Assay Detail
Binding
CHEMBL4380596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.06 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 9.40 |
| CHEMBL2107822 | FILOREXANT | 2.0 | 1 | 9.20 |
| CHEMBL4297590 | DARIDOREXANT | 4.0 | 1 | 8.80 |
| CHEMBL2413522 | — | — | 1 | 8.70 |
| CHEMBL3545367 | LEMBOREXANT | 4.0 | 1 | 8.60 |
| CHEMBL3597952 | ACT-462206 | 1.0 | 1 | 8.20 |
| CHEMBL4592653 | — | — | 1 | 7.80 |
| CHEMBL291536 | — | — | 1 | 7.80 |
| CHEMBL1334465 | — | — | 1 | 7.60 |
| CHEMBL3740099 | — | — | 1 | 7.50 |
| CHEMBL4590386 | — | — | 1 | 7.10 |
| CHEMBL2385132 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083659 | SUVOREXANT | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL2107822 | FILOREXANT | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL4297590 | DARIDOREXANT | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL2413522 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL3545367 | LEMBOREXANT | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL3597952 | ACT-462206 | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL4592653 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL291536 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1334465 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3740099 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL4590386 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL2385132 | — | Ki | = | 1000.0 | nM | 6.00 |