Assay Detail
Binding
CHEMBL5363863
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DAMGO from human MOR receptor expressed in HEK293T cell membrane assessed as inhibition constant incubated for 60 mins by MicroBeta scintillation counting method
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacological and Physicochemical Properties Optimization for Dual-Target Dopamine D<sub>3</sub> (D<sub>3</sub>R) and μ-Opioid (MOR) Receptor Ligands as Potentially Safer Analgesics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 6.68 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5409322 | — | — | 1 | 9.44 |
| CHEMBL5417253 | — | — | 1 | 8.91 |
| CHEMBL2443262 | OLICERIDINE | 4.0 | 1 | 8.36 |
| CHEMBL5398913 | — | — | 1 | 7.91 |
| CHEMBL5418819 | — | — | 1 | 7.63 |
| CHEMBL5406129 | — | — | 1 | 7.62 |
| CHEMBL5410159 | — | — | 1 | 7.57 |
| CHEMBL5397609 | — | — | 1 | 7.51 |
| CHEMBL5436551 | — | — | 1 | 7.33 |
| CHEMBL5415557 | — | — | 1 | 7.26 |
| CHEMBL5412995 | — | — | 1 | 7.26 |
| CHEMBL5417643 | — | — | 1 | 7.09 |
| CHEMBL5433458 | — | — | 1 | 7.07 |
| CHEMBL5395539 | — | — | 1 | 6.84 |
| CHEMBL5413807 | — | — | 1 | 6.78 |
| CHEMBL5412606 | — | — | 1 | 6.72 |
| CHEMBL5434650 | — | — | 1 | 6.42 |
| CHEMBL5432993 | — | — | 1 | 6.28 |
| CHEMBL5407845 | — | — | 1 | 6.27 |
| CHEMBL5414796 | — | — | 1 | 6.25 |
| CHEMBL5399270 | — | — | 1 | 6.16 |
| CHEMBL5415842 | — | — | 1 | 6.13 |
| CHEMBL5398747 | — | — | 1 | 6.11 |
| CHEMBL5404724 | — | — | 1 | 6.10 |
| CHEMBL5421714 | — | — | 1 | 6.10 |
| CHEMBL5435235 | — | — | 1 | 6.06 |
| CHEMBL5407747 | — | — | 1 | 5.84 |
| CHEMBL5418730 | — | — | 1 | 5.80 |
| CHEMBL5423250 | — | — | 1 | 5.79 |
| CHEMBL5429207 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5409322 | — | Ki | = | 0.364 | nM | 9.44 |
| CHEMBL5417253 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL2443262 | OLICERIDINE | Ki | = | 4.38 | nM | 8.36 |
| CHEMBL5398913 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL5418819 | — | Ki | = | 23.5 | nM | 7.63 |
| CHEMBL5406129 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL5410159 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL5397609 | — | Ki | = | 31.2 | nM | 7.51 |
| CHEMBL5436551 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL5412995 | — | Ki | = | 55.2 | nM | 7.26 |
| CHEMBL5415557 | — | Ki | = | 54.7 | nM | 7.26 |
| CHEMBL5417643 | — | Ki | = | 81.8 | nM | 7.09 |
| CHEMBL5433458 | — | Ki | = | 85.2 | nM | 7.07 |
| CHEMBL5395539 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL5413807 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL5412606 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL5434650 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL5432993 | — | Ki | = | 529.0 | nM | 6.28 |
| CHEMBL5407845 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL5414796 | — | Ki | = | 564.0 | nM | 6.25 |
| CHEMBL5399270 | — | Ki | = | 691.0 | nM | 6.16 |
| CHEMBL5415842 | — | Ki | = | 745.0 | nM | 6.13 |
| CHEMBL5398747 | — | Ki | = | 782.0 | nM | 6.11 |
| CHEMBL5404724 | — | Ki | = | 791.0 | nM | 6.10 |
| CHEMBL5421714 | — | Ki | = | 787.0 | nM | 6.10 |
| CHEMBL5435235 | — | Ki | = | 867.0 | nM | 6.06 |
| CHEMBL5407747 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL5418730 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL5423250 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL5429207 | — | Ki | = | 1670.0 | nM | 5.78 |
| CHEMBL5425944 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL5400356 | — | Ki | = | 2070.0 | nM | 5.68 |
| CHEMBL5415451 | — | Ki | = | 2120.0 | nM | 5.67 |
| CHEMBL5415691 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL5407131 | — | Ki | = | 2380.0 | nM | 5.62 |
| CHEMBL5413237 | — | Ki | = | 2520.0 | nM | 5.60 |