Assay Detail
Binding
CHEMBL757498
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Binding affinity towards human Opioid receptor delta 1 on NxG108CC15 (human neuroglioblastoma) cell membranes by [3H]DPDPE displacement.
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Side chain methyl substitution in the delta-opioid receptor antagonist TIPP has an important effect on the activity profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 8.24 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2371018 | — | — | 1 | 9.42 |
| CHEMBL191751 | — | — | 2 | 9.32 |
| CHEMBL2369139 | — | — | 1 | 9.30 |
| CHEMBL2372509 | — | — | 1 | 9.28 |
| CHEMBL2371020 | — | — | 1 | 9.18 |
| CHEMBL2371027 | — | — | 1 | 9.12 |
| CHEMBL557035 | — | — | 1 | 9.08 |
| CHEMBL2371023 | — | — | 1 | 8.92 |
| CHEMBL2371015 | — | — | 1 | 8.80 |
| CHEMBL2371019 | — | — | 1 | 8.78 |
| CHEMBL2371016 | — | — | 1 | 8.54 |
| CHEMBL2371009 | — | — | 1 | 8.54 |
| CHEMBL2371026 | — | — | 1 | 8.39 |
| CHEMBL3350370 | — | — | 1 | 8.17 |
| CHEMBL2364557 | — | — | 1 | 8.11 |
| CHEMBL2371025 | — | — | 1 | 7.96 |
| CHEMBL2371014 | — | — | 1 | 7.55 |
| CHEMBL2370013 | — | — | 1 | 7.13 |
| CHEMBL2371013 | — | — | 1 | 6.95 |
| CHEMBL2371017 | — | — | 1 | 6.32 |
| CHEMBL365581 | — | — | 1 | 6.29 |
| CHEMBL2371024 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2371018 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL191751 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL2369139 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2372509 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL2371020 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL2371027 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL557035 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL2371023 | — | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL2371015 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2371019 | — | Ki | = | 1.68 | nM | 8.78 |
| CHEMBL2371016 | — | Ki | = | 2.91 | nM | 8.54 |
| CHEMBL2371009 | — | Ki | = | 2.88 | nM | 8.54 |
| CHEMBL2371026 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3350370 | — | Ki | = | 6.81 | nM | 8.17 |
| CHEMBL191751 | — | Ki | = | 6.76 | nM | 8.17 |
| CHEMBL2364557 | — | Ki | = | 7.83 | nM | 8.11 |
| CHEMBL2371025 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2371014 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2370013 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL2371013 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL2371017 | — | Ki | = | 474.0 | nM | 6.32 |
| CHEMBL365581 | — | Ki | = | 519.0 | nM | 6.29 |
| CHEMBL2371024 | — | Ki | = | 543.0 | nM | 6.26 |