Assay Detail
Functional
CHEMBL3745069
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human orexin-1 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 | 7.73 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3742089 | — | — | 1 | 8.57 |
| CHEMBL3742235 | — | — | 1 | 8.47 |
| CHEMBL3739711 | — | — | 1 | 8.46 |
| CHEMBL3741779 | — | — | 1 | 8.42 |
| CHEMBL3742341 | — | — | 1 | 8.27 |
| CHEMBL3742040 | — | — | 1 | 8.08 |
| CHEMBL3740506 | — | — | 1 | 8.07 |
| CHEMBL3742079 | — | — | 1 | 8.04 |
| CHEMBL3739958 | — | — | 1 | 7.96 |
| CHEMBL3741194 | — | — | 1 | 7.96 |
| CHEMBL3739577 | — | — | 1 | 7.89 |
| CHEMBL3739682 | — | — | 1 | 7.80 |
| CHEMBL3741003 | — | — | 1 | 7.80 |
| CHEMBL3740186 | — | — | 1 | 7.77 |
| CHEMBL3741767 | — | — | 1 | 7.66 |
| CHEMBL3739859 | — | — | 1 | 7.64 |
| CHEMBL3741058 | — | — | 1 | 7.58 |
| CHEMBL3739704 | — | — | 1 | 7.55 |
| CHEMBL3742247 | — | — | 1 | 7.55 |
| CHEMBL3740773 | — | — | 1 | 7.48 |
| CHEMBL3739613 | — | — | 1 | 7.48 |
| CHEMBL3742301 | — | — | 1 | 7.46 |
| CHEMBL3740565 | — | — | 1 | 7.35 |
| CHEMBL3740670 | — | — | 1 | 7.22 |
| CHEMBL3741099 | — | — | 1 | 7.19 |
| CHEMBL3740505 | — | — | 1 | 6.97 |
| CHEMBL3740088 | — | — | 1 | 6.96 |
| CHEMBL3741221 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3742089 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3742235 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3739711 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3741779 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3742341 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3742040 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3740506 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3742079 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3739958 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3741194 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3739577 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3739682 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3741003 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3740186 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3741767 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3739859 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3741058 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3739704 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3742247 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3740773 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3739613 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3742301 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3740565 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3740670 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3741099 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3740505 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL3740088 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3741221 | — | IC50 | = | 131.0 | nM | 6.88 |