Assay Detail
Binding
CHEMBL659688
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Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the absence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 5.92 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL120526 | METHANANDAMIDE | — | 1 | 7.55 |
| CHEMBL421967 | — | — | 1 | 7.01 |
| CHEMBL150942 | — | — | 1 | 6.98 |
| CHEMBL330974 | — | — | 1 | 6.96 |
| CHEMBL150849 | — | — | 1 | 6.87 |
| CHEMBL359278 | — | — | 1 | 6.84 |
| CHEMBL151496 | — | — | 1 | 6.80 |
| CHEMBL149691 | — | — | 1 | 6.72 |
| CHEMBL151862 | — | — | 1 | 6.42 |
| CHEMBL151864 | — | — | 1 | 6.41 |
| CHEMBL151717 | — | — | 1 | 6.38 |
| CHEMBL348466 | — | — | 1 | 6.23 |
| CHEMBL346659 | — | — | 1 | 6.20 |
| CHEMBL357526 | — | — | 1 | 6.17 |
| CHEMBL151504 | — | — | 1 | 5.62 |
| CHEMBL274016 | — | — | 1 | 5.53 |
| CHEMBL151167 | — | — | 1 | 5.47 |
| CHEMBL74909 | — | — | 1 | 5.33 |
| CHEMBL359165 | — | — | 1 | 5.31 |
| CHEMBL15848 | ANANDAMIDE | — | 1 | 5.24 |
| CHEMBL346428 | — | — | 1 | 5.09 |
| CHEMBL151068 | — | — | 1 | 4.85 |
| CHEMBL356213 | — | — | 1 | 4.68 |
| CHEMBL151084 | — | — | 1 | 4.48 |
| CHEMBL149859 | LINOLEOYLETHANOLAMIDE | — | 1 | 4.40 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | — | 1 | 4.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL120526 | METHANANDAMIDE | Ki | = | 28.3 | nM | 7.55 |
| CHEMBL421967 | — | Ki | = | 98.1 | nM | 7.01 |
| CHEMBL150942 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL330974 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL150849 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL359278 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL151496 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL149691 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL151862 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL151864 | — | Ki | = | 387.0 | nM | 6.41 |
| CHEMBL151717 | — | Ki | = | 419.0 | nM | 6.38 |
| CHEMBL348466 | — | Ki | = | 589.0 | nM | 6.23 |
| CHEMBL346659 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL357526 | — | Ki | = | 679.0 | nM | 6.17 |
| CHEMBL151504 | — | Ki | = | 2380.0 | nM | 5.62 |
| CHEMBL274016 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL151167 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL74909 | — | Ki | = | 4640.0 | nM | 5.33 |
| CHEMBL359165 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL15848 | ANANDAMIDE | Ki | = | 5810.0 | nM | 5.24 |
| CHEMBL346428 | — | Ki | = | 8090.0 | nM | 5.09 |
| CHEMBL151068 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL356213 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL151084 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL149859 | LINOLEOYLETHANOLAMIDE | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | Ki | = | 44000.0 | nM | 4.36 |