Potency data for probe A-1155463 and control A-1107969
In vitro potency
| Target name | Target information | Species | Assay description | A-1155463 | A-1107969 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BCL2L1 | recombinant protein (GST-Bcl-xL); full length | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) with BCL2L1 | IC50 = 0.55 nM (n=3) | IC50 = 270 nM (n=3) | PMID: 25313317 |
| BCL2 | recombinant protein (GST-Bcl-2); full length | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) with BCL2 | IC50 = 382 nM (n=3) | IC50 = 3.78 µM (n=3) | PMID: 25313317 |
| MCL1 | recombinant protein (GST-Mcl-1); full length | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) with MCL1 | IC50 = 14 µM (n=3) | IC50 = 2 µM (n=3) | PMID: 25313317 |
In cell potency
| Target name | Target information | Species | Assay description | A-1155463 | A-1107969 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| H146 (BCL-XL dependent cell line) | Homo sapiens | CellTiter-Glo Luminescent Cell Viability Assay (BCL-XL dependent cell line H146): Apoptosis test: 10% HS/ 48 hr | EC50 = 70 nM | PMID: 25313317 | ||
| MOLT-4 (BCL-XL dependent cell line) | Homo sapiens | CellTiter-Glo Luminescent Cell Viability Assay (BCL-XL dependent cell line MOLT-4): Apoptosis test: 10% HS/ 48 hr | EC50 = 214 nM | EC50 > 10 µM | PMID: 25313317 | |
| RS4-11 (BCL-2 dependent cell line) | Homo sapiens | CellTiter-Glo Luminescent Cell Viability Assay (BCL-2 dependent cell line RS4-11): Apoptosis test: 10% HS/ 48 hr | EC50 > 10 µM | PMID: 25313317 |