Assay Detail
Functional
CHEMBL917828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293EM |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Thyrotropin-releasing hormone receptor (CHEMBL1810) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.07 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 8.52 |
| CHEMBL223972 | — | — | 1 | 8.31 |
| CHEMBL224730 | — | — | 1 | 8.30 |
| CHEMBL390942 | — | — | 1 | 7.85 |
| CHEMBL224525 | — | — | 1 | 6.42 |
| CHEMBL388528 | — | — | 1 | 5.29 |
| CHEMBL389037 | — | — | 1 | 4.77 |
| CHEMBL388812 | — | — | 1 | - |
| CHEMBL376135 | — | — | 1 | - |
| CHEMBL389955 | — | — | 1 | - |
| CHEMBL388350 | — | — | 1 | - |
| CHEMBL224715 | — | — | 1 | - |
| CHEMBL375196 | — | — | 1 | - |
| CHEMBL389858 | — | — | 1 | - |
| CHEMBL223876 | — | — | 1 | - |
| CHEMBL374625 | — | — | 1 | - |
| CHEMBL437735 | — | — | 1 | - |
| CHEMBL224655 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1472 | PROTIRELIN | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL223972 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL224730 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL390942 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL224525 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL388528 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL389037 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL388812 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL376135 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL389955 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL388350 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL224715 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL375196 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL389858 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL223876 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL374625 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL437735 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL224655 | — | EC50 | > | 100000.0 | nM | - |