Assay Detail
Binding
CHEMBL3887286
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CB2 Receptor Binding Protocol: 15.3 ug of membranes (20 ul of 1:20 dilution in incubation buffer) was incubated with 5 ul of drug solution (10E-4M to 10E-12M) and 5ul of 5.4 nM [3H]CP55,940 in a total volume of 200 ul for 90 mins at 30 C. Non-specific binding was determined using 10 uM WIN55,212-2 (Ki=4.4 nM). The membranes were filtered and the filters washed 7x with 0.2 ml ice-cold incubation buffer and allowed to air dry under vacuum.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Tri-aryl/heteroaromatic cannabinoids and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.12 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076685 | — | — | 1 | 9.57 |
| CHEMBL525067 | — | — | 1 | 8.97 |
| CHEMBL3950898 | — | — | 1 | 8.85 |
| CHEMBL460544 | — | — | 1 | 8.78 |
| CHEMBL3937621 | — | — | 1 | 8.76 |
| CHEMBL3922001 | — | — | 1 | 8.64 |
| CHEMBL1081624 | — | — | 1 | 8.63 |
| CHEMBL460545 | — | — | 1 | 8.53 |
| CHEMBL3915185 | — | — | 1 | 8.33 |
| CHEMBL460754 | — | — | 1 | 8.32 |
| CHEMBL3959623 | — | — | 1 | 8.24 |
| CHEMBL3928596 | — | — | 1 | 7.43 |
| CHEMBL3923170 | — | — | 1 | 7.09 |
| CHEMBL3907723 | — | — | 1 | 6.80 |
| CHEMBL3967280 | — | — | 1 | 6.65 |
| CHEMBL3978261 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076685 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL525067 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL3950898 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL460544 | — | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL3937621 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL3922001 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1081624 | — | Ki | = | 2.32 | nM | 8.63 |
| CHEMBL460545 | — | Ki | = | 2.94 | nM | 8.53 |
| CHEMBL3915185 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL460754 | — | Ki | = | 4.77 | nM | 8.32 |
| CHEMBL3959623 | — | Ki | = | 5.69 | nM | 8.24 |
| CHEMBL3928596 | — | Ki | = | 37.18 | nM | 7.43 |
| CHEMBL3923170 | — | Ki | = | 81.95 | nM | 7.09 |
| CHEMBL3907723 | — | Ki | = | 159.09 | nM | 6.80 |
| CHEMBL3967280 | — | Ki | = | 224.98 | nM | 6.65 |
| CHEMBL3978261 | — | Ki | = | 454.0 | nM | 6.34 |