Assay Detail
Binding
CHEMBL2167727
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Displacement of [125I]-BNtxA from Mu-type opioid receptor exon 11-associated truncated six transmembrane domain splice variant in mouse brain membranes after 90 mins
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of aryl-naloxamide opiate analgesics targeting truncated exon 11-associated μ opioid receptor (MOR-1) splice variants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 8.14 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1795711 | — | — | 1 | 9.80 |
| CHEMBL1795712 | — | — | 1 | 9.60 |
| CHEMBL2163536 | — | — | 1 | 9.19 |
| CHEMBL2163543 | — | — | 1 | 8.79 |
| CHEMBL2163539 | — | — | 1 | 8.69 |
| CHEMBL2164295 | — | — | 1 | 8.34 |
| CHEMBL2163546 | — | — | 1 | 8.28 |
| CHEMBL2163538 | — | — | 1 | 8.26 |
| CHEMBL2163540 | — | — | 1 | 8.23 |
| CHEMBL2164297 | — | — | 1 | 8.18 |
| CHEMBL2164298 | — | — | 1 | 8.14 |
| CHEMBL2164296 | — | — | 1 | 8.13 |
| CHEMBL2163544 | — | — | 1 | 8.12 |
| CHEMBL2163537 | — | — | 1 | 8.09 |
| CHEMBL2163534 | — | — | 1 | 8.07 |
| CHEMBL2163541 | — | — | 1 | 8.05 |
| CHEMBL2163542 | — | — | 1 | 8.03 |
| CHEMBL2163545 | — | — | 1 | 7.97 |
| CHEMBL2163535 | — | — | 1 | 7.54 |
| CHEMBL2164300 | — | — | 1 | 7.53 |
| CHEMBL2163532 | — | — | 1 | 7.52 |
| CHEMBL2163531 | — | — | 1 | 7.52 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.49 |
| CHEMBL2164301 | — | — | 1 | 7.40 |
| CHEMBL1795713 | — | — | 1 | 7.38 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.27 |
| CHEMBL2164299 | — | — | 1 | - |
| CHEMBL2163533 | — | — | 1 | - |
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1795711 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL1795712 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL2163536 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL2163543 | — | Ki | = | 1.64 | nM | 8.79 |
| CHEMBL2163539 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL2164295 | — | Ki | = | 4.53 | nM | 8.34 |
| CHEMBL2163546 | — | Ki | = | 5.21 | nM | 8.28 |
| CHEMBL2163538 | — | Ki | = | 5.49 | nM | 8.26 |
| CHEMBL2163540 | — | Ki | = | 5.82 | nM | 8.23 |
| CHEMBL2164297 | — | Ki | = | 6.64 | nM | 8.18 |
| CHEMBL2164298 | — | Ki | = | 7.17 | nM | 8.14 |
| CHEMBL2164296 | — | Ki | = | 7.43 | nM | 8.13 |
| CHEMBL2163544 | — | Ki | = | 7.62 | nM | 8.12 |
| CHEMBL2163537 | — | Ki | = | 8.09 | nM | 8.09 |
| CHEMBL2163534 | — | Ki | = | 8.46 | nM | 8.07 |
| CHEMBL2163541 | — | Ki | = | 8.98 | nM | 8.05 |
| CHEMBL2163542 | — | Ki | = | 9.32 | nM | 8.03 |
| CHEMBL2163545 | — | Ki | = | 10.79 | nM | 7.97 |
| CHEMBL2163535 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2164300 | — | Ki | = | 29.65 | nM | 7.53 |
| CHEMBL2163532 | — | Ki | = | 30.27 | nM | 7.52 |
| CHEMBL2163531 | — | Ki | = | 30.17 | nM | 7.52 |
| CHEMBL19019 | NALTREXONE | Ki | = | 32.7 | nM | 7.49 |
| CHEMBL2164301 | — | Ki | = | 39.43 | nM | 7.40 |
| CHEMBL1795713 | — | Ki | = | 41.22 | nM | 7.38 |
| CHEMBL80 | NALOXONE | Ki | = | 53.2 | nM | 7.27 |
| CHEMBL2164299 | — | Ki | > | 100.0 | nM | - |
| CHEMBL2163533 | — | Ki | > | 100.0 | nM | - |
| CHEMBL963 | OXYMORPHONE | Ki | > | 1000.0 | nM | - |