Assay Detail
Binding
CHEMBL659689
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Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the presence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand
23
Total Activities
23
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 | 23 | 6.83 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL151167 | — | — | 1 | 8.28 |
| CHEMBL274016 | — | — | 1 | 8.00 |
| CHEMBL359165 | — | — | 1 | 7.97 |
| CHEMBL120526 | METHANANDAMIDE | — | 1 | 7.75 |
| CHEMBL151864 | — | — | 1 | 7.59 |
| CHEMBL74909 | — | — | 1 | 7.57 |
| CHEMBL330974 | — | — | 1 | 7.45 |
| CHEMBL151504 | — | — | 1 | 7.44 |
| CHEMBL150942 | — | — | 1 | 7.29 |
| CHEMBL15848 | ANANDAMIDE | — | 1 | 7.21 |
| CHEMBL359278 | — | — | 1 | 7.13 |
| CHEMBL151496 | — | — | 1 | 7.08 |
| CHEMBL421967 | — | — | 1 | 7.04 |
| CHEMBL150849 | — | — | 1 | 6.94 |
| CHEMBL346659 | — | — | 1 | 6.89 |
| CHEMBL149691 | — | — | 1 | 6.82 |
| CHEMBL151862 | — | — | 1 | 6.54 |
| CHEMBL348466 | — | — | 1 | 6.51 |
| CHEMBL151717 | — | — | 1 | 6.38 |
| CHEMBL149859 | LINOLEOYLETHANOLAMIDE | — | 1 | 5.00 |
| CHEMBL151084 | — | — | 1 | 4.72 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | — | 1 | 4.70 |
| CHEMBL356213 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL151167 | — | Ki | = | 5.29 | nM | 8.28 |
| CHEMBL274016 | — | Ki | = | 9.91 | nM | 8.00 |
| CHEMBL359165 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL120526 | METHANANDAMIDE | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL151864 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL74909 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL330974 | — | Ki | = | 35.6 | nM | 7.45 |
| CHEMBL151504 | — | Ki | = | 36.2 | nM | 7.44 |
| CHEMBL150942 | — | Ki | = | 51.2 | nM | 7.29 |
| CHEMBL15848 | ANANDAMIDE | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL359278 | — | Ki | = | 73.6 | nM | 7.13 |
| CHEMBL151496 | — | Ki | = | 83.2 | nM | 7.08 |
| CHEMBL421967 | — | Ki | = | 90.2 | nM | 7.04 |
| CHEMBL150849 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL346659 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL149691 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL151862 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL348466 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL151717 | — | Ki | = | 421.0 | nM | 6.38 |
| CHEMBL149859 | LINOLEOYLETHANOLAMIDE | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL151084 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL280065 | OLEOYLETHANOLAMIDE | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL356213 | — | Ki | = | 21000.0 | nM | 4.68 |