Assay Detail
Binding
CHEMBL744610
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against rat mu-opioid receptor expressed in CHO cells by competitive inhibition of 1 nM [3H]DAMGO
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 | 8.03 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2115493 | — | — | 1 | 9.60 |
| CHEMBL15595 | — | — | 1 | 8.74 |
| CHEMBL2114469 | — | — | 1 | 8.60 |
| CHEMBL38874 | DAMGO | — | 1 | 8.52 |
| CHEMBL60936 | — | — | 1 | 8.20 |
| CHEMBL2114470 | — | — | 1 | 7.30 |
| CHEMBL2373084 | — | — | 1 | 6.80 |
| CHEMBL2115492 | — | — | 1 | 6.50 |
| CHEMBL62688 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2115493 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL15595 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2114469 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL38874 | DAMGO | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL60936 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2114470 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2373084 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL2115492 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL62688 | — | IC50 | > | 10000.0 | nM | - |