Potency data for probe JNJ-42226314 and control JNJ-8034
In vitro potency
| Target name | Target information | Species | Assay description | JNJ-42226314 | JNJ-8034 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MGLL, MGLL | purified wild-type MGLL (wt-MGLL 6H-11-313) ; full length human | Homo sapiens | Fluorometric Assay (Inhibition of 4MU-B cleavage) | IC50 < 5 nM (n=10) | IC50 > 10 µM (n=6) | PMID: 31818916 |
In cell potency
| Target name | Target information | Species | Assay description | JNJ-42226314 | JNJ-8034 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| MGLL | human HeLa cells | Homo sapiens | [3H] 2-OG cleavage activity assay (HeLa): Radiometric assay | IC50 = 1.13 nM ± 0.050 nM (n=10) | PMID: 31818916 | |
| MGLL | human PBMC (blood) | Homo sapiens | [3H] 2-OG cleavage activity assay (PBMC): Radiometric assay | IC50 = 1.88 nM ± 0.410 nM (n=6) | PMID: 31818916 | |
| MGLL | mouse brain | Mus musculus | [3H] 2-OG cleavage activity assay (mouse brain): Radiometric assay | IC50 = 0.67 nM ± 0.110 nM (n=9) | PMID: 31818916 | |
| MGLL | rat brain | Rattus sp. | [3H] 2-OG cleavage activity assay (rat brain): Radiometric assay | IC50 = 0.97 nM ± 0.120 nM (n=10) | PMID: 31818916 |