Assay Detail
Binding
CHEMBL994494
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.96 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL519159 | — | — | 1 | 8.80 |
| CHEMBL483162 | — | — | 1 | 8.62 |
| CHEMBL482752 | — | — | 1 | 8.52 |
| CHEMBL516242 | — | — | 1 | 8.51 |
| CHEMBL519967 | — | — | 1 | 8.51 |
| CHEMBL473069 | — | — | 1 | 8.46 |
| CHEMBL474289 | — | — | 1 | 8.35 |
| CHEMBL500013 | — | — | 1 | 8.31 |
| CHEMBL473070 | — | — | 1 | 8.29 |
| CHEMBL473277 | — | — | 1 | 8.24 |
| CHEMBL482950 | PEXACERFONT | 3.0 | 1 | 8.21 |
| CHEMBL475507 | — | — | 1 | 8.18 |
| CHEMBL474288 | — | — | 1 | 8.15 |
| CHEMBL483350 | — | — | 1 | 8.09 |
| CHEMBL514465 | — | — | 1 | 8.07 |
| CHEMBL473276 | — | — | 1 | 7.92 |
| CHEMBL482543 | — | — | 1 | 7.89 |
| CHEMBL520955 | — | — | 1 | 7.86 |
| CHEMBL482751 | — | — | 1 | 7.84 |
| CHEMBL473275 | — | — | 1 | 7.83 |
| CHEMBL483349 | — | — | 1 | 7.75 |
| CHEMBL484930 | — | — | 1 | 7.62 |
| CHEMBL520344 | — | — | 1 | 7.61 |
| CHEMBL474491 | — | — | 1 | 7.59 |
| CHEMBL482542 | — | — | 1 | 7.48 |
| CHEMBL474493 | — | — | 1 | 7.24 |
| CHEMBL453001 | — | — | 1 | 7.09 |
| CHEMBL482544 | — | — | 1 | 7.04 |
| CHEMBL474492 | — | — | 1 | 6.88 |
| CHEMBL515583 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL519159 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL483162 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL482752 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL516242 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL519967 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL473069 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL474289 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL500013 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL473070 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL473277 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL482950 | PEXACERFONT | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL475507 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL474288 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL483350 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL514465 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL473276 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL482543 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL520955 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL482751 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL473275 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL483349 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL484930 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL520344 | — | IC50 | = | 24.8 | nM | 7.61 |
| CHEMBL474491 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL482542 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL474493 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL453001 | — | IC50 | = | 81.6 | nM | 7.09 |
| CHEMBL482544 | — | IC50 | = | 91.9 | nM | 7.04 |
| CHEMBL474492 | — | IC50 | = | 133.3 | nM | 6.88 |
| CHEMBL515583 | — | IC50 | > | 10000.0 | nM | - |