Assay Detail
Binding
CHEMBL930555
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Designed modification of partial agonist of ORL1 nociceptin receptor for conversion into highly potent antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.08 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL396460 | NOCICEPTIN | — | 1 | 9.22 |
| CHEMBL271478 | — | — | 1 | 9.18 |
| CHEMBL437723 | — | — | 1 | 9.10 |
| CHEMBL403807 | — | — | 1 | 8.77 |
| CHEMBL428076 | — | — | 1 | 8.73 |
| CHEMBL436852 | — | — | 1 | 8.55 |
| CHEMBL256687 | — | — | 1 | 8.47 |
| CHEMBL272084 | — | — | 1 | 8.25 |
| CHEMBL404530 | — | — | 1 | 8.13 |
| CHEMBL257921 | — | — | 1 | 7.83 |
| CHEMBL270231 | — | — | 1 | 7.83 |
| CHEMBL270216 | — | — | 1 | 7.77 |
| CHEMBL270394 | — | — | 1 | 7.67 |
| CHEMBL438383 | — | — | 1 | 7.66 |
| CHEMBL403588 | — | — | 1 | 7.34 |
| CHEMBL437601 | — | — | 1 | 7.33 |
| CHEMBL443765 | — | — | 1 | 7.03 |
| CHEMBL444110 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL396460 | NOCICEPTIN | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL271478 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL437723 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL403807 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL428076 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL436852 | — | IC50 | = | 2.81 | nM | 8.55 |
| CHEMBL256687 | — | IC50 | = | 3.42 | nM | 8.47 |
| CHEMBL272084 | — | IC50 | = | 5.67 | nM | 8.25 |
| CHEMBL404530 | — | IC50 | = | 7.42 | nM | 8.13 |
| CHEMBL257921 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL270231 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL270216 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL270394 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL438383 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL403588 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL437601 | — | IC50 | = | 47.3 | nM | 7.33 |
| CHEMBL443765 | — | IC50 | = | 92.6 | nM | 7.03 |
| CHEMBL444110 | — | IC50 | = | 218.0 | nM | 6.66 |