Potency data for probe BAY-293 and control BAY-294
In vitro potency
| Target name | Target information | Species | Assay description | BAY-293 | BAY-294 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| SOS1 | Homo sapiens | KRAS(G12C)–SOS1(cat) interaction assay | IC50 = 21 nM ± 8.000 nM (n=4) | IC50 = 2340 nM ± 970.000 nM (n=4) | PMID: 30683722 | |
| SOS2 | Homo sapiens | KRAS(G12C)–SOS2(cat) activation assay | IC50 > 20 µM (n=4) | IC50 > 20 µM (n=4) | PMID: 30683722 | |
| MCF2L | Homo sapiens | CDC42 activation by DBS assay | IC50 > 20 µM (n=2) | IC50 > 20 µM (n=2) | PMID: 30683722 | |
| EGFR | Homo sapiens | EGFR kinase inhibition assay | IC50 > 20 µM (n=2) | IC50 > 20 µM (n=2) | PMID: 30683722 |
In cell potency
| Target name | Target information | Species | Assay description | BAY-293 | BAY-294 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| RAS | Homo sapiens | Cellular assay: Active RAS (KRAS, HRAS, NRAS) in HeLa cells (KRASwt): Quantification of the amount of activated, GTP-loaded total RAS from cellular lysates with G-LISA kit | IC50 = 0.41 µM (n=1) | IC50 = 18.6 µM (n=1) | PMID: 30683722 | |
| RAS | Homo sapiens | Cellular assay: Active RAS (KRAS, HRAS, NRAS)in Calu-1 cells (KRASwt): Quantification of the amount of activated, GTP-loaded total RAS from cellular lysates with G-LISA kit | IC50 = 200 nM ± 13.000 nM (n=2) | IC50 = 4120 nM (n=1) | PMID: 30683722 | |
| MAPK1 | Homo sapiens | Cellular assay: Inhibition of phospho-ERK (pERK) in K-562 cells: Quantification of phospho-ERK (pERK) | IC50 = 180 nM ± 100.000 nM (n=2) | IC50 = 4570 nM ± 910.000 nM (n=2) | PMID: 30683722 |