Assay Detail
Binding
CHEMBL1106770
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Inhibition of COX1 in human whole blood assessed as TXB2 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 | 5.86 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1204023 | — | — | 1 | 7.10 |
| CHEMBL1079876 | — | — | 1 | 7.00 |
| CHEMBL1080231 | — | — | 1 | 6.77 |
| CHEMBL224400 | — | — | 1 | 6.75 |
| CHEMBL1075636 | — | — | 1 | 6.72 |
| CHEMBL1204024 | — | — | 1 | 6.57 |
| CHEMBL1079878 | — | — | 1 | 6.32 |
| CHEMBL1081856 | — | — | 1 | 6.32 |
| CHEMBL1078683 | — | — | 1 | 6.25 |
| CHEMBL1078374 | — | — | 1 | 6.25 |
| CHEMBL1080405 | — | — | 1 | 6.16 |
| CHEMBL1079073 | — | — | 1 | 6.12 |
| CHEMBL1079335 | — | — | 1 | 6.04 |
| CHEMBL1204025 | — | — | 1 | 6.03 |
| CHEMBL1079875 | — | — | 1 | 6.00 |
| CHEMBL1077403 | — | — | 1 | 6.00 |
| CHEMBL1077388 | — | — | 1 | 5.96 |
| CHEMBL1080407 | — | — | 1 | 5.96 |
| CHEMBL1079333 | — | — | 1 | 5.94 |
| CHEMBL1078860 | — | — | 1 | 5.94 |
| CHEMBL1080406 | — | — | 1 | 5.91 |
| CHEMBL1077398 | — | — | 1 | 5.88 |
| CHEMBL1078376 | — | — | 1 | 5.88 |
| CHEMBL1081855 | — | — | 1 | 5.80 |
| CHEMBL1079074 | — | — | 1 | 5.69 |
| CHEMBL1078373 | — | — | 1 | 5.67 |
| CHEMBL1079877 | — | — | 1 | 5.65 |
| CHEMBL1078375 | — | — | 1 | 5.59 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 5.58 |
| CHEMBL1078557 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1204023 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1079876 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1080231 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL224400 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1075636 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1204024 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1079878 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1081856 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1078683 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1078374 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1080405 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1079073 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL1079335 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1204025 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1077403 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL1079875 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1077388 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL1080407 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL1078860 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL1079333 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL1080406 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL1077398 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL1078376 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL1081855 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1079074 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL1078373 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL1079877 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL1078375 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL118 | CELECOXIB | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1078557 | — | IC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL1080404 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL56367 | NIMESULIDE | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL1078377 | — | IC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL1078090 | — | IC50 | = | 7150.0 | nM | 5.15 |
| CHEMBL1077436 | — | IC50 | = | 8550.0 | nM | 5.07 |
| CHEMBL1077442 | — | IC50 | = | 9760.0 | nM | 5.01 |
| CHEMBL1078091 | — | IC50 | = | 20020.0 | nM | 4.70 |
| CHEMBL1078682 | — | IC50 | = | 25240.0 | nM | 4.60 |
| CHEMBL1078378 | — | IC50 | = | 60390.0 | nM | 4.22 |