Assay Detail
Binding
CHEMBL2416555
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Binding affinity to orexin receptor 1 (unknown origin)
37
Total Activities
37
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective orexin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.73 | 9.52 |
| Kb | 12 | - | - |
| IC50 | 6 | 7.94 | 8.30 |
| Kd | 2 | 5.84 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1272307 | SB-649868 | 2.0 | 1 | 9.52 |
| CHEMBL2413365 | — | — | 1 | 9.30 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 9.22 |
| CHEMBL2413366 | — | — | 1 | 9.00 |
| CHEMBL2110363 | — | — | 1 | 8.96 |
| CHEMBL2413521 | — | — | 1 | 8.96 |
| CHEMBL2107822 | FILOREXANT | 2.0 | 1 | 8.60 |
| CHEMBL2413523 | — | — | 1 | 8.30 |
| CHEMBL2031493 | — | — | 1 | 8.22 |
| CHEMBL2413367 | — | — | 1 | 8.22 |
| CHEMBL2031484 | — | — | 1 | 8.10 |
| CHEMBL522758 | — | — | 1 | 8.06 |
| CHEMBL455136 | ALMOREXANT | 3.0 | 1 | 7.89 |
| CHEMBL1334465 | — | — | 1 | 7.66 |
| CHEMBL2111553 | — | — | 1 | 7.55 |
| CHEMBL2413519 | — | — | 1 | 7.44 |
| CHEMBL2031488 | — | — | 1 | 6.84 |
| CHEMBL2413517 | — | — | 1 | 6.16 |
| CHEMBL2385132 | — | — | 1 | 6.05 |
| CHEMBL2385134 | — | — | 1 | 6.05 |
| CHEMBL2385133 | — | — | 1 | 6.05 |
| CHEMBL359632 | — | — | 1 | 5.78 |
| CHEMBL2413518 | — | — | 1 | 5.51 |
| CHEMBL2413520 | — | — | 1 | 5.36 |
| CHEMBL2413527 | — | — | 1 | - |
| CHEMBL2413526 | — | — | 1 | - |
| CHEMBL2413525 | — | — | 1 | - |
| CHEMBL2413524 | — | — | 1 | - |
| CHEMBL2381071 | — | — | 1 | - |
| CHEMBL2381072 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1272307 | SB-649868 | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2413365 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1083659 | SUVOREXANT | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2413366 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2110363 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2413521 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2107822 | FILOREXANT | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2413523 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2031493 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2413367 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2031484 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL522758 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL455136 | ALMOREXANT | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1334465 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2111553 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2413519 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL2031488 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL2413517 | — | Kd | = | 696.0 | nM | 6.16 |
| CHEMBL2385132 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL2385133 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL2385134 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL359632 | — | Ki | = | 1644.0 | nM | 5.78 |
| CHEMBL2413518 | — | Kd | = | 3052.0 | nM | 5.51 |
| CHEMBL2413520 | — | Ki | = | 4363.0 | nM | 5.36 |
| CHEMBL142009 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1771571 | — | Kb | = | 64.2 | nM | - |
| CHEMBL2413522 | — | Kb | = | 1.6 | nM | - |
| CHEMBL2413364 | — | Kb | = | 1.0 | nM | - |
| CHEMBL2413363 | — | Kb | = | 0.8 | nM | - |
| CHEMBL2413528 | — | Kb | = | 0.5 | nM | - |
| CHEMBL2381098 | — | Kb | = | 5.0 | nM | - |
| CHEMBL2381072 | — | Kb | = | 158.0 | nM | - |
| CHEMBL2381071 | — | Kb | = | 31.6 | nM | - |
| CHEMBL2413524 | — | Kb | = | 0.6 | nM | - |
| CHEMBL2413525 | — | Kb | = | 0.3 | nM | - |
| CHEMBL2413526 | — | Kb | = | 0.3 | nM | - |
| CHEMBL2413527 | — | Kb | = | 0.6 | nM | - |