Assay Detail
Binding
CHEMBL3887378
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Inhibition Assay: The murine monocyte/macrophage cell line J774 is grown in Dulbecco's modified Eagle's medium (DMEM), enriched with glutamine (2 mM), HEPES (25 mM), penicillin (100 ug/mL), streptomycin (100 ug/mL), 10% of fetal bovine serum (FBS) and 1.2% of sodium pyruvate. The cells are distributed in 24-well plates at a density of 2.5x105 cells/mL or in culture dishes with a diameter of 10 cm (1x107 cells/10 mL/dish) and kept for 2 hours at 37° C. in a CO2 (5%)/O2 (95%) atmosphere. Just before the experiments, the culture medium is replaced with fresh medium without FBS to avoid interference during the radio-immunological phase and the cells are stimulated as described below.Evaluation of COX-1 Activity.The cells are pretreated with the test compounds for 15 minutes and then incubated for 30 minutes with arachidonic acid (15x10-6 m). At the end of incubation the supernatants are collected for evaluating, by means of radio-immunological assays, the amount of PGE2 produced.
50
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
1,5-Diary1-2-alkylpyrrole-3-substituted nitro esters, selective COX-2 inhibitors and nitric oxide donors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 6.89 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1939677 | — | — | 1 | 8.70 |
| CHEMBL1939671 | — | — | 1 | 8.15 |
| CHEMBL3104559 | — | — | 1 | 7.85 |
| CHEMBL2337402 | — | — | 1 | 7.85 |
| CHEMBL2337404 | — | — | 1 | 7.82 |
| CHEMBL2337400 | — | — | 1 | 7.77 |
| CHEMBL1939670 | — | — | 1 | 7.72 |
| CHEMBL1939511 | — | — | 1 | 7.64 |
| CHEMBL1939678 | — | — | 1 | 7.57 |
| CHEMBL2337407 | — | — | 1 | 7.57 |
| CHEMBL1939675 | — | — | 1 | 7.57 |
| CHEMBL2337401 | — | — | 1 | 7.55 |
| CHEMBL1939668 | — | — | 1 | 7.37 |
| CHEMBL2337408 | — | — | 1 | 7.34 |
| CHEMBL3949091 | — | — | 1 | 7.26 |
| CHEMBL4109738 | — | — | 1 | 7.24 |
| CHEMBL3104540 | — | — | 1 | 7.17 |
| CHEMBL3905421 | — | — | 1 | 7.16 |
| CHEMBL3104548 | — | — | 1 | 7.07 |
| CHEMBL1939680 | — | — | 1 | 7.07 |
| CHEMBL1939514 | — | — | 1 | 7.07 |
| CHEMBL2337409 | — | — | 1 | 7.05 |
| CHEMBL1939512 | — | — | 1 | 7.05 |
| CHEMBL3906128 | — | — | 1 | 6.96 |
| CHEMBL4111609 | — | — | 2 | 6.85 |
| CHEMBL4109772 | — | — | 1 | 6.80 |
| CHEMBL1939676 | — | — | 1 | 6.77 |
| CHEMBL2337406 | — | — | 1 | 6.72 |
| CHEMBL3927500 | — | — | 1 | 6.66 |
| CHEMBL3104556 | — | — | 2 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1939677 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1939671 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2337402 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3104559 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2337404 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2337400 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1939670 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1939511 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1939678 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2337407 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1939675 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2337401 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1939668 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2337408 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3949091 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4109738 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3104540 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3905421 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3104548 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1939680 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1939514 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2337409 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1939512 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3906128 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4111609 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4111609 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4109772 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1939676 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2337406 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3927500 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3104556 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3104556 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1939515 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3104558 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3104539 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4110339 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2337396 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2337405 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3908211 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1939517 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3104553 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL2153825 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2337403 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2337399 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2153827 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1939516 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3971575 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2337398 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3104544 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3104544 | — | IC50 | = | 1600.0 | nM | 5.80 |