Assay Detail
Functional
CHEMBL3745065
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Inhibition of human orexin-2 receptor expressed in CHO cells assessed as calcium release preincubated for 120 mins followed by addition of orexin-A by fluo-4 AM based-FLIPR analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and optimisation of 1-acyl-2-benzylpyrrolidines as potent dual orexin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.84 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3742341 | — | — | 1 | 8.85 |
| CHEMBL3741779 | — | — | 1 | 8.74 |
| CHEMBL3739711 | — | — | 1 | 8.51 |
| CHEMBL3742089 | — | — | 1 | 8.48 |
| CHEMBL3739682 | — | — | 1 | 8.46 |
| CHEMBL3739859 | — | — | 1 | 8.40 |
| CHEMBL3742235 | — | — | 1 | 8.37 |
| CHEMBL3741003 | — | — | 1 | 8.33 |
| CHEMBL3742079 | — | — | 1 | 8.20 |
| CHEMBL3741194 | — | — | 1 | 8.18 |
| CHEMBL3739958 | — | — | 1 | 8.11 |
| CHEMBL3742040 | — | — | 1 | 8.10 |
| CHEMBL3740506 | — | — | 1 | 8.08 |
| CHEMBL3739577 | — | — | 1 | 8.00 |
| CHEMBL3740186 | — | — | 1 | 8.00 |
| CHEMBL3739613 | — | — | 1 | 7.92 |
| CHEMBL3742247 | — | — | 1 | 7.80 |
| CHEMBL3741058 | — | — | 1 | 7.80 |
| CHEMBL3740773 | — | — | 1 | 7.75 |
| CHEMBL3742301 | — | — | 1 | 7.41 |
| CHEMBL3741099 | — | — | 1 | 7.40 |
| CHEMBL3740088 | — | — | 1 | 7.21 |
| CHEMBL3740565 | — | — | 1 | 7.19 |
| CHEMBL3741767 | — | — | 1 | 7.18 |
| CHEMBL3740670 | — | — | 1 | 7.15 |
| CHEMBL3739704 | — | — | 1 | 6.99 |
| CHEMBL3740505 | — | — | 1 | 6.61 |
| CHEMBL3741221 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3742341 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3741779 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3739711 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3742089 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3739682 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3739859 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3742235 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3741003 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3742079 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3741194 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3739958 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3742040 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3740506 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3739577 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3740186 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3739613 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3742247 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3741058 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3740773 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3742301 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3741099 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3740088 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3740565 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3741767 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3740670 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3739704 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3740505 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL3741221 | — | IC50 | = | 428.0 | nM | 6.37 |