Assay Detail
Binding
CHEMBL3742876
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Displacement of [3H]EMPA from human orexin receptor-2 expressed in HEK293 cells after 90 mins by scintillation counting
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.61 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3741853 | — | — | 1 | 10.00 |
| CHEMBL3740471 | — | — | 1 | 9.70 |
| CHEMBL3740971 | — | — | 1 | 9.60 |
| CHEMBL3741474 | — | — | 1 | 9.40 |
| CHEMBL3742398 | — | — | 1 | 9.30 |
| CHEMBL3739451 | — | — | 1 | 9.20 |
| CHEMBL3742392 | — | — | 1 | 9.10 |
| CHEMBL3741094 | — | — | 1 | 9.10 |
| CHEMBL3740873 | — | — | 1 | 9.00 |
| CHEMBL3741648 | — | — | 1 | 8.90 |
| CHEMBL3741721 | — | — | 1 | 8.80 |
| CHEMBL3741584 | — | — | 1 | 8.80 |
| CHEMBL3741978 | — | — | 1 | 8.70 |
| CHEMBL3740099 | — | — | 1 | 8.60 |
| CHEMBL3741125 | — | — | 1 | 8.30 |
| CHEMBL3741373 | — | — | 1 | 8.20 |
| CHEMBL3739510 | — | — | 1 | 8.20 |
| CHEMBL3740284 | — | — | 1 | 8.00 |
| CHEMBL3742141 | — | — | 1 | 7.60 |
| CHEMBL3742143 | — | — | 1 | 7.20 |
| CHEMBL3740976 | — | — | 1 | 7.10 |
| CHEMBL3742402 | — | — | 1 | 6.60 |
| CHEMBL3741065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3741853 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3740471 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL3740971 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL3741474 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL3742398 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL3739451 | — | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL3742392 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL3741094 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL3740873 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3741648 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL3741721 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL3741584 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL3741978 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL3740099 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3741125 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL3741373 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL3739510 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL3740284 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3742141 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3742143 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3740976 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL3742402 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL3741065 | — | Ki | > | 10000.0 | nM | - |