Potency data for probe JNJ-78911118 and control JNJ-77914993
In vitro potency
| Target name | Target information | Species | Assay description | JNJ-78911118 | JNJ-77914993 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| GRIN1, GRIN2A | hippocampal neuron membranes | Rattus norvegicus | Displacement of the GRIN1/GRIN2A interface binding radioligand [3H]-1 in hippocampal neuron membranes: Displacement occurs in a concentration dependent manner. | Ki = 78 nM (n=3) | PMID: 40361296 |
In cell potency
| Target name | Target information | Species | Assay description | JNJ-78911118 | JNJ-77914993 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| GRIN2A | human recombinant expressed in T-REx CHO-K1 cells | Homo sapiens | Fluorometric Calcium Mobilization Assays (GRIN2A): FLIPR assay | IC50 = 40 nM | IC50 = 48 µM | PMID: 39960408 |
| GRIN2A | human recombinant expressed in T-REx CHO-K1 cells | Homo sapiens | Fluorometric Calcium Mobilization Assays (GRIN2A, Current blocking): FLIPR assay | Blocking of GRIN1/GRIN2A-induced calcium flux = 100% | PMID: 39960408 | |
| GRIN2B | human recombinant expressed in T-REx CHO-K1 cells | Homo sapiens | Fluorometric Calcium Mobilization Assays (GRIN2B): FLIPR assay | IC50 > 50 µM | IC50 > 50 µM | PMID: 39960408 |
| GRIN2C | human recombinant expressed in T-REx CHO-K1 cells | Homo sapiens | Fluorometric Calcium Mobilization Assays (GRIN2C): FLIPR assay | IC50 > 50 µM | IC50 > 50 µM | PMID: 39960408 |
| GRIN2D | human recombinant expressed in T-REx CHO-K1 cells | Homo sapiens | Fluorometric Calcium Mobilization Assays (GRIN2D): FLIPR assay | IC50 > 50 µM | IC50 > 50 µM | PMID: 39960408 |
| GRIN1, GRIN2A | cRNA | Rattus norvegicus | Xenopus oocytes recordings (dimeric GRIN1, GRIN2A): Fully blocks glutamate/glycine-evoked currents in oocytes. | IC50 = 44 nM (n=16) | PMID: 40361296 | |
| GRIN1, GRIN2A, GRIN2B | cRNA | Rattus norvegicus | Xenopus oocytes recordings (trimeric GRIN1, GRIN2A, GRIN2B): Reduced glutamate/glycine-evoked currents in oocytes. (53% maximal block); two-electrode voltage clamp | IC50 = 202 nM (n=12) | PMID: 40361296 | |
| GRIN1, GRIN2A, GRIN2C | cRNA | Rattus norvegicus | Xenopus oocytes recordings (trimeric GRIN1, GRIN2A, GRIN2C): Reduced glutamate/glycine-evoked currents in oocytes. (83% maximal block); two-electrode voltage clamp | IC50 = 88 nM (n=10) | PMID: 40361296 | |
| GRIN1, GRIN2A, GRIN2D | cRNA | Rattus norvegicus | Xenopus oocytes recordings (trimeric GRIN1, GRIN2A, GRIN2D): Reduced glutamate/glycine-evoked currents in oocytes. (48% maximal block); two-electrode voltage clamp | IC50 = 72 nM (n=10) | PMID: 40361296 |