Potency data for probe TP-008 and control Al11
In vitro potency
| Target name | Target information | Species | Assay description | TP-008 | Al11 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| ACVR1B | Homo sapiens | Lathascreen (Takeda) (ACVR1B) | pIC50 = 6 | |||
| TGFBR1 | Homo sapiens | Lathascreen (Takeda) (TGFBR1) | pIC50 = 7.6 | PMID: 27460209 | ||
| TGFBR1 | Homo sapiens | Enzyme kinetic assays | IC50 = 25 nM | |||
| ACVR1B | Homo sapiens | Radioactive kinase assay (ACVR1B) | pIC50 = 6.9 | |||
| TGFBR1 | Homo sapiens | Radioactive kinase assay (TGFBR1) | pIC50 = 6.5 |
In cell potency
| Target name | Target information | Species | Assay description | TP-008 | Al11 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| ACVR1B | HEK293 cells | Homo sapiens | Reporter gene assay (ACVR1B): Dual Luciferase Assay (10ng/ml TGF-beta) with CAGA promoter, Stimulation with Activin A | IC50 = 526 nM ± 96.000 nM | ||
| TGFBR1 | HEK293 cells | Homo sapiens | Reporter gene assay (TGFBR1): Dual Luciferase Assay (10ng/ml TGF-beta) with CAGA promoter | IC50 = 245 nM ± 41.000 nM | ||
| MAPK9 | Homo sapiens | NanoBRET (SGC Frankfurt) (MAPK9) | IC50 > 20 µM | |||
| JAK1 | Homo sapiens | NanoBRET (SGC Frankfurt) (JAK1) | IC50 > 20 µM | |||
| PIK3CA | Homo sapiens | NanoBRET (SGC Frankfurt) (PIK3CA) | IC50 > 20 µM | |||
| PNCK | Homo sapiens | NanoBRET (SGC Frankfurt) (PNCK) | IC50 > 20 µM | |||
| DDR1 | Homo sapiens | NanoBRET (SGC Frankfurt) (DDR1) | IC50 > 20 µM | |||
| ACVR1B | Homo sapiens | NanoBRET (SGC Frankfurt) (ACVR1B) | IC50 > 10 µM | |||
| TGFBR1 | Homo sapiens | NanoBRET (SGC Frankfurt) (TGFBR1) | IC50 > 10 µM |