Assay Detail
Binding
CHEMBL1049259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 57 | 6.85 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576549 | — | — | 1 | 8.89 |
| CHEMBL574480 | — | — | 1 | 8.80 |
| CHEMBL272203 | — | — | 1 | 8.77 |
| CHEMBL573546 | — | — | 1 | 8.62 |
| CHEMBL579249 | — | — | 1 | 8.38 |
| CHEMBL381689 | SR-144528 | — | 1 | 8.27 |
| CHEMBL574270 | — | — | 1 | 8.24 |
| CHEMBL577165 | — | — | 1 | 7.92 |
| CHEMBL575395 | — | — | 1 | 7.92 |
| CHEMBL575382 | — | — | 1 | 7.92 |
| CHEMBL578848 | — | — | 1 | 7.70 |
| CHEMBL572887 | — | — | 1 | 7.70 |
| CHEMBL572613 | — | — | 1 | 7.10 |
| CHEMBL574052 | — | — | 1 | 7.10 |
| CHEMBL575193 | — | — | 1 | 7.00 |
| CHEMBL572860 | — | — | 1 | 6.96 |
| CHEMBL285932 | — | — | 1 | 6.95 |
| CHEMBL579247 | — | — | 1 | 6.77 |
| CHEMBL572620 | — | — | 1 | 6.70 |
| CHEMBL573805 | — | — | 1 | 6.51 |
| CHEMBL574970 | — | — | 1 | 6.43 |
| CHEMBL574965 | — | — | 1 | 6.26 |
| CHEMBL574959 | — | — | 1 | 6.21 |
| CHEMBL585177 | — | — | 1 | 6.18 |
| CHEMBL574036 | — | — | 1 | 6.14 |
| CHEMBL573098 | — | — | 1 | 6.13 |
| CHEMBL574740 | — | — | 1 | 6.10 |
| CHEMBL111 | RIMONABANT | 4.0 | 1 | 6.10 |
| CHEMBL577361 | — | — | 1 | 6.10 |
| CHEMBL576142 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576549 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL574480 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL272203 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL573546 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL579249 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL381689 | SR-144528 | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL574270 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL577165 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL575395 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL575382 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL578848 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL572887 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL572613 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL574052 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL575193 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL572860 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL285932 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL579247 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL572620 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL573805 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL574970 | — | Ki | = | 373.0 | nM | 6.43 |
| CHEMBL574965 | — | Ki | = | 553.0 | nM | 6.26 |
| CHEMBL574959 | — | Ki | = | 609.0 | nM | 6.21 |
| CHEMBL585177 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL574036 | — | Ki | = | 721.0 | nM | 6.14 |
| CHEMBL573098 | — | Ki | = | 739.0 | nM | 6.13 |
| CHEMBL111 | RIMONABANT | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL577361 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL574740 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL576142 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL574722 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL573087 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL575186 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL575163 | — | Ki | = | 1291.0 | nM | 5.89 |
| CHEMBL575164 | — | Ki | = | 1945.0 | nM | 5.71 |
| CHEMBL578003 | — | Ki | = | 2887.0 | nM | 5.54 |
| CHEMBL574053 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL573796 | — | Ki | = | 3483.0 | nM | 5.46 |
| CHEMBL410727 | — | Ki | = | 3940.0 | nM | 5.41 |
| CHEMBL573086 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL575401 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL576977 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL574971 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL574046 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL574499 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL574279 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL573099 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL576366 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL574031 | — | Ki | > | 3940.0 | nM | - |
| CHEMBL575178 | — | Ki | > | 3940.0 | nM | - |