Assay Detail
Functional
CHEMBL4122629
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Extracellular calcium-sensing receptor (CHEMBL1878) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.55 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126450 | — | — | 1 | 7.77 |
| CHEMBL4126877 | — | — | 1 | 7.30 |
| CHEMBL4128835 | — | — | 1 | 7.03 |
| CHEMBL4129011 | — | — | 1 | 6.92 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | 4.0 | 1 | 6.75 |
| CHEMBL4128542 | — | — | 1 | 6.72 |
| CHEMBL4129371 | — | — | 1 | 6.64 |
| CHEMBL4126482 | — | — | 1 | 6.54 |
| CHEMBL4126057 | — | — | 1 | 6.50 |
| CHEMBL4125917 | — | — | 1 | 6.42 |
| CHEMBL4125688 | — | — | 1 | 6.37 |
| CHEMBL4127153 | — | — | 1 | 6.35 |
| CHEMBL4130093 | — | — | 1 | 6.22 |
| CHEMBL4125724 | — | — | 1 | 6.22 |
| CHEMBL4130141 | — | — | 1 | 5.96 |
| CHEMBL4127295 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126450 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4126877 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4128835 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4129011 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1200776 | CINACALCET HYDROCHLORIDE | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4128542 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4129371 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4126482 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4126057 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4125917 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4125688 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4127153 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4130093 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4125724 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4130141 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4127295 | — | EC50 | = | 8800.0 | nM | 5.06 |