Assay Detail
Binding
CHEMBL923348
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Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.42 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251386 | — | — | 1 | 8.40 |
| CHEMBL413134 | — | — | 1 | 7.90 |
| CHEMBL248962 | — | — | 1 | 7.90 |
| CHEMBL9946 | CP-154526 | — | 1 | 7.80 |
| CHEMBL178949 | — | — | 1 | 7.80 |
| CHEMBL179435 | — | — | 1 | 7.60 |
| CHEMBL179608 | — | — | 1 | 7.50 |
| CHEMBL251551 | — | — | 1 | 7.40 |
| CHEMBL250182 | — | — | 1 | 7.40 |
| CHEMBL44698 | — | — | 1 | 7.40 |
| CHEMBL250996 | — | — | 1 | 7.30 |
| CHEMBL180025 | — | — | 1 | 7.30 |
| CHEMBL251344 | — | — | 1 | 7.20 |
| CHEMBL250603 | — | — | 1 | 7.10 |
| CHEMBL250982 | — | — | 1 | 7.00 |
| CHEMBL430396 | — | — | 1 | 6.90 |
| CHEMBL250803 | — | — | 1 | 6.90 |
| CHEMBL249333 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251386 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL413134 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL248962 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL9946 | CP-154526 | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL178949 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL179435 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL179608 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL251551 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL250182 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL44698 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL250996 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL180025 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL251344 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL250603 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL250982 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL430396 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL250803 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL249333 | — | IC50 | = | 158.49 | nM | 6.80 |