Assay Detail
Binding
CHEMBL4327232
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Displacement of [3H]CP55940 from recombinant human CB2R expressed in HEK293 cell membranes measured after 90 mins
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.22 | 8.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4462947 | — | — | 1 | 8.76 |
| CHEMBL381791 | — | — | 1 | 8.74 |
| CHEMBL2349625 | — | — | 1 | 8.61 |
| CHEMBL4441693 | — | — | 1 | 8.37 |
| CHEMBL4471470 | — | — | 1 | 8.29 |
| CHEMBL4476681 | — | — | 1 | 8.23 |
| CHEMBL4557732 | — | — | 1 | 8.19 |
| CHEMBL4545068 | — | — | 1 | 8.14 |
| CHEMBL4537616 | — | — | 1 | 8.10 |
| CHEMBL4440363 | — | — | 1 | 8.03 |
| CHEMBL4437411 | — | — | 1 | 7.68 |
| CHEMBL4472381 | — | — | 1 | 7.64 |
| CHEMBL181633 | — | — | 1 | 7.51 |
| CHEMBL4456199 | — | — | 1 | 7.46 |
| CHEMBL4437727 | — | — | 1 | 7.29 |
| CHEMBL4471569 | — | — | 1 | 7.19 |
| CHEMBL4565110 | — | — | 1 | 6.71 |
| CHEMBL4449619 | — | — | 1 | 6.61 |
| CHEMBL4464850 | — | — | 1 | 6.30 |
| CHEMBL2349633 | — | — | 1 | 6.21 |
| CHEMBL4516896 | — | — | 1 | 6.07 |
| CHEMBL4437336 | — | — | 1 | 5.97 |
| CHEMBL4561828 | — | — | 1 | 5.91 |
| CHEMBL4542322 | — | — | 1 | 5.88 |
| CHEMBL4448698 | — | — | 1 | 5.78 |
| CHEMBL4593144 | — | — | 1 | 5.67 |
| CHEMBL4468403 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4462947 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL381791 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2349625 | — | Ki | = | 2.46 | nM | 8.61 |
| CHEMBL4441693 | — | Ki | = | 4.28 | nM | 8.37 |
| CHEMBL4471470 | — | Ki | = | 5.08 | nM | 8.29 |
| CHEMBL4476681 | — | Ki | = | 5.92 | nM | 8.23 |
| CHEMBL4557732 | — | Ki | = | 6.48 | nM | 8.19 |
| CHEMBL4545068 | — | Ki | = | 7.21 | nM | 8.14 |
| CHEMBL4537616 | — | Ki | = | 8.03 | nM | 8.10 |
| CHEMBL4440363 | — | Ki | = | 9.24 | nM | 8.03 |
| CHEMBL4437411 | — | Ki | = | 20.97 | nM | 7.68 |
| CHEMBL4472381 | — | Ki | = | 23.09 | nM | 7.64 |
| CHEMBL181633 | — | Ki | = | 31.2 | nM | 7.51 |
| CHEMBL4456199 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4437727 | — | Ki | = | 50.7 | nM | 7.29 |
| CHEMBL4471569 | — | Ki | = | 64.72 | nM | 7.19 |
| CHEMBL4565110 | — | Ki | = | 195.7 | nM | 6.71 |
| CHEMBL4449619 | — | Ki | = | 244.06 | nM | 6.61 |
| CHEMBL4464850 | — | Ki | = | 495.77 | nM | 6.30 |
| CHEMBL2349633 | — | Ki | = | 621.0 | nM | 6.21 |
| CHEMBL4516896 | — | Ki | = | 845.42 | nM | 6.07 |
| CHEMBL4437336 | — | Ki | = | 1081.88 | nM | 5.97 |
| CHEMBL4561828 | — | Ki | = | 1220.19 | nM | 5.91 |
| CHEMBL4542322 | — | Ki | = | 1324.12 | nM | 5.88 |
| CHEMBL4448698 | — | Ki | = | 1673.74 | nM | 5.78 |
| CHEMBL4593144 | — | Ki | = | 2141.79 | nM | 5.67 |
| CHEMBL4468403 | — | Ki | = | 2494.08 | nM | 5.60 |