Assay Detail
Functional
CHEMBL3602664
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Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method
18
Total Activities
18
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 of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 6.20 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 9.00 |
| CHEMBL3600447 | — | — | 1 | 7.77 |
| CHEMBL3600454 | — | — | 1 | 7.11 |
| CHEMBL3600446 | — | — | 1 | 6.82 |
| CHEMBL3601782 | — | — | 1 | 6.54 |
| CHEMBL3601785 | — | — | 1 | 6.47 |
| CHEMBL3601781 | — | — | 1 | 6.30 |
| CHEMBL3600444 | — | — | 1 | 6.13 |
| CHEMBL3600449 | — | — | 1 | 6.03 |
| CHEMBL3600445 | — | — | 1 | 6.01 |
| CHEMBL3600450 | — | — | 1 | 6.00 |
| CHEMBL3601783 | — | — | 1 | 5.85 |
| CHEMBL3600448 | — | — | 1 | 5.81 |
| CHEMBL3600453 | — | — | 1 | 5.59 |
| CHEMBL3600452 | — | — | 1 | 5.40 |
| CHEMBL3601786 | — | — | 1 | 5.14 |
| CHEMBL3601784 | — | — | 1 | 4.95 |
| CHEMBL3600451 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3600447 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3600454 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3600446 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3601782 | — | EC50 | = | 287.0 | nM | 6.54 |
| CHEMBL3601785 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3601781 | — | EC50 | = | 498.0 | nM | 6.30 |
| CHEMBL3600444 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3600449 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3600445 | — | EC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3600450 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3601783 | — | EC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL3600448 | — | EC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL3600453 | — | EC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL3600452 | — | EC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL3601786 | — | EC50 | = | 7210.0 | nM | 5.14 |
| CHEMBL3601784 | — | EC50 | = | 11280.0 | nM | 4.95 |
| CHEMBL3600451 | — | EC50 | = | 19350.0 | nM | 4.71 |