Assay Detail
Binding
CHEMBL768738
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IC50 against Prostaglandin G/H synthase 1 from human platelet rich plasma
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Plasma |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, structure-activity relationships, and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent, selective, and orally active cyclooxygenase-2 inhibitors. 1. Thiazolone and oxazolone series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.81 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6 | INDOMETHACIN | 4.0 | 1 | 8.09 |
| CHEMBL16434 | — | — | 1 | 6.60 |
| CHEMBL275835 | DARBUFELONE | 2.0 | 1 | 6.22 |
| CHEMBL16251 | — | — | 1 | 5.57 |
| CHEMBL7162 | NS-398 | — | 1 | 5.48 |
| CHEMBL16855 | — | — | 1 | 5.24 |
| CHEMBL16550 | — | — | 1 | 5.19 |
| CHEMBL277721 | — | — | 1 | 5.04 |
| CHEMBL280226 | — | — | 1 | 4.84 |
| CHEMBL16048 | — | — | 1 | - |
| CHEMBL276506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6 | INDOMETHACIN | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL16434 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL275835 | DARBUFELONE | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL16251 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL7162 | NS-398 | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL16855 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL16550 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL277721 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL280226 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL16048 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL276506 | — | IC50 | > | 20000.0 | nM | - |