Assay Detail
Binding
CHEMBL1106905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL4649) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.19 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL574852 | — | — | 1 | 9.62 |
| CHEMBL583387 | — | — | 1 | 9.52 |
| CHEMBL1084423 | — | — | 1 | 9.17 |
| CHEMBL1089036 | — | — | 1 | 9.10 |
| CHEMBL1077301 | — | — | 1 | 8.92 |
| CHEMBL1089037 | — | — | 1 | 8.92 |
| CHEMBL1086180 | — | — | 1 | 8.92 |
| CHEMBL1086179 | — | — | 1 | 8.92 |
| CHEMBL573748 | — | — | 1 | 8.82 |
| CHEMBL559764 | — | — | 1 | 8.80 |
| CHEMBL558280 | — | — | 1 | 8.77 |
| CHEMBL1086181 | — | — | 1 | 8.68 |
| CHEMBL1077249 | — | — | 1 | 8.57 |
| CHEMBL1091818 | — | — | 1 | 8.54 |
| CHEMBL1089038 | — | — | 1 | 8.33 |
| CHEMBL1085930 | — | — | 1 | 8.17 |
| CHEMBL1084413 | — | — | 1 | 7.96 |
| CHEMBL1082241 | — | — | 1 | 7.92 |
| CHEMBL1084414 | — | — | 1 | 7.77 |
| CHEMBL1090739 | — | — | 1 | 7.51 |
| CHEMBL1085683 | — | — | 1 | 7.19 |
| CHEMBL1090740 | — | — | 1 | 7.05 |
| CHEMBL1090738 | — | — | 1 | 6.85 |
| CHEMBL1077299 | — | — | 1 | 6.62 |
| CHEMBL1085931 | — | — | 1 | 6.14 |
| CHEMBL1084422 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL574852 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL583387 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1084423 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL1089036 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL1077301 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1089037 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1086180 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1086179 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL573748 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL559764 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL558280 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1086181 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1077249 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1091818 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1089038 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL1085930 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1084413 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1082241 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1084414 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1090739 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1085683 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1090740 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1090738 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1077299 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1085931 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL1084422 | — | IC50 | = | 740.0 | nM | 6.13 |