
| DDR1 | Homo sapiens | NanoBRET (DDR1) | IC50 = 3 µM | IC50 = 13 µM ± 3.200 µM (n=2) | PMID: 31702918 | ||
| DDR2 | Homo sapiens | NanoBRET (DDR2) | IC50 = 5.6 µM ± 1.700 µM (n=2) | IC50 = 0.22 µM | PMID: 31702918 | ||
| KIT | Homo sapiens | NanoBRET (KIT) | IC50 = 8.5 µM | IC50 > 20 µM | PMID: 31702918 | ||
| MAP3K20 | Homo sapiens | NanoBRET (MAP3K20) | IC50 = 0.91 µM | IC50 = 5.8 µM | PMID: 31702918 | ||
| RPS6KA6 | Homo sapiens | NanoBRET (RPS6KA6) | IC50 = 14 µM | IC50 > 20 µM | PMID: 31702918 | ||
| MYLK4 | Homo sapiens | NanoBRET (MYLK4) | IC50 = 10 µM | IC50 > 20 µM | PMID: 31702918 |