Assay Detail
Functional
CHEMBL1109768
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Antagonist activity at OX2 receptor assessed as inhibition of calcium flux by FLIPR assay
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.76 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL469146 | — | — | 1 | 7.57 |
| CHEMBL1089406 | — | — | 1 | 7.57 |
| CHEMBL1091110 | — | — | 3 | 7.36 |
| CHEMBL1091111 | — | — | 1 | 6.96 |
| CHEMBL1093724 | — | — | 1 | 5.43 |
| CHEMBL1091112 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL469146 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1089406 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1091110 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1091110 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1091111 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1093724 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1091110 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1091112 | — | IC50 | > | 10000.0 | nM | - |