Assay Detail
Binding
CHEMBL4429655
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Displacement of [125I]-orexin A from human OX1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting
23
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacophore Model To Discover OX1 and OX2 Orexin Receptor Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.66 | 7.85 |
| IC50 | 11 | 5.19 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL291536 | — | — | 1 | 7.85 |
| CHEMBL4471376 | — | — | 2 | 6.10 |
| CHEMBL4548914 | — | — | 2 | 5.96 |
| CHEMBL4578783 | — | — | 2 | 5.92 |
| CHEMBL3798017 | (R)-Carvedilol | — | 2 | 5.89 |
| CHEMBL4544095 | — | — | 2 | 5.57 |
| CHEMBL4531556 | — | — | 2 | 5.20 |
| CHEMBL1481561 | — | — | 2 | 5.17 |
| CHEMBL4445194 | — | — | 2 | 5.12 |
| CHEMBL4473709 | — | — | 2 | 4.92 |
| CHEMBL4475736 | — | — | 2 | 4.51 |
| CHEMBL4472213 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL291536 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4471376 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL4548914 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4578783 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL3798017 | (R)-Carvedilol | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4471376 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4548914 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4578783 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3798017 | (R)-Carvedilol | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4544095 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL4544095 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4531556 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL1481561 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL4445194 | — | Ki | = | 7600.0 | nM | 5.12 |
| CHEMBL4531556 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL1481561 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4473709 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL4445194 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4473709 | — | IC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL4475736 | — | Ki | = | 30700.0 | nM | 4.51 |
| CHEMBL4475736 | — | IC50 | = | 53700.0 | nM | 4.27 |
| CHEMBL4472213 | — | Ki | - | — | - | |
| CHEMBL4472213 | — | IC50 | - | — | - |