Assay Detail
Binding
CHEMBL2167537
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Displacement of [125I]-BNtxA from mouse cloned KOR-1 expressed in CHO cell membrane after 90 mins
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| 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 | 26 | 8.62 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1795711 | — | — | 1 | 10.52 |
| CHEMBL1795712 | — | — | 1 | 10.10 |
| CHEMBL2163542 | — | — | 1 | 9.66 |
| CHEMBL2163536 | — | — | 1 | 9.55 |
| CHEMBL2163544 | — | — | 1 | 9.40 |
| CHEMBL2163538 | — | — | 1 | 9.28 |
| CHEMBL2163535 | — | — | 1 | 9.00 |
| CHEMBL2164297 | — | — | 1 | 8.89 |
| CHEMBL2164295 | — | — | 1 | 8.82 |
| CHEMBL2163539 | — | — | 1 | 8.80 |
| CHEMBL2163541 | — | — | 1 | 8.79 |
| CHEMBL2163537 | — | — | 1 | 8.69 |
| CHEMBL2163546 | — | — | 1 | 8.56 |
| CHEMBL2164296 | — | — | 1 | 8.50 |
| CHEMBL2163543 | — | — | 1 | 8.30 |
| CHEMBL2163532 | — | — | 1 | 8.15 |
| CHEMBL2164300 | — | — | 1 | 8.04 |
| CHEMBL2164301 | — | — | 1 | 8.03 |
| CHEMBL2163534 | — | — | 1 | 7.92 |
| CHEMBL2163540 | — | — | 1 | 7.85 |
| CHEMBL2163531 | — | — | 1 | 7.75 |
| CHEMBL2164298 | — | — | 1 | 7.59 |
| CHEMBL2163545 | — | — | 1 | 7.46 |
| CHEMBL1795713 | — | — | 1 | 7.33 |
| CHEMBL2163533 | — | — | 1 | - |
| CHEMBL2164299 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1795711 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL1795712 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL2163542 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2163536 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL2163544 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2163538 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL2163535 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2164297 | — | Ki | = | 1.29 | nM | 8.89 |
| CHEMBL2164295 | — | Ki | = | 1.51 | nM | 8.82 |
| CHEMBL2163539 | — | Ki | = | 1.58 | nM | 8.80 |
| CHEMBL2163541 | — | Ki | = | 1.62 | nM | 8.79 |
| CHEMBL2163537 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL2163546 | — | Ki | = | 2.75 | nM | 8.56 |
| CHEMBL2164296 | — | Ki | = | 3.16 | nM | 8.50 |
| CHEMBL2163543 | — | Ki | = | 4.97 | nM | 8.30 |
| CHEMBL2163532 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL2164300 | — | Ki | = | 9.15 | nM | 8.04 |
| CHEMBL2164301 | — | Ki | = | 9.35 | nM | 8.03 |
| CHEMBL2163534 | — | Ki | = | 12.16 | nM | 7.92 |
| CHEMBL2163540 | — | Ki | = | 14.27 | nM | 7.85 |
| CHEMBL2163531 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL2164298 | — | Ki | = | 25.79 | nM | 7.59 |
| CHEMBL2163545 | — | Ki | = | 34.91 | nM | 7.46 |
| CHEMBL1795713 | — | Ki | = | 47.22 | nM | 7.33 |
| CHEMBL2163533 | — | Ki | > | 100.0 | nM | - |
| CHEMBL2164299 | — | Ki | > | 100.0 | nM | - |