Potency data for probe JNJ-79883960 and control JNJ-78832000
In cell potency
| Target name | Target information | Species | Assay description | Probe result (SD) | Control result (SD) | Publication of assay conditions |
|---|---|---|---|---|---|---|
| NRLP3 | PBMC cells | Homo sapiens | NLRP-3 cell assay (IL1-beta inhibition): The inhibition of IL-1beta on 100 ng/ml LPS-treated human PBMCs (6 h) was determined using Mesoscale discovery (MSD). | IC50 = 27.600 nM | IC50 > 20 µM | PMID: 39653810 |
| NRLP3 | PBMC cells | Homo sapiens | NLRP-3 cell assay (IL6 inhibition): The inhibition of IL-6 on 100 ng/ml LPS-treated human PBMCs (6 h) was determined using Mesoscale discovery (MSD). | IC50 > 10 µM | IC50 > 20 µM | PMID: 39653810 |
| NRLP3 | PBMC cells | Homo sapiens | NLRP-3 cell assay (TNF inhibition): The inhibition of TNF on 100 ng/ml LPS-treated human PBMCs (6 h) was determined using Mesoscale discovery (MSD). | IC50 > 10 µM | IC50 > 20 µM | PMID: 39653810 |
| NRLP3 | Whole blood | Homo sapiens | Whole blood assay (IL1-beta inhibition): Human fresh whole blood was primed with 100 ng/ml LPS for 2 h followed by 5 mM ATP for another 3 h in the presence of JNJ-79883960. Plasma is collected by centrifugation of the blood for 15 min at 2000 × g and used to determine levels of IL-1β by MSD. Blood from three independent healthy donors was used. | IC50 = 2.663 µM (n=12) | PMID: 39653810 | |
| NRLP3 | BMDMs from C57BL/6 mice | Mus musculus | BMDM cell assay (IL1-beta inhibition): LPS-primed BMDMs from C57BL/6 mice were treated with 20 μM Nig in the presence of JNJ-79883960. After 1 h, supernatant was collected and levels of IL-1β were determined using MSD. | IC50 = 0.247 µM (n=6) | PMID: 39653810 | |
| NRLP3 | Splenocytes from C57BL/6 mice | Mus musculus | Mouse splenocytes assay (IL1-beta inhibition): LPS-primed splenocytes from C57BL/6 mice were treated with 5 mM ATP in the presence of a dose response of JNJ-79883960. After 1 h, supernatant was collected and levels of IL-1β were determined using MSD. | IC50 = 68 nM | PMID: 39653810 |