Assay Detail
Binding
CHEMBL700237
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Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Syntheses of potent Leu-enkephalin analogs possessing beta-hydroxy-alpha,alpha-disubstituted-alpha-amino acid and their characterization to opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.93 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL440765 | U-69593 | — | 1 | 9.20 |
| CHEMBL15595 | — | — | 1 | 6.40 |
| CHEMBL2115493 | — | — | 1 | 5.20 |
| CHEMBL2115492 | — | — | 1 | - |
| CHEMBL2373084 | — | — | 1 | - |
| CHEMBL60936 | — | — | 1 | - |
| CHEMBL2114470 | — | — | 1 | - |
| CHEMBL62688 | — | — | 1 | - |
| CHEMBL2114469 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL440765 | U-69593 | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL15595 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2115493 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL2115492 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2373084 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL60936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2114470 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL62688 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2114469 | — | IC50 | > | 10000.0 | nM | - |