Potency data for probe TP-050 and control TP-050n
In vitro potency
| Target name | Target information | Species | Assay description | TP-050 | TP-050n | Publication of assay conditions |
|---|---|---|---|---|---|---|
| AMPA | His-tagged GluA2 LBD protein; ligand binding domain | Homo sapiens | AMPA receptor scintillation proximity binding assay: SPA | IC50 > 30 µM | IC50 > 30 µM | PMID: 35051811 |
In cell potency
| Target name | Target information | Species | Assay description | TP-050 | TP-050n | Publication of assay conditions |
|---|---|---|---|---|---|---|
| GRIN2A | CHO cells expressing GluN2A/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2A-containing NMDA receptor (Ca2+ influx) assay (EC50) | EC50 = 510 nM | EC50 > 30 µM | PMID: 35051811 |
| GRIN2A | CHO cells expressing GluN2A/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2A-containing NMDA receptor (Ca2+ influx) assay (potentiation) | Max. potentiation = 350% | Max. potentiation < 150% | PMID: 35051811 |
| GRIN2B | CHO cells expressing GluN2B/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2B-containing NMDA receptor (Ca2+ influx) assay (EC50) | EC50 > 30 µM | PMID: 35051811 | |
| GRIN2B | CHO cells expressing GluN2B/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2B-containing NMDA receptor (Ca2+ influx) assay (potentiation) | Max. potentiation < 150% | PMID: 35051811 | |
| GRIN2C | CHO cells expressing GluN2C/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2C-containing NMDA receptor (Ca2+ influx) assay (EC50) | EC50 > 30 µM | PMID: 35051811 | |
| GRIN2C | CHO cells expressing GluN2C/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2C-containing NMDA receptor (Ca2+ influx) assay (potentiation) | Max. potentiation < 200% | PMID: 35051811 | |
| GRIN2D | CHO cells expressing GluN2D/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2D-containing NMDA receptor (Ca2+ influx) assay (EC50) | EC50 > 9.6 µM | PMID: 35051811 | |
| GRIN2D | CHO cells expressing GluN2D/GluN1a in the presence of glutamate at an EC30 concentration | Homo sapiens | GluN2D-containing NMDA receptor (Ca2+ influx) assay (potentiation) | Max. potentiation < 260% | PMID: 35051811 |