Assay Detail
Binding
CHEMBL3625143
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Binding affinity to human orexin 1 receptor Ile408-Val mutant expressed in CHO cells after 3 hrs by radioligand binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.91 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083358 | — | — | 1 | 9.70 |
| CHEMBL3622331 | — | — | 1 | 9.40 |
| CHEMBL3622326 | — | — | 1 | 9.40 |
| CHEMBL3622332 | — | — | 1 | 9.30 |
| CHEMBL3622330 | — | — | 1 | 9.30 |
| CHEMBL3622328 | — | — | 1 | 9.22 |
| CHEMBL3622327 | — | — | 1 | 9.22 |
| CHEMBL3622325 | — | — | 1 | 9.22 |
| CHEMBL3622333 | — | — | 1 | 9.15 |
| CHEMBL3622329 | — | — | 1 | 9.15 |
| CHEMBL3622323 | — | — | 1 | 8.96 |
| CHEMBL3622336 | — | — | 1 | 8.59 |
| CHEMBL3622324 | — | — | 1 | 8.44 |
| CHEMBL3622334 | — | — | 1 | 8.11 |
| CHEMBL3622322 | — | — | 1 | 7.92 |
| CHEMBL3622335 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083358 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3622331 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3622326 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3622332 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3622330 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3622328 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3622327 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3622325 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3622333 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3622329 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3622323 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3622336 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL3622324 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3622334 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL3622322 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3622335 | — | Ki | = | 31.0 | nM | 7.51 |