Assay Detail
Binding
CHEMBL5734652
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Intracellular cAMP Accumulation Assay: HEK293 cells stably expressing human APJ receptor were used to assess the activity of compounds. Cultured cells were detached and resuspended in the cAMP Homogeneous Time-Resolved Fluorescence (HTRF) assay buffer (Cisbio cat; #62AM4PEJ). The assay was performed in 384-well assay plates (Perkin-Elmer; cat #6008289) according to assay protocol provided by the manufacturer. Serial dilutions of a compound together with assay buffer containing 0.2 nM IBMX and 2 μM forskolin were added to each well containing 5,000 cells and incubated for 30 minutes at room temperature. Subsequently, cAMP D2 reagent was added in the lysis buffer followed by the EuK antibody (Cisbio; cat #62AM4PEJ) and incubated for 60 min. The fluorescence emission ratio was measured using fluorometer. The intracellular cAMP concentrations (compound-stimulated inhibition of forskolin-mediated cAMP production) were calculated by extrapolation from a standard curve using known cAMP concentrations. The EC50 values were obtained by fitting the data to a sigmoidal concentration-response curve with variable slope. The maximal achievable inhibition of forskolin-induced cAMP levels (Ymax) for each compound was expressed as relative percentage of inhibition attained using pyroglutamated apelin-13 ((Pyrl)apelin-13) peptide, which was set to 100%.
1593
Total Activities
513
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
6-hydroxy-5-(phenyl/heteroarylsulfonyl)pyrimidin-4(1H)-one as APJ agonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 531 | 8.18 | 8.30 |
| kon | 531 | - | - |
| k_off | 531 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5948209 | — | — | 3 | 8.30 |
| CHEMBL5948568 | — | — | 3 | 8.30 |
| CHEMBL5919446 | — | — | 3 | 8.30 |
| CHEMBL5890083 | — | — | 3 | 8.30 |
| CHEMBL5768207 | — | — | 3 | 8.30 |
| CHEMBL5988374 | — | — | 3 | 8.30 |
| CHEMBL4878056 | — | — | 3 | 8.30 |
| CHEMBL5994351 | — | — | 3 | 8.30 |
| CHEMBL4851100 | — | — | 3 | 8.30 |
| CHEMBL6009819 | — | — | 3 | 8.30 |
| CHEMBL5972562 | — | — | 3 | 8.30 |
| CHEMBL5790057 | — | — | 3 | 8.30 |
| CHEMBL5908769 | — | — | 3 | 8.30 |
| CHEMBL5748736 | — | — | 3 | 8.30 |
| CHEMBL6063247 | — | — | 3 | 8.30 |
| CHEMBL4877813 | — | — | 3 | 8.30 |
| CHEMBL5991898 | — | — | 3 | 8.30 |
| CHEMBL5828396 | — | — | 3 | 8.30 |
| CHEMBL6042643 | — | — | 3 | 8.30 |
| CHEMBL4855004 | — | — | 3 | 8.30 |
| CHEMBL5751784 | — | — | 3 | 8.30 |
| CHEMBL4855918 | — | — | 3 | 8.30 |
| CHEMBL5805771 | — | — | 3 | 8.30 |
| CHEMBL5984642 | — | — | 3 | 8.30 |
| CHEMBL5879354 | — | — | 3 | 8.30 |
| CHEMBL5841145 | — | — | 3 | 8.30 |
| CHEMBL5853659 | — | — | 3 | 8.30 |
| CHEMBL5787594 | — | — | 3 | 8.30 |
| CHEMBL5825512 | — | — | 3 | 8.30 |
| CHEMBL5782688 | — | — | 3 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5754140 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5846479 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5949606 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5756137 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5851741 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5925054 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5907526 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4859490 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5915783 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6049438 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5857942 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5918794 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5952409 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5950529 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5815819 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5918180 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5970034 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5943610 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6025439 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5801610 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5962039 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5771813 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5820425 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6026448 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5881556 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5814817 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5994240 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5868759 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5983445 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5896768 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5759263 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5991207 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5882265 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5840275 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6043287 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5907118 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5764966 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5953208 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5908552 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5999820 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5746943 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5850784 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5848315 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6038015 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5907449 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5954384 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6002077 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5850548 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5999807 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL6054014 | — | EC50 | = | 5.0 | nM | 8.30 |