Potency data for probe SM311 and control SM311-NC
In vitro potency
| Target name | Target information | Species | Assay description | SM311 | SM311-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|
| LIMK1 | Homo sapiens | TR-FRET assay (LIMK1, KIapp) | KIapp = 40.71 nM | |||
| LIMK1 | Homo sapiens | TR-FRET assay (LIMK1, kinact/KIapp) | kinact/KIapp = 69516 M-1s-1 |
In cell potency
| Target name | Target information | Species | Assay description | Compound conc. | SM311 | SM311-NC | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| LIMK1 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (LIMK1) | EC50 = 45 nM | EC50 > 25 µM | ||
| LIMK2 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (LIMK2) | EC50 = 6.74 µM | |||
| CDKL2 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (CDKL2) | EC50 = 1.5 µM | |||
| AAK1 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (AAK1) | EC50 = 10.4 µM | |||
| MAPK8 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (MAPK8) | EC50 = 23 µM | |||
| MAPK9 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (MAPK9) | EC50 = 14.3 µM | |||
| MAPK10 | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (MAPK10) | EC50 = 25.5 µM | |||
| STK32B | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (STK32B) | EC50 = 31 µM | |||
| SRC | HEK293 cells | Homo sapiens | NanoBRET Target Engagement (SRC) | EC50 > 50 µM | |||
| LIMK1 | HEK293 cells | Homo sapiens | NanoBRET K192 (LIMK1): Tracer displacement assay | 1 µM | Occupancy = 91% | ||
| CDKL2 | HEK293 cells | Homo sapiens | NanoBRET K192 (CDKL2): Tracer displacement assay | 1 µM | Occupancy = 85% | ||
| NLK | HEK293 cells | Homo sapiens | NanoBRET K192 (NLK): Tracer displacement assay | 1 µM | Occupancy = 73% | ||
| TXK | HEK293 cells | Homo sapiens | NanoBRET K192 (TXK): Tracer displacement assay | 1 µM | Occupancy = 73% | ||
| AAK1 | HEK293 cells | Homo sapiens | NanoBRET K192 (AAK1): Tracer displacement assay | 1 µM | Occupancy = 66% | ||
| MAPK9 | HEK293 cells | Homo sapiens | NanoBRET K192 (MAPK9): Tracer displacement assay | 1 µM | Occupancy = 65% |