Assay Detail
Binding
CHEMBL4810363
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Inhibition of human recombinant COX-2 assessed as reduction in peroxidase activity using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.05 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 7.55 |
| CHEMBL4870569 | — | — | 1 | 6.92 |
| CHEMBL4865464 | — | — | 1 | 6.65 |
| CHEMBL4859571 | — | — | 1 | 6.44 |
| CHEMBL49319 | — | — | 1 | 6.41 |
| CHEMBL416146 | ETORICOXIB | 4.0 | 1 | 6.37 |
| CHEMBL4857474 | — | — | 1 | 6.35 |
| CHEMBL4868446 | — | — | 1 | 6.30 |
| CHEMBL4862802 | — | — | 1 | 6.08 |
| CHEMBL4848190 | — | — | 1 | 5.49 |
| CHEMBL4848265 | — | — | 1 | 5.39 |
| CHEMBL4866615 | — | — | 1 | 5.20 |
| CHEMBL4866509 | — | — | 1 | 4.77 |
| CHEMBL4867405 | — | — | 1 | 4.74 |
| CHEMBL4864897 | — | — | 1 | - |
| CHEMBL4846538 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118 | CELECOXIB | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4870569 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4865464 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4859571 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL49319 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL416146 | ETORICOXIB | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4857474 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4868446 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4862802 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4848190 | — | IC50 | = | 3240.0 | nM | 5.49 |
| CHEMBL4848265 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4866615 | — | IC50 | = | 6360.0 | nM | 5.20 |
| CHEMBL4866509 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL4867405 | — | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL4864897 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4846538 | — | IC50 | > | 50000.0 | nM | - |