Assay Detail
Functional
CHEMBL4840247
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
23
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of 6-Hydroxypyrimidin-4(1<i>H</i>)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 9.11 | 10.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861895 | — | — | 1 | 10.64 |
| CHEMBL4854412 | — | — | 1 | 10.57 |
| CHEMBL4867145 | — | — | 1 | 10.49 |
| CHEMBL3184840 | — | — | 1 | 10.30 |
| CHEMBL4874120 | — | — | 2 | 9.92 |
| CHEMBL4854048 | — | — | 2 | 9.82 |
| CHEMBL4855254 | — | — | 1 | 9.66 |
| CHEMBL4866732 | AZELAPRAG | 1.0 | 1 | 9.64 |
| CHEMBL4872407 | — | — | 1 | 9.59 |
| CHEMBL4863297 | — | — | 2 | 9.54 |
| CHEMBL4870497 | — | — | 1 | 9.36 |
| CHEMBL4851693 | — | — | 1 | 9.00 |
| CHEMBL4875108 | — | — | 2 | 8.82 |
| CHEMBL4869091 | — | — | 1 | 8.74 |
| CHEMBL4856612 | — | — | 1 | 8.03 |
| CHEMBL4845664 | — | — | 1 | 6.92 |
| CHEMBL4848469 | — | — | 1 | 5.96 |
| CHEMBL4854830 | — | — | 1 | 5.96 |
| CHEMBL4863722 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861895 | — | EC50 | = | 0.023 | nM | 10.64 |
| CHEMBL4854412 | — | EC50 | = | 0.027 | nM | 10.57 |
| CHEMBL4867145 | — | EC50 | = | 0.032 | nM | 10.49 |
| CHEMBL3184840 | — | EC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4874120 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4854048 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4874120 | — | EC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4855254 | — | EC50 | = | 0.22 | nM | 9.66 |
| CHEMBL4866732 | AZELAPRAG | EC50 | = | 0.23 | nM | 9.64 |
| CHEMBL4854048 | — | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4872407 | — | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL4863297 | — | EC50 | = | 0.29 | nM | 9.54 |
| CHEMBL4863297 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4870497 | — | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL4851693 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4875108 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4869091 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4875108 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4856612 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4845664 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4854830 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4848469 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4863722 | — | EC50 | > | 30000.0 | nM | - |