Assay Detail
Binding
CHEMBL3784640
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| IC50 | 16 | 5.63 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 7.58 |
| CHEMBL3780746 | — | — | 1 | 6.77 |
| CHEMBL3780645 | — | — | 1 | 6.49 |
| CHEMBL3782037 | — | — | 1 | 5.93 |
| CHEMBL3779931 | — | — | 1 | 4.73 |
| CHEMBL3780248 | — | — | 1 | 4.69 |
| CHEMBL3780802 | — | — | 1 | 4.53 |
| CHEMBL3780633 | — | — | 1 | 4.32 |
| CHEMBL3781873 | — | — | 1 | - |
| CHEMBL3780549 | — | — | 1 | - |
| CHEMBL3780191 | — | — | 1 | - |
| CHEMBL3780836 | — | — | 1 | - |
| CHEMBL3781773 | — | — | 1 | - |
| CHEMBL3781024 | — | — | 1 | - |
| CHEMBL3780373 | — | — | 1 | - |
| CHEMBL3781522 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3780746 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3780645 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL3782037 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL3779931 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL3780248 | — | IC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL3780802 | — | IC50 | = | 29340.0 | nM | 4.53 |
| CHEMBL3780633 | — | IC50 | = | 48030.0 | nM | 4.32 |
| CHEMBL3781873 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3780549 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3780191 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3780836 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3781773 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3781024 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3780373 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3781522 | — | IC50 | > | 50000.0 | nM | - |