Assay Detail
Functional
CHEMBL985714
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.12 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL484158 | — | — | 1 | 7.44 |
| CHEMBL483993 | — | — | 1 | 7.42 |
| CHEMBL475306 | — | — | 1 | 7.18 |
| CHEMBL506214 | — | — | 1 | 6.96 |
| CHEMBL526149 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL484158 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL483993 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL475306 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL506214 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL526149 | — | IC50 | = | 264.0 | nM | 6.58 |