Assay Detail
Binding
CHEMBL917826
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Displacement of [3H]N(1)-Me-His-TRH from TRHR1
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 18 | 7.37 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL224730 | — | — | 1 | 8.52 |
| CHEMBL223972 | — | — | 1 | 8.49 |
| CHEMBL390942 | — | — | 1 | 7.96 |
| CHEMBL1472 | PROTIRELIN | 4.0 | 1 | 7.70 |
| CHEMBL224525 | — | — | 1 | 6.40 |
| CHEMBL388528 | — | — | 1 | 5.12 |
| CHEMBL389037 | — | — | 1 | - |
| CHEMBL388812 | — | — | 1 | - |
| CHEMBL224655 | — | — | 1 | - |
| CHEMBL437735 | — | — | 1 | - |
| CHEMBL374625 | — | — | 1 | - |
| CHEMBL223876 | — | — | 1 | - |
| CHEMBL389858 | — | — | 1 | - |
| CHEMBL375196 | — | — | 1 | - |
| CHEMBL224715 | — | — | 1 | - |
| CHEMBL388350 | — | — | 1 | - |
| CHEMBL389955 | — | — | 1 | - |
| CHEMBL376135 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL224730 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL223972 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL390942 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1472 | PROTIRELIN | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL224525 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL388528 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL389037 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL388812 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL224655 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL437735 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL374625 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL223876 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL389858 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL375196 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL224715 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL388350 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL389955 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL376135 | — | Ki | > | 100000.0 | nM | - |