Assay Detail
Functional
CHEMBL965359
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Agonist activity at kappa opioid receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.00 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488635 | — | — | 1 | 10.00 |
| CHEMBL527199 | — | — | 1 | 9.70 |
| CHEMBL38576 | ICI-199,441 | — | 1 | 9.40 |
| CHEMBL488470 | — | — | 1 | 8.40 |
| CHEMBL488642 | — | — | 1 | 7.80 |
| CHEMBL453587 | — | — | 1 | 7.50 |
| CHEMBL452808 | — | — | 1 | 7.40 |
| CHEMBL453067 | — | — | 1 | 7.00 |
| CHEMBL453329 | — | — | 1 | 6.80 |
| CHEMBL453074 | — | — | 1 | 6.50 |
| CHEMBL453075 | — | — | 1 | 6.10 |
| CHEMBL449192 | — | — | 1 | 6.10 |
| CHEMBL452298 | — | — | 1 | 5.80 |
| CHEMBL507691 | — | — | 1 | 5.70 |
| CHEMBL254153 | — | — | 1 | 5.70 |
| CHEMBL254356 | — | — | 1 | 5.50 |
| CHEMBL499582 | — | — | 1 | 5.40 |
| CHEMBL402303 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488635 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL527199 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL38576 | ICI-199,441 | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL488470 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL488642 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL453587 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL452808 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL453067 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL453329 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL453074 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL453075 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL449192 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL452298 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL507691 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL254153 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL254356 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL499582 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL402303 | — | EC50 | = | 6300.0 | nM | 5.20 |