Assay Detail
Binding
CHEMBL1811340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | IMR-32 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.26 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475306 | — | — | 1 | 8.38 |
| CHEMBL270948 | — | — | 1 | 8.29 |
| CHEMBL482950 | PEXACERFONT | 3.0 | 1 | 8.21 |
| CHEMBL270738 | — | — | 1 | 8.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475306 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL270948 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL482950 | PEXACERFONT | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL270738 | — | IC50 | = | 6.8 | nM | 8.17 |