Assay Detail
Functional
CHEMBL4823532
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
36
Total Activities
36
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
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 6.60 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3184840 | — | — | 1 | 9.52 |
| CHEMBL4867710 | — | — | 1 | 9.00 |
| CHEMBL4851755 | — | — | 1 | 8.30 |
| CHEMBL4849104 | — | — | 1 | 8.10 |
| CHEMBL4857978 | — | — | 1 | 8.05 |
| CHEMBL4846191 | — | — | 1 | 7.48 |
| CHEMBL4850375 | — | — | 1 | 7.03 |
| CHEMBL4647910 | — | — | 1 | 7.01 |
| CHEMBL4850694 | — | — | 1 | 6.98 |
| CHEMBL4876051 | — | — | 1 | 6.87 |
| CHEMBL4875417 | — | — | 1 | 6.79 |
| CHEMBL4873660 | — | — | 1 | 6.78 |
| CHEMBL4856959 | — | — | 1 | 6.74 |
| CHEMBL4859298 | — | — | 1 | 6.71 |
| CHEMBL4862328 | — | — | 1 | 6.62 |
| CHEMBL4863277 | — | — | 1 | 6.62 |
| CHEMBL4641469 | — | — | 1 | 6.62 |
| CHEMBL4864641 | — | — | 1 | 6.54 |
| CHEMBL4861663 | — | — | 1 | 6.45 |
| CHEMBL4863764 | — | — | 1 | 6.44 |
| CHEMBL4847403 | — | — | 1 | 6.40 |
| CHEMBL4854216 | — | — | 1 | 6.16 |
| CHEMBL4851385 | — | — | 1 | 6.15 |
| CHEMBL4857246 | — | — | 1 | 6.14 |
| CHEMBL4868247 | — | — | 1 | 6.11 |
| CHEMBL4875648 | — | — | 1 | 6.09 |
| CHEMBL3817879 | — | — | 1 | 6.07 |
| CHEMBL4865671 | — | — | 1 | 5.93 |
| CHEMBL4869477 | — | — | 1 | 5.87 |
| CHEMBL4852570 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3184840 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4867710 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4851755 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4849104 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4857978 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4846191 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4850375 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4647910 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4850694 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4876051 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4875417 | — | EC50 | = | 162.0 | nM | 6.79 |
| CHEMBL4873660 | — | EC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4856959 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4859298 | — | EC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4641469 | — | EC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4862328 | — | EC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4863277 | — | EC50 | = | 237.0 | nM | 6.62 |
| CHEMBL4864641 | — | EC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4861663 | — | EC50 | = | 352.0 | nM | 6.45 |
| CHEMBL4863764 | — | EC50 | = | 363.0 | nM | 6.44 |
| CHEMBL4847403 | — | EC50 | = | 398.0 | nM | 6.40 |
| CHEMBL4854216 | — | EC50 | = | 693.0 | nM | 6.16 |
| CHEMBL4851385 | — | EC50 | = | 703.0 | nM | 6.15 |
| CHEMBL4857246 | — | EC50 | = | 721.0 | nM | 6.14 |
| CHEMBL4868247 | — | EC50 | = | 779.0 | nM | 6.11 |
| CHEMBL4875648 | — | EC50 | = | 805.0 | nM | 6.09 |
| CHEMBL3817879 | — | EC50 | = | 844.0 | nM | 6.07 |
| CHEMBL4865671 | — | EC50 | = | 1185.0 | nM | 5.93 |
| CHEMBL4869477 | — | EC50 | = | 1365.0 | nM | 5.87 |
| CHEMBL4852570 | — | EC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL4858793 | — | EC50 | = | 2112.0 | nM | 5.67 |
| CHEMBL4856227 | — | EC50 | = | 2411.0 | nM | 5.62 |
| CHEMBL4870280 | — | EC50 | = | 2642.0 | nM | 5.58 |
| CHEMBL4865583 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4866809 | — | EC50 | = | 5892.0 | nM | 5.23 |
| CHEMBL4851809 | — | EC50 | = | 7562.0 | nM | 5.12 |