Assay Detail
Functional
CHEMBL4122630
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Agonist activity at CaSR in rat parathyroid cells assessed as inhibition of PTH (1 to 84 residues) production in presence of Cacl2 by ELISA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Extracellular calcium-sensing receptor (CHEMBL2516) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.17 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126450 | — | — | 1 | 9.33 |
| CHEMBL4126877 | — | — | 1 | 9.04 |
| CHEMBL4128542 | — | — | 1 | 8.85 |
| CHEMBL4125917 | — | — | 1 | 8.68 |
| CHEMBL4126057 | — | — | 1 | 8.37 |
| CHEMBL4129011 | — | — | 1 | 8.11 |
| CHEMBL4126482 | — | — | 1 | 8.10 |
| CHEMBL4125688 | — | — | 1 | 8.01 |
| CHEMBL4125724 | — | — | 1 | 7.93 |
| CHEMBL4127153 | — | — | 1 | 7.88 |
| CHEMBL4128835 | — | — | 1 | 7.51 |
| CHEMBL4130093 | — | — | 1 | 7.50 |
| CHEMBL4129371 | — | — | 1 | 6.94 |
| CHEMBL4130141 | — | — | 1 | - |
| CHEMBL4127295 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126450 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL4126877 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL4128542 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4125917 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4126057 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4129011 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4126482 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4125688 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4125724 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4127153 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL4128835 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL4130093 | — | IC50 | = | 31.8 | nM | 7.50 |
| CHEMBL4129371 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4130141 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4127295 | — | IC50 | - | — | - |