Assay Detail
Functional
CHEMBL1785979
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Extracellular calcium-sensing receptor (CHEMBL1878) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of novel calcium sensing receptor negative allosteric modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.94 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783764 | — | — | 1 | 8.22 |
| CHEMBL1783935 | — | — | 1 | 7.75 |
| CHEMBL180672 | — | — | 1 | 7.64 |
| CHEMBL1783931 | — | — | 1 | 7.64 |
| CHEMBL1783933 | — | — | 1 | 7.60 |
| CHEMBL1783934 | — | — | 1 | 7.30 |
| CHEMBL1783762 | — | — | 1 | 7.25 |
| CHEMBL1198855 | RONACALERET | 2.0 | 1 | 6.84 |
| CHEMBL1783766 | — | — | 1 | 6.52 |
| CHEMBL1783932 | — | — | 1 | 6.46 |
| CHEMBL1783763 | — | — | 1 | 6.05 |
| CHEMBL1783765 | — | — | 1 | 5.46 |
| CHEMBL1783936 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783764 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1783935 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL180672 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1783931 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1783933 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1783934 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1783762 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1198855 | RONACALERET | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL1783766 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1783932 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1783763 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1783765 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1783936 | — | IC50 | = | 3500.0 | nM | 5.46 |