Assay Detail
Functional
CHEMBL2089414
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.08 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087562 | — | — | 1 | 7.70 |
| CHEMBL2087567 | — | — | 1 | 7.64 |
| CHEMBL2087574 | — | — | 1 | 7.52 |
| CHEMBL2087796 | — | — | 1 | 7.41 |
| CHEMBL2087575 | — | — | 1 | 7.30 |
| CHEMBL2087794 | — | — | 1 | 7.28 |
| CHEMBL2087553 | — | — | 1 | 7.23 |
| CHEMBL2087554 | — | — | 1 | 7.05 |
| CHEMBL2087550 | — | — | 1 | 7.00 |
| CHEMBL2087552 | — | — | 1 | 7.00 |
| CHEMBL2087573 | — | — | 1 | 6.96 |
| CHEMBL2087801 | — | — | 1 | 6.91 |
| CHEMBL2087795 | — | — | 1 | 6.85 |
| CHEMBL2087551 | — | — | 1 | 6.82 |
| CHEMBL2087799 | — | — | 1 | 6.75 |
| CHEMBL2087555 | — | — | 1 | 6.70 |
| CHEMBL2087556 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087562 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2087567 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2087574 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2087796 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2087575 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2087794 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2087553 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2087554 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2087550 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2087552 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2087573 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2087801 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL2087795 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2087551 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2087799 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2087555 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2087556 | — | IC50 | = | 480.0 | nM | 6.32 |