Assay Detail
Functional
CHEMBL3784643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse TRH-R1 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 (CHEMBL2467) ↗| 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 | 6.99 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 9.00 |
| CHEMBL3780746 | — | — | 1 | 8.47 |
| CHEMBL3782037 | — | — | 1 | 8.31 |
| CHEMBL3780645 | — | — | 1 | 8.23 |
| CHEMBL3779931 | — | — | 1 | 7.92 |
| CHEMBL3780373 | — | — | 1 | 7.50 |
| CHEMBL3780549 | — | — | 1 | 7.28 |
| CHEMBL3780802 | — | — | 1 | 6.60 |
| CHEMBL3780633 | — | — | 1 | 6.57 |
| CHEMBL3781773 | — | — | 1 | 6.47 |
| CHEMBL3781522 | — | — | 1 | 6.10 |
| CHEMBL3780191 | — | — | 1 | 5.62 |
| CHEMBL3780836 | — | — | 1 | 5.22 |
| CHEMBL3780248 | — | — | 1 | 4.58 |
| CHEMBL3781024 | — | — | 1 | - |
| CHEMBL3781873 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3780746 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3782037 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3780645 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3779931 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3780373 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3780549 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3780802 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL3780633 | — | EC50 | = | 272.0 | nM | 6.57 |
| CHEMBL3781773 | — | EC50 | = | 339.0 | nM | 6.47 |
| CHEMBL3781522 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3780191 | — | EC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3780836 | — | EC50 | = | 5970.0 | nM | 5.22 |
| CHEMBL3780248 | — | EC50 | = | 26270.0 | nM | 4.58 |
| CHEMBL3781024 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL3781873 | — | EC50 | > | 50000.0 | nM | - |