Potency data for probe JNJ-54119936 and control JNJ-53721590
In vitro potency
| Target name | Target information | Species | Assay description | JNJ-54119936 | JNJ-53721590 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| RORC | RORC ligand binding domain (aa 258-516) | Homo sapiens | ThermoFluor Binding Assay (RORC) | qKD = 5.3 nM | qKD = 515.7 nM | |
| RORA | Homo sapiens | ThermoFluor Binding Assay (RORA) | qKD > 75 µM | qKD = 16.8 µM | ||
| RORB | Homo sapiens | ThermoFluor Binding Assay (RORB) | qKD > 75 µM | qKD = 40 µM |
In cell potency
| Target name | Target information | Species | Assay description | Compound conc. | JNJ-54119936 | JNJ-53721590 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| Genbank accession no. NP_001001523, aa 1–497; full-length | Homo sapiens | One-hybrid LBD : One-hybrid background: AF2 mutant (Y502F) RORC LBD | 6 µM | IC50 = 30 nM | IC50 = 670 nM | PMID: 34040108 | |
| Heparinized human whole blood diluted (1:1) in RPMI 1640 | Homo sapiens | Human whole blood assay: Stimulation with anti-CD3, anti-CD8 and IL-23 in the presence of the inhibitor/ IL-17A levels were measured after two days by MSD cytokine assay. | 10 µM | IC50 = 332 nM | IC50 > 10 µM | PMID: 34040108 |