Assay Detail
Functional
CHEMBL1647712
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Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]-GTPgammaS binding
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 7.87 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381689 | SR-144528 | — | 1 | 8.74 |
| CHEMBL1641948 | — | — | 1 | 8.72 |
| CHEMBL1641947 | — | — | 1 | 8.72 |
| CHEMBL1641945 | — | — | 1 | 8.49 |
| CHEMBL1641936 | — | — | 1 | 8.26 |
| CHEMBL1641943 | — | — | 1 | 8.24 |
| CHEMBL559612 | CP-55940 | — | 1 | 8.21 |
| CHEMBL1641940 | — | — | 1 | 8.19 |
| CHEMBL1641944 | — | — | 1 | 8.13 |
| CHEMBL1641938 | — | — | 1 | 8.11 |
| CHEMBL1641946 | — | — | 1 | 8.06 |
| CHEMBL1641942 | — | — | 1 | 7.96 |
| CHEMBL1641937 | — | — | 1 | 7.91 |
| CHEMBL1641951 | — | — | 1 | 7.85 |
| CHEMBL1641959 | — | — | 1 | 7.77 |
| CHEMBL1641953 | — | — | 1 | 7.66 |
| CHEMBL1641952 | — | — | 1 | 7.64 |
| CHEMBL188 | WIN-552122 | — | 1 | 7.61 |
| CHEMBL1641962 | — | — | 1 | 7.60 |
| CHEMBL1641950 | — | — | 1 | 7.58 |
| CHEMBL1641960 | — | — | 1 | 7.57 |
| CHEMBL1641949 | — | — | 1 | 7.22 |
| CHEMBL1641963 | — | — | 1 | 6.84 |
| CHEMBL1641954 | — | — | 1 | 6.80 |
| CHEMBL1641961 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381689 | SR-144528 | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1641948 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1641947 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1641945 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1641936 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL1641943 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL559612 | CP-55940 | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL1641940 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1641944 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1641938 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL1641946 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL1641942 | — | EC50 | = | 10.9 | nM | 7.96 |
| CHEMBL1641937 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL1641951 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1641959 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1641953 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1641952 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL188 | WIN-552122 | EC50 | = | 24.6 | nM | 7.61 |
| CHEMBL1641962 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1641950 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1641960 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1641949 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1641963 | — | EC50 | = | 145.6 | nM | 6.84 |
| CHEMBL1641954 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL1641961 | — | EC50 | = | 164.0 | nM | 6.79 |