Assay Detail
Functional
CHEMBL3602665
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Agonist activity at mouse TRH-R2 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 2 (CHEMBL3600274) ↗| 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 | 7.26 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 9.28 |
| CHEMBL3600449 | — | — | 1 | 8.40 |
| CHEMBL3601782 | — | — | 1 | 8.22 |
| CHEMBL3600447 | — | — | 1 | 7.82 |
| CHEMBL3600445 | — | — | 1 | 7.52 |
| CHEMBL3601785 | — | — | 1 | 7.52 |
| CHEMBL3601781 | — | — | 1 | 7.40 |
| CHEMBL3600452 | — | — | 1 | 7.32 |
| CHEMBL3600453 | — | — | 1 | 7.30 |
| CHEMBL3600444 | — | — | 1 | 7.30 |
| CHEMBL3600446 | — | — | 1 | 7.22 |
| CHEMBL3600454 | — | — | 1 | 7.00 |
| CHEMBL3600448 | — | — | 1 | 6.92 |
| CHEMBL3601783 | — | — | 1 | 6.54 |
| CHEMBL3601784 | — | — | 1 | 6.51 |
| CHEMBL3600451 | — | — | 1 | 6.28 |
| CHEMBL3600450 | — | — | 1 | 6.11 |
| CHEMBL3601786 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | EC50 | = | 0.52 | nM | 9.28 |
| CHEMBL3600449 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3601782 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3600447 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3600445 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3601785 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3601781 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3600452 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3600453 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3600444 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3600446 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3600454 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3600448 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3601783 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3601784 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3600451 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3600450 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3601786 | — | EC50 | = | 960.0 | nM | 6.02 |