Potency data for probe A-1211212 and control A-1210227
In vitro potency
| Target name | Target information | Species | Assay description | A-1211212 | A-1210227 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| BCL2L1 | recombinant protein (GST-Bcl-xL); full length | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) with BCL2L1 | IC50 = 753 nM (n=3) | IC50 > 25 µM (n=3) | PMID: 25313317 |
| BCL2 | recombinant protein (GST-Bcl-2); full length | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) with BCL2 | IC50 = 1.4 nM (n=3) | IC50 = 296 nM (n=3) | PMID: 25313317 |
| MCL1 | recombinant protein (GST-Mcl-1); full length | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) with MCL1 | IC50 = 2.05 µM (n=3) | PMID: 25313317 |
In cell potency
| Target name | Target information | Species | Assay description | A-1211212 | A-1210227 | 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 > 5 µM | EC50 > 5 µM | ||
| AMO-1 (MCL-1 dependent cell line) | Homo sapiens | CellTiter-Glo Luminescent Cell Viability Assay ( MCL-1 dependent cell line AMO-1): Apoptosis test: 10% HS/ 48 hr | EC50 > 1 µM | |||
| BCL-2 dependent cell line: RS4-11 | Homo sapiens | CellTiter-Glo Luminescent Cell Viability Assay with RS4-11 cells (BCL-2 dependent cell line): Apoptosis test: 10% HS/ 48 hr | EC50 = 6 nM | EC50 > 5 µM |