Assay Detail
Functional
CHEMBL866784
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Extracellular calcium-sensing receptor (CHEMBL2516) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
N1-Benzoyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.90 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL536975 | — | — | 1 | 6.60 |
| CHEMBL537870 | — | — | 1 | 6.48 |
| CHEMBL180672 | — | — | 1 | 6.34 |
| CHEMBL557567 | — | — | 1 | 6.05 |
| CHEMBL556781 | — | — | 1 | 5.77 |
| CHEMBL537427 | — | — | 1 | 5.58 |
| CHEMBL537426 | — | — | 1 | 5.27 |
| CHEMBL559185 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL536975 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL537870 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL180672 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL557567 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL556781 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL537427 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL537426 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL559185 | — | IC50 | = | 8000.0 | nM | 5.10 |