Assay Detail
Binding
CHEMBL3070221
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Antagonist activity at CB1 receptor (unknown origin)
52
Total Activities
26
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
Activity landscape analysis, CoMFA and CoMSIA studies of pyrazole CB1 antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 52 | 6.98 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2296777 | — | — | 2 | 8.22 |
| CHEMBL2296781 | — | — | 2 | 8.22 |
| CHEMBL285932 | — | — | 2 | 8.13 |
| CHEMBL2296784 | — | — | 2 | 7.93 |
| CHEMBL476833 | — | — | 2 | 7.88 |
| CHEMBL2296786 | — | — | 2 | 7.74 |
| CHEMBL2296782 | — | — | 2 | 7.70 |
| CHEMBL2296783 | — | — | 2 | 7.51 |
| CHEMBL2296779 | — | — | 2 | 7.33 |
| CHEMBL36250 | — | — | 2 | 7.22 |
| CHEMBL2296780 | — | — | 2 | 7.20 |
| CHEMBL286188 | — | — | 2 | 7.12 |
| CHEMBL349955 | — | — | 2 | 7.09 |
| CHEMBL285259 | — | — | 2 | 7.09 |
| CHEMBL2296774 | — | — | 2 | 7.00 |
| CHEMBL285153 | — | — | 2 | 6.91 |
| CHEMBL287472 | — | — | 2 | 6.69 |
| CHEMBL2296785 | — | — | 2 | 6.62 |
| CHEMBL2296775 | — | — | 2 | 6.59 |
| CHEMBL2296776 | — | — | 2 | 6.49 |
| CHEMBL94239 | — | — | 2 | 6.43 |
| CHEMBL2296787 | — | — | 2 | 6.40 |
| CHEMBL432857 | — | — | 2 | 6.22 |
| CHEMBL285486 | — | — | 2 | 5.95 |
| CHEMBL32929 | — | — | 2 | 5.45 |
| CHEMBL2296778 | — | — | 2 | 4.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2296781 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2296777 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2296777 | — | Ki | = | 5.984 | nM | 8.22 |
| CHEMBL2296781 | — | Ki | = | 5.998 | nM | 8.22 |
| CHEMBL285932 | — | Ki | = | 7.482 | nM | 8.13 |
| CHEMBL285932 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL2296784 | — | Ki | = | 11.67 | nM | 7.93 |
| CHEMBL2296784 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL476833 | — | Ki | = | 13.24 | nM | 7.88 |
| CHEMBL476833 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL2296786 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL2296786 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL2296782 | — | Ki | = | 19.82 | nM | 7.70 |
| CHEMBL2296782 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL2296783 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL2296783 | — | Ki | = | 31.12 | nM | 7.51 |
| CHEMBL2296779 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2296779 | — | Ki | = | 46.99 | nM | 7.33 |
| CHEMBL36250 | — | Ki | = | 60.39 | nM | 7.22 |
| CHEMBL36250 | — | Ki | = | 60.4 | nM | 7.22 |
| CHEMBL2296780 | — | Ki | = | 62.95 | nM | 7.20 |
| CHEMBL2296780 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL286188 | — | Ki | = | 76.7 | nM | 7.12 |
| CHEMBL286188 | — | Ki | = | 76.74 | nM | 7.12 |
| CHEMBL349955 | — | Ki | = | 81.5 | nM | 7.09 |
| CHEMBL349955 | — | Ki | = | 81.47 | nM | 7.09 |
| CHEMBL285259 | — | Ki | = | 81.85 | nM | 7.09 |
| CHEMBL285259 | — | Ki | = | 81.8 | nM | 7.09 |
| CHEMBL2296774 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2296774 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL285153 | — | Ki | = | 122.74 | nM | 6.91 |
| CHEMBL285153 | — | Ki | = | 122.7 | nM | 6.91 |
| CHEMBL287472 | — | Ki | = | 203.24 | nM | 6.69 |
| CHEMBL287472 | — | Ki | = | 203.2 | nM | 6.69 |
| CHEMBL2296785 | — | Ki | = | 240.99 | nM | 6.62 |
| CHEMBL2296785 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL2296775 | — | Ki | = | 256.4 | nM | 6.59 |
| CHEMBL2296775 | — | Ki | = | 256.45 | nM | 6.59 |
| CHEMBL2296776 | — | Ki | = | 327.3 | nM | 6.49 |
| CHEMBL2296776 | — | Ki | = | 327.34 | nM | 6.49 |
| CHEMBL94239 | — | Ki | = | 374.1 | nM | 6.43 |
| CHEMBL94239 | — | Ki | = | 374.11 | nM | 6.43 |
| CHEMBL2296787 | — | Ki | = | 399.9 | nM | 6.40 |
| CHEMBL2296787 | — | Ki | = | 399.94 | nM | 6.40 |
| CHEMBL432857 | — | Ki | = | 605.3 | nM | 6.22 |
| CHEMBL432857 | — | Ki | = | 605.34 | nM | 6.22 |
| CHEMBL285486 | — | Ki | = | 1119.4 | nM | 5.95 |
| CHEMBL285486 | — | Ki | = | 1119.44 | nM | 5.95 |
| CHEMBL32929 | — | Ki | = | 3564.5 | nM | 5.45 |
| CHEMBL32929 | — | Ki | = | 3564.51 | nM | 5.45 |