Assay Detail
Binding
CHEMBL4429656
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Displacement of [125I]-orexin A from human OX2 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 | 6.36 | 9.70 |
| IC50 | 11 | 6.20 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429848 | — | — | 1 | 9.70 |
| CHEMBL4531556 | — | — | 2 | 7.16 |
| CHEMBL4578783 | — | — | 2 | 6.89 |
| CHEMBL4548914 | — | — | 2 | 6.52 |
| CHEMBL1481561 | — | — | 2 | 6.30 |
| CHEMBL4471376 | — | — | 2 | 6.16 |
| CHEMBL4473709 | — | — | 2 | 6.16 |
| CHEMBL4544095 | — | — | 2 | 6.10 |
| CHEMBL3798017 | (R)-Carvedilol | — | 2 | 6.05 |
| CHEMBL4475736 | — | — | 2 | 5.77 |
| CHEMBL4445194 | — | — | 2 | 4.93 |
| CHEMBL4472213 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429848 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4531556 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4531556 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4578783 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4578783 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4548914 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4548914 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL1481561 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4471376 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4473709 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4544095 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1481561 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL3798017 | (R)-Carvedilol | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4473709 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4471376 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4544095 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL3798017 | (R)-Carvedilol | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL4475736 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4475736 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL4445194 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL4445194 | — | Ki | = | 17800.0 | nM | 4.75 |
| CHEMBL4472213 | — | Ki | - | — | - | |
| CHEMBL4472213 | — | IC50 | - | — | - |