Assay Detail
Binding
CHEMBL4030006
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Inhibition of COX1 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay
12
Total Activities
12
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
Novel pyrazoles and pyrazolo[1,2-a]pyridazines as selective COX-2 inhibitors; Ultrasound-assisted synthesis, biological evaluation, and DFT calculations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.08 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071983 | — | — | 1 | 7.18 |
| CHEMBL4065530 | — | — | 1 | 7.15 |
| CHEMBL4074153 | — | — | 1 | 7.13 |
| CHEMBL4059594 | — | — | 1 | 7.09 |
| CHEMBL4086962 | — | — | 1 | 7.05 |
| CHEMBL4103357 | — | — | 1 | 7.04 |
| CHEMBL118 | CELECOXIB | 4.0 | 1 | 6.90 |
| CHEMBL296266 | — | — | 1 | - |
| CHEMBL4095610 | — | — | 1 | - |
| CHEMBL4068239 | — | — | 1 | - |
| CHEMBL4079108 | — | — | 1 | - |
| CHEMBL4094661 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071983 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL4065530 | — | IC50 | = | 70.4 | nM | 7.15 |
| CHEMBL4074153 | — | IC50 | = | 74.4 | nM | 7.13 |
| CHEMBL4059594 | — | IC50 | = | 82.1 | nM | 7.09 |
| CHEMBL4086962 | — | IC50 | = | 88.1 | nM | 7.05 |
| CHEMBL4103357 | — | IC50 | = | 92.2 | nM | 7.04 |
| CHEMBL118 | CELECOXIB | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL296266 | — | IC50 | - | — | - | |
| CHEMBL4095610 | — | IC50 | - | — | - | |
| CHEMBL4068239 | — | IC50 | - | — | - | |
| CHEMBL4079108 | — | IC50 | - | — | - | |
| CHEMBL4094661 | — | IC50 | - | — | - |