Target & Activity
| Target | Activity | Value |
|---|---|---|
| CB1 | pEC50 | 8.24 |
Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| CHO | EC50 | 83 nM | Positive allosteric modulator activity at human CB1R expressed in CHO cells assessed as enhanced binding of [3H]CP55,940 after 60 mins by liquid scintillation spectrometric analysis | [PMID: 26529344] |
| CHO-K1 | IC50 | 2 nM | Negative allosteric modulation of human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940 induced beta arrestin recruitment preincubated for 30 mins followed by addition of CP55940 for 90 mins by chemiluminescence assay | [PMID: 27542310] |
| CHO-K1 | EC50 | 324 nM | Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte | [PMID: 26529344] |
| CHO-K1 | EC50 | 9.05 nM | Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay | [PMID: 26529344] |
| HEK293 | EC50 | 0.64 μM | Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins in presence of CP55,940 by cAMP BRET assay | [PMID: 26203658] |
| HEK293 | EC50 | 10.59 μM | Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 5 mins in presence of CP55,940 by cAMP BRET assay | [PMID: 26203658] |
| HEK293 | EC50 | 2.09 μM | Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation after 10 mins in presence of CP55,940 by cAMP BRET assay | [PMID: 26203658] |
| HEK293 | EC50 | 2.24 μM | Activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as effect on forskolin-induced cAMP accumulation in presence of CP55,940 by cAMP BRET assay | [PMID: 26203658] |