Assay Detail
Binding
CHEMBL985698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
46
Total Activities
46
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
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 8.39 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL484158 | — | — | 1 | 9.00 |
| CHEMBL474498 | — | — | 1 | 9.00 |
| CHEMBL482982 | — | — | 1 | 8.93 |
| CHEMBL484420 | — | — | 1 | 8.92 |
| CHEMBL526149 | — | — | 1 | 8.91 |
| CHEMBL515740 | — | — | 1 | 8.83 |
| CHEMBL482981 | — | — | 1 | 8.79 |
| CHEMBL474901 | — | — | 1 | 8.76 |
| CHEMBL473075 | — | — | 1 | 8.75 |
| CHEMBL515396 | — | — | 1 | 8.74 |
| CHEMBL474701 | — | — | 1 | 8.73 |
| CHEMBL519340 | — | — | 1 | 8.72 |
| CHEMBL475706 | — | — | 1 | 8.71 |
| CHEMBL483993 | — | — | 1 | 8.70 |
| CHEMBL474700 | — | — | 1 | 8.67 |
| CHEMBL484781 | — | — | 1 | 8.67 |
| CHEMBL475705 | — | — | 1 | 8.64 |
| CHEMBL484421 | — | — | 1 | 8.61 |
| CHEMBL475506 | — | — | 1 | 8.59 |
| CHEMBL482976 | — | — | 1 | 8.56 |
| CHEMBL519677 | — | — | 1 | 8.54 |
| CHEMBL521457 | — | — | 1 | 8.49 |
| CHEMBL519999 | — | — | 1 | 8.43 |
| CHEMBL451693 | — | — | 1 | 8.42 |
| CHEMBL516026 | — | — | 1 | 8.39 |
| CHEMBL519339 | — | — | 1 | 8.38 |
| CHEMBL44698 | — | — | 1 | 8.38 |
| CHEMBL475306 | — | — | 1 | 8.38 |
| CHEMBL506214 | — | — | 1 | 8.36 |
| CHEMBL474699 | — | — | 1 | 8.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL484158 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL474498 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL482982 | — | IC50 | = | 1.18 | nM | 8.93 |
| CHEMBL484420 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL526149 | — | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL515740 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL482981 | — | IC50 | = | 1.64 | nM | 8.79 |
| CHEMBL474901 | — | IC50 | = | 1.72 | nM | 8.76 |
| CHEMBL473075 | — | IC50 | = | 1.78 | nM | 8.75 |
| CHEMBL515396 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL474701 | — | IC50 | = | 1.88 | nM | 8.73 |
| CHEMBL519340 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL475706 | — | IC50 | = | 1.96 | nM | 8.71 |
| CHEMBL483993 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL484781 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL474700 | — | IC50 | = | 2.16 | nM | 8.67 |
| CHEMBL475705 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL484421 | — | IC50 | = | 2.48 | nM | 8.61 |
| CHEMBL475506 | — | IC50 | = | 2.58 | nM | 8.59 |
| CHEMBL482976 | — | IC50 | = | 2.74 | nM | 8.56 |
| CHEMBL519677 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL521457 | — | IC50 | = | 3.26 | nM | 8.49 |
| CHEMBL519999 | — | IC50 | = | 3.72 | nM | 8.43 |
| CHEMBL451693 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL516026 | — | IC50 | = | 4.06 | nM | 8.39 |
| CHEMBL519339 | — | IC50 | = | 4.22 | nM | 8.38 |
| CHEMBL44698 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL475306 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL506214 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL474699 | — | IC50 | = | 4.92 | nM | 8.31 |
| CHEMBL484408 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL472874 | — | IC50 | = | 4.99 | nM | 8.30 |
| CHEMBL472873 | — | IC50 | = | 6.08 | nM | 8.22 |
| CHEMBL475505 | — | IC50 | = | 6.08 | nM | 8.22 |
| CHEMBL474499 | — | IC50 | = | 6.48 | nM | 8.19 |
| CHEMBL473076 | — | IC50 | = | 7.96 | nM | 8.10 |
| CHEMBL482983 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL524616 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL474907 | — | IC50 | = | 11.32 | nM | 7.95 |
| CHEMBL455588 | — | IC50 | = | 11.52 | nM | 7.94 |
| CHEMBL473077 | — | IC50 | = | 13.68 | nM | 7.86 |
| CHEMBL484419 | — | IC50 | = | 17.42 | nM | 7.76 |
| CHEMBL485140 | — | IC50 | = | 19.34 | nM | 7.71 |
| CHEMBL484407 | — | IC50 | = | 24.64 | nM | 7.61 |
| CHEMBL474906 | — | IC50 | = | 38.56 | nM | 7.41 |
| CHEMBL514649 | — | IC50 | = | 80.66 | nM | 7.09 |