Assay Detail
Functional
CHEMBL3784644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Thyrotropin-releasing hormone receptor 2 (CHEMBL3600274) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.09 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3782037 | — | — | 1 | 10.00 |
| CHEMBL3780645 | — | — | 1 | 9.40 |
| CHEMBL3780746 | — | — | 1 | 9.34 |
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 9.30 |
| CHEMBL3780633 | — | — | 1 | 9.00 |
| CHEMBL3780373 | — | — | 1 | 8.89 |
| CHEMBL3779931 | — | — | 1 | 8.84 |
| CHEMBL3781773 | — | — | 1 | 7.57 |
| CHEMBL3780549 | — | — | 1 | 7.52 |
| CHEMBL3780802 | — | — | 1 | 7.42 |
| CHEMBL3781522 | — | — | 1 | 7.06 |
| CHEMBL3780191 | — | — | 1 | 6.69 |
| CHEMBL3780836 | — | — | 1 | 6.44 |
| CHEMBL3780248 | — | — | 1 | 5.72 |
| CHEMBL3781024 | — | — | 1 | - |
| CHEMBL3781873 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3782037 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3780645 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3780746 | — | EC50 | = | 0.46 | nM | 9.34 |
| CHEMBL1472 | PROTIRELIN | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3780633 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3780373 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3779931 | — | EC50 | = | 1.46 | nM | 8.84 |
| CHEMBL3781773 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3780549 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3780802 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3781522 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3780191 | — | EC50 | = | 206.0 | nM | 6.69 |
| CHEMBL3780836 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3780248 | — | EC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL3781024 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL3781873 | — | EC50 | > | 50000.0 | nM | - |