Assay Detail
Functional
CHEMBL4041234
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Allosteric modulation of human CB1 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.80 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096928 | — | — | 1 | 7.75 |
| CHEMBL4067016 | — | — | 1 | 7.66 |
| CHEMBL4078901 | — | — | 1 | 7.64 |
| CHEMBL4077975 | — | — | 1 | 7.57 |
| CHEMBL4086756 | — | — | 1 | 7.52 |
| CHEMBL4070648 | — | — | 1 | 7.50 |
| CHEMBL3341861 | — | — | 1 | 7.48 |
| CHEMBL4089126 | — | — | 1 | 7.33 |
| CHEMBL4064299 | — | — | 1 | 7.16 |
| CHEMBL4085844 | — | — | 1 | 7.13 |
| CHEMBL4097779 | — | — | 1 | 7.09 |
| CHEMBL4094495 | — | — | 1 | 7.02 |
| CHEMBL4091847 | — | — | 1 | 6.88 |
| CHEMBL4078811 | — | — | 1 | 6.88 |
| CHEMBL4062376 | — | — | 1 | 6.87 |
| CHEMBL4064182 | — | — | 1 | 6.85 |
| CHEMBL4081259 | — | — | 1 | 6.75 |
| CHEMBL4102237 | — | — | 1 | 6.72 |
| CHEMBL4073727 | — | — | 1 | 6.71 |
| CHEMBL4093478 | — | — | 1 | 6.64 |
| CHEMBL4067924 | — | — | 1 | 6.61 |
| CHEMBL4105512 | — | — | 1 | 6.54 |
| CHEMBL4071010 | — | — | 1 | 6.48 |
| CHEMBL4104660 | — | — | 1 | 6.47 |
| CHEMBL4092811 | — | — | 1 | 6.34 |
| CHEMBL4099590 | — | — | 1 | 6.29 |
| CHEMBL4065139 | — | — | 1 | 6.23 |
| CHEMBL4085745 | — | — | 1 | 6.08 |
| CHEMBL4081586 | — | — | 1 | 5.90 |
| CHEMBL4096828 | — | — | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096928 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4067016 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4078901 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4077975 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4086756 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4070648 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3341861 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4089126 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4064299 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4085844 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4097779 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4094495 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4091847 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4078811 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4062376 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4064182 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4081259 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4102237 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4073727 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4093478 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4067924 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4105512 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4071010 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL4104660 | — | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL4092811 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4099590 | — | IC50 | = | 516.0 | nM | 6.29 |
| CHEMBL4065139 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL4085745 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4081586 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4096828 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4100542 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL4084091 | — | IC50 | = | 1570.0 | nM | 5.80 |