Assay Detail
Functional
CHEMBL2187017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | IMR-32 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and structure-activity relationships of novel pyrazolo[5,1-b]thiazole derivatives as potent and orally active corticotropin-releasing factor 1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.28 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309138 | — | — | 1 | 8.40 |
| CHEMBL2179195 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309138 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2179195 | — | IC50 | = | 7.1 | nM | 8.15 |