Assay Detail
Functional
CHEMBL2378664
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay
31
Total Activities
31
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
New potent calcimimetics: II. Discovery of benzothiazole trisubstituted ureas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 31 | 6.88 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2377735 | — | — | 1 | 7.70 |
| CHEMBL2377740 | — | — | 1 | 7.70 |
| CHEMBL2377741 | — | — | 1 | 7.52 |
| CHEMBL2377743 | — | — | 1 | 7.52 |
| CHEMBL2377749 | — | — | 1 | 7.52 |
| CHEMBL2377748 | — | — | 1 | 7.52 |
| CHEMBL2377744 | — | — | 1 | 7.40 |
| CHEMBL2377736 | — | — | 1 | 7.22 |
| CHEMBL2377746 | — | — | 1 | 7.22 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | 2.0 | 1 | 7.10 |
| CHEMBL2377739 | — | — | 1 | 7.10 |
| CHEMBL2377747 | — | — | 1 | 7.10 |
| CHEMBL2377752 | — | — | 1 | 7.10 |
| CHEMBL2377727 | — | — | 1 | 7.10 |
| CHEMBL2377745 | — | — | 1 | 7.05 |
| CHEMBL2375383 | — | — | 1 | 7.00 |
| CHEMBL2377737 | — | — | 1 | 6.82 |
| CHEMBL2377732 | — | — | 1 | 6.70 |
| CHEMBL2377730 | — | — | 1 | 6.70 |
| CHEMBL2375386 | — | — | 1 | 6.70 |
| CHEMBL2377750 | — | — | 1 | 6.70 |
| CHEMBL2377751 | — | — | 1 | 6.70 |
| CHEMBL2377738 | — | — | 1 | 6.52 |
| CHEMBL2377731 | — | — | 1 | 6.52 |
| CHEMBL2377734 | — | — | 1 | 6.40 |
| CHEMBL2377729 | — | — | 1 | 6.40 |
| CHEMBL2377728 | — | — | 1 | 6.35 |
| CHEMBL2377742 | — | — | 1 | 6.22 |
| CHEMBL2375385 | — | — | 1 | 6.00 |
| CHEMBL2377726 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2377735 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2377740 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2377741 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2377743 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2377749 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2377748 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2377744 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2377736 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2377746 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2107572 | TECALCET HYDROCHLORIDE | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2377739 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2377747 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2377752 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2377727 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2377745 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2375383 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2377737 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2377732 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2377730 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2375386 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2377750 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2377751 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2377738 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2377731 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2377734 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2377729 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2377728 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2377742 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2375385 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2377726 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2377733 | — | EC50 | = | 1700.0 | nM | 5.77 |