Assay Detail
Binding
CHEMBL2089413
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 34 | 7.37 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087550 | — | — | 1 | 8.00 |
| CHEMBL2087552 | — | — | 1 | 7.92 |
| CHEMBL2087554 | — | — | 1 | 7.89 |
| CHEMBL2087555 | — | — | 1 | 7.82 |
| CHEMBL2087551 | — | — | 1 | 7.80 |
| CHEMBL2087558 | — | — | 1 | 7.70 |
| CHEMBL2087562 | — | — | 1 | 7.66 |
| CHEMBL2087561 | — | — | 1 | 7.66 |
| CHEMBL2087553 | — | — | 1 | 7.62 |
| CHEMBL2087795 | — | — | 1 | 7.60 |
| CHEMBL2087799 | — | — | 1 | 7.57 |
| CHEMBL2087801 | — | — | 1 | 7.47 |
| CHEMBL2087560 | — | — | 1 | 7.47 |
| CHEMBL2087574 | — | — | 1 | 7.46 |
| CHEMBL2087559 | — | — | 1 | 7.42 |
| CHEMBL2087563 | — | — | 1 | 7.40 |
| CHEMBL2087571 | — | — | 1 | 7.40 |
| CHEMBL2087557 | — | — | 1 | 7.39 |
| CHEMBL2087564 | — | — | 1 | 7.38 |
| CHEMBL2087796 | — | — | 1 | 7.33 |
| CHEMBL2087569 | — | — | 1 | 7.31 |
| CHEMBL2087567 | — | — | 1 | 7.30 |
| CHEMBL2087573 | — | — | 1 | 7.29 |
| CHEMBL2087794 | — | — | 1 | 7.28 |
| CHEMBL2087556 | — | — | 1 | 7.24 |
| CHEMBL2087572 | — | — | 1 | 7.05 |
| CHEMBL2087797 | — | — | 1 | 7.01 |
| CHEMBL2087570 | — | — | 1 | 6.98 |
| CHEMBL2087800 | — | — | 1 | 6.95 |
| CHEMBL2087575 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087550 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2087552 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2087554 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2087555 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2087551 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2087558 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2087562 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2087561 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2087553 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2087795 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2087799 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2087801 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2087560 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2087574 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2087559 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2087563 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2087571 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2087557 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2087564 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2087796 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2087569 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2087567 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2087573 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2087794 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2087556 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2087572 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2087797 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2087570 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL2087800 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL2087575 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2087568 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2087565 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2087798 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL2087566 | — | IC50 | = | 200.0 | nM | 6.70 |