Assay Detail
Binding
CHEMBL959186
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Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 5.86 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL559612 | CP-55940 | — | 1 | 8.91 |
| CHEMBL188 | WIN-552122 | — | 1 | 8.22 |
| CHEMBL476833 | — | — | 1 | 7.91 |
| CHEMBL471248 | — | — | 1 | 6.13 |
| CHEMBL470602 | — | — | 1 | 6.01 |
| CHEMBL470212 | — | — | 1 | 5.96 |
| CHEMBL470618 | — | — | 1 | 5.93 |
| CHEMBL512509 | — | — | 1 | 5.86 |
| CHEMBL513034 | — | — | 1 | 5.68 |
| CHEMBL470224 | — | — | 1 | 5.56 |
| CHEMBL470199 | — | — | 1 | 5.46 |
| CHEMBL511304 | — | — | 1 | 5.39 |
| CHEMBL513763 | — | — | 1 | 5.38 |
| CHEMBL470820 | — | — | 1 | 5.31 |
| CHEMBL471249 | — | — | 1 | 5.21 |
| CHEMBL470016 | — | — | 1 | 5.21 |
| CHEMBL470018 | — | — | 1 | 5.21 |
| CHEMBL470619 | — | — | 1 | 5.04 |
| CHEMBL505327 | — | — | 1 | 5.02 |
| CHEMBL470017 | — | — | 1 | 4.91 |
| CHEMBL471247 | — | — | 1 | 4.72 |
| CHEMBL470019 | — | — | 1 | - |
| CHEMBL506746 | — | — | 1 | - |
| CHEMBL453459 | — | — | 1 | - |
| CHEMBL472068 | — | — | 1 | - |
| CHEMBL472493 | — | — | 1 | - |
| CHEMBL469340 | — | — | 1 | - |
| CHEMBL447225 | — | — | 1 | - |
| CHEMBL511303 | — | — | 1 | - |
| CHEMBL508042 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL559612 | CP-55940 | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL188 | WIN-552122 | Ki | = | 6.06 | nM | 8.22 |
| CHEMBL476833 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL471248 | — | Ki | = | 738.0 | nM | 6.13 |
| CHEMBL470602 | — | Ki | = | 978.0 | nM | 6.01 |
| CHEMBL470212 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL470618 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL512509 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL513034 | — | Ki | = | 2080.0 | nM | 5.68 |
| CHEMBL470224 | — | Ki | = | 2760.0 | nM | 5.56 |
| CHEMBL470199 | — | Ki | = | 3460.0 | nM | 5.46 |
| CHEMBL511304 | — | Ki | = | 4110.0 | nM | 5.39 |
| CHEMBL513763 | — | Ki | = | 4190.0 | nM | 5.38 |
| CHEMBL470820 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL470018 | — | Ki | = | 6180.0 | nM | 5.21 |
| CHEMBL471249 | — | Ki | = | 6140.0 | nM | 5.21 |
| CHEMBL470016 | — | Ki | = | 6230.0 | nM | 5.21 |
| CHEMBL470619 | — | Ki | = | 9140.0 | nM | 5.04 |
| CHEMBL505327 | — | Ki | = | 9570.0 | nM | 5.02 |
| CHEMBL470017 | — | Ki | = | 12300.0 | nM | 4.91 |
| CHEMBL471247 | — | Ki | = | 19100.0 | nM | 4.72 |
| CHEMBL508042 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL472067 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL470198 | — | Ki | >= | 10000.0 | nM | - |
| CHEMBL469519 | — | Ki | >= | 10000.0 | nM | - |
| CHEMBL470197 | — | Ki | >= | 10000.0 | nM | - |
| CHEMBL516339 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL472635 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL472634 | — | Ki | >= | 10000.0 | nM | - |
| CHEMBL443168 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL455557 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL511303 | — | Ki | >= | 10000.0 | nM | - |
| CHEMBL447225 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL469340 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL472493 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL472068 | — | Ki | >= | 10000.0 | nM | - |
| CHEMBL453459 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL506746 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL470019 | — | Ki | > | 10000.0 | nM | - |