Assay Detail
Functional
CHEMBL1039645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assay
18
Total Activities
18
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 | Intermediate |
Target
Extracellular calcium-sensing receptor (CHEMBL1878) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.64 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569182 | — | — | 1 | 7.64 |
| CHEMBL571476 | — | — | 1 | 7.39 |
| CHEMBL577333 | — | — | 1 | 7.24 |
| CHEMBL569863 | — | — | 1 | 7.16 |
| CHEMBL568485 | — | — | 1 | 7.04 |
| CHEMBL572363 | — | — | 1 | 6.83 |
| CHEMBL292376 | TECALCET | 2.0 | 1 | 6.71 |
| CHEMBL583522 | — | — | 1 | 6.63 |
| CHEMBL577306 | — | — | 1 | 5.93 |
| CHEMBL571048 | — | — | 1 | 5.80 |
| CHEMBL583469 | — | — | 1 | 5.72 |
| CHEMBL572362 | — | — | 1 | 5.63 |
| CHEMBL568947 | — | — | 1 | - |
| CHEMBL566524 | — | — | 1 | - |
| CHEMBL572172 | — | — | 1 | - |
| CHEMBL571047 | — | — | 1 | - |
| CHEMBL568946 | — | — | 1 | - |
| CHEMBL566747 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569182 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL571476 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL577333 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL569863 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL568485 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL572363 | — | EC50 | = | 148.0 | nM | 6.83 |
| CHEMBL292376 | TECALCET | EC50 | = | 194.0 | nM | 6.71 |
| CHEMBL583522 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL577306 | — | EC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL571048 | — | EC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL583469 | — | EC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL572362 | — | EC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL568947 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566524 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL572172 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL571047 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL568946 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL566747 | — | EC50 | > | 5000.0 | nM | - |