Assay Detail
Binding
CHEMBL831660
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Displacement of [125I]o-CRF from recombinant human CRF receptors expressed in Chinese Hamster Ovary (CHO) cell membranes
19
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.32 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL369510 | — | — | 3 | 7.96 |
| CHEMBL178949 | — | — | 1 | 7.85 |
| CHEMBL360348 | — | — | 3 | 7.84 |
| CHEMBL9946 | CP-154526 | — | 1 | 7.76 |
| CHEMBL179435 | — | — | 1 | 7.58 |
| CHEMBL361344 | — | — | 1 | 7.57 |
| CHEMBL179608 | — | — | 1 | 7.52 |
| CHEMBL44698 | — | — | 1 | 7.42 |
| CHEMBL361346 | — | — | 1 | 7.39 |
| CHEMBL180025 | — | — | 1 | 7.35 |
| CHEMBL179041 | — | — | 1 | 7.21 |
| CHEMBL176145 | — | — | 1 | 7.16 |
| CHEMBL180116 | — | — | 1 | 6.74 |
| CHEMBL180222 | — | — | 1 | 5.90 |
| CHEMBL178176 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL369510 | — | IC50 | = | 10.96 | nM | 7.96 |
| CHEMBL369510 | — | IC50 | = | 12.88 | nM | 7.89 |
| CHEMBL178949 | — | IC50 | = | 14.13 | nM | 7.85 |
| CHEMBL360348 | — | IC50 | = | 14.45 | nM | 7.84 |
| CHEMBL9946 | CP-154526 | IC50 | = | 17.38 | nM | 7.76 |
| CHEMBL369510 | — | IC50 | = | 22.39 | nM | 7.65 |
| CHEMBL179435 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL361344 | — | IC50 | = | 26.92 | nM | 7.57 |
| CHEMBL360348 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL179608 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL360348 | — | IC50 | = | 36.31 | nM | 7.44 |
| CHEMBL44698 | — | IC50 | = | 38.02 | nM | 7.42 |
| CHEMBL361346 | — | IC50 | = | 40.74 | nM | 7.39 |
| CHEMBL180025 | — | IC50 | = | 44.67 | nM | 7.35 |
| CHEMBL179041 | — | IC50 | = | 61.66 | nM | 7.21 |
| CHEMBL176145 | — | IC50 | = | 69.18 | nM | 7.16 |
| CHEMBL180116 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL180222 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL178176 | — | IC50 | = | 4466.84 | nM | 5.35 |