Assay Detail
Binding
CHEMBL1106771
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of COX2 in LPS-stimulated human whole blood assessed as PGE2 production by enzyme immunoassay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.75 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224400 | — | — | 1 | 7.05 |
| CHEMBL1079335 | — | — | 1 | 6.92 |
| CHEMBL1079876 | — | — | 1 | 6.80 |
| CHEMBL1080405 | — | — | 1 | 6.62 |
| CHEMBL1077388 | — | — | 1 | 6.57 |
| CHEMBL1204023 | — | — | 1 | 6.48 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 6.46 |
| CHEMBL1079333 | — | — | 1 | 6.39 |
| CHEMBL1077403 | — | — | 1 | 6.35 |
| CHEMBL1080231 | — | — | 1 | 6.34 |
| CHEMBL56367 | NIMESULIDE | 4.0 | 1 | 6.16 |
| CHEMBL1078090 | — | — | 1 | 6.14 |
| CHEMBL1080406 | — | — | 1 | 6.04 |
| CHEMBL1081855 | — | — | 1 | 6.04 |
| CHEMBL1079875 | — | — | 1 | 5.80 |
| CHEMBL1079073 | — | — | 1 | 5.79 |
| CHEMBL1075636 | — | — | 1 | 5.68 |
| CHEMBL1204024 | — | — | 1 | 5.61 |
| CHEMBL1080407 | — | — | 1 | 5.60 |
| CHEMBL1078091 | — | — | 1 | 5.59 |
| CHEMBL1081856 | — | — | 1 | 5.57 |
| CHEMBL1079877 | — | — | 1 | 5.57 |
| CHEMBL1078860 | — | — | 1 | 5.43 |
| CHEMBL1077398 | — | — | 1 | 5.23 |
| CHEMBL1080404 | — | — | 1 | 5.14 |
| CHEMBL1078557 | — | — | 1 | 5.09 |
| CHEMBL1078375 | — | — | 1 | 5.05 |
| CHEMBL1079878 | — | — | 1 | 5.03 |
| CHEMBL1079074 | — | — | 1 | 4.96 |
| CHEMBL1078376 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224400 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1079335 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1079876 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1080405 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1077388 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1204023 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL118 | CELECOXIB | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1079333 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1077403 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1080231 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL56367 | NIMESULIDE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1078090 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1080406 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1081855 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1079875 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL1079073 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL1075636 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL1204024 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL1080407 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL1078091 | — | IC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL1079877 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL1081856 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL1078860 | — | IC50 | = | 3740.0 | nM | 5.43 |
| CHEMBL1077398 | — | IC50 | = | 5930.0 | nM | 5.23 |
| CHEMBL1080404 | — | IC50 | = | 7240.0 | nM | 5.14 |
| CHEMBL1078557 | — | IC50 | = | 8150.0 | nM | 5.09 |
| CHEMBL1078375 | — | IC50 | = | 8810.0 | nM | 5.05 |
| CHEMBL1079878 | — | IC50 | = | 9380.0 | nM | 5.03 |
| CHEMBL1079074 | — | IC50 | = | 10830.0 | nM | 4.96 |
| CHEMBL1078376 | — | IC50 | = | 12030.0 | nM | 4.92 |
| CHEMBL1204025 | — | IC50 | = | 13530.0 | nM | 4.87 |
| CHEMBL1078374 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL1078683 | — | IC50 | = | 21610.0 | nM | 4.67 |
| CHEMBL1078373 | — | IC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL1077442 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1078682 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1078378 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1077436 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1078377 | — | IC50 | > | 100000.0 | nM | - |