Assay Detail
Binding
CHEMBL5737215
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay: Principle of the assay: The HTRF® assay kit was purchased from Cisbio-US, Inc. (Bedford, Mass.; Catalog #62AM4PEC). The HTRF® assay supported by the kit is a competitive immunoassay between endogenous cAMP produced by the CHO-K1 cells and tracer cAMP labeled with the dye d2. The tracer binding is visualized by a monoclonal anti-cAMP antibody labeled with Cryptate. The specific signal (i.e., fluorescence resonance energy transfer, FRET) is inversely proportional to the concentration of unlabeled cAMP in the standard or sample.
12
Total Activities
4
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
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.15 | 8.70 |
| kon | 4 | - | - |
| k_off | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6019262 | — | — | 3 | 8.70 |
| CHEMBL5852849 | — | — | 3 | 8.15 |
| CHEMBL6061566 | — | — | 3 | 7.96 |
| CHEMBL5779401 | — | — | 3 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6019262 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5852849 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL6061566 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5779401 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5852849 | — | kon | = | - | — | - |
| CHEMBL5852849 | — | k_off | = | - | s-1 | - |
| CHEMBL5779401 | — | kon | = | - | — | - |
| CHEMBL5779401 | — | k_off | = | - | s-1 | - |
| CHEMBL6061566 | — | kon | = | - | — | - |
| CHEMBL6061566 | — | k_off | = | - | s-1 | - |
| CHEMBL6019262 | — | kon | = | - | — | - |
| CHEMBL6019262 | — | k_off | = | - | s-1 | - |