Potency data for probe BI-3231 and control BI-0955
In vitro potency
| Target name | Target information | Species | Assay description | Compound conc. | BI-3231 | BI-0955 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| HSD17B13 | recombinant protein expressed in HEK293 cells with C-terminal Histidine-tag; full length human | Homo sapiens | Enzymatic assay (hHSD17B13): Assay for High-Throughput Screening via MALDI-TOF MS | Ki = 0.7 nM ± 0.200 nM (n=3) | Ki > 10 µM (n=3) | PMID: 36727857 (Compound 45) | |
| HSD17B13 | recombinant protein expressed in HEK293 cells with C-terminal Histidine-tag; full length human | Homo sapiens | nanoDSF (HSD17B13): HSD17B13 (10 μM) was preincubated with NAD+ | 10 µM | delta T = 16.7 K | PMID: 36727857 (Compound 45) | |
| HSD17B13 | recombinant protein expressed in HEK293 cells with C-terminal Histidine-tag; full length mouse | Mus musculus | Enzymatic assay (mHSD17B13) | Ki = 0.5 nM ± 0.100 nM (n=3) | Ki > 10 µM (n=3) | PMID: 36727857 (Compound 45) | |
| HSD17B11 | recombinant protein expressed in HEK293 cells with C-terminal Histidine-tag; full length human | Homo sapiens | Enzymatic assay (hHSD17B11) | IC50 > 10 µM (n=3) | IC50 > 10 µM (n=3) | PMID: 36727857 (Compound 45) |
In cell potency
| Target name | Target information | Species | Assay description | BI-3231 | BI-0955 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| HSD17B13 | Homo sapiens | Cellular hHSD17B13 assay (HEK cells) | IC50 = 11 nM ± 5.000 nM (n=2) | IC50 > 10 µM (n=2) | PMID: 36727857 (Compound 45) |