Assay Detail
Binding
CHEMBL910349
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Inhibition of [3H]diprenorphine binding to human KOR expressed in CHO cells
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 7.25 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | 1.0 | 2 | 8.89 |
| CHEMBL290543 | — | — | 1 | 8.85 |
| CHEMBL212648 | — | — | 1 | 8.80 |
| CHEMBL386883 | — | — | 1 | 8.64 |
| CHEMBL212647 | — | — | 1 | 8.49 |
| CHEMBL379138 | — | — | 1 | 8.31 |
| CHEMBL386665 | — | — | 1 | 8.16 |
| CHEMBL370272 | — | — | 1 | 8.14 |
| CHEMBL378635 | DEOXY SALVINORIN A | — | 1 | 8.10 |
| CHEMBL213074 | — | — | 1 | 7.78 |
| CHEMBL212435 | — | — | 1 | 7.75 |
| CHEMBL424902 | — | — | 1 | 7.56 |
| CHEMBL384411 | — | — | 1 | 7.54 |
| CHEMBL215389 | — | — | 1 | 7.42 |
| CHEMBL385548 | — | — | 1 | 7.19 |
| CHEMBL213567 | — | — | 1 | 7.04 |
| CHEMBL215301 | — | — | 1 | 6.93 |
| CHEMBL435108 | SALVINORIN A (ESTER) | — | 1 | 6.85 |
| CHEMBL213155 | — | — | 1 | 6.83 |
| CHEMBL424698 | SALVINORIN B | — | 1 | 6.81 |
| CHEMBL212483 | — | — | 1 | 6.78 |
| CHEMBL413774 | — | — | 1 | 6.66 |
| CHEMBL212714 | — | — | 1 | 6.65 |
| CHEMBL214144 | — | — | 1 | 6.62 |
| CHEMBL215560 | — | — | 1 | 6.48 |
| CHEMBL213399 | — | — | 1 | 6.48 |
| CHEMBL212022 | — | — | 1 | 6.43 |
| CHEMBL384403 | — | — | 1 | 6.42 |
| CHEMBL378767 | — | — | 1 | 6.37 |
| CHEMBL385846 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL290543 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL212648 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL386883 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL445332 | SALVINORIN A | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL212647 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL379138 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL386665 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL370272 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL378635 | DEOXY SALVINORIN A | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL213074 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL212435 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL424902 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL384411 | — | Ki | = | 28.9 | nM | 7.54 |
| CHEMBL215389 | — | Ki | = | 38.1 | nM | 7.42 |
| CHEMBL385548 | — | Ki | = | 65.2 | nM | 7.19 |
| CHEMBL213567 | — | Ki | = | 90.9 | nM | 7.04 |
| CHEMBL215301 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL435108 | SALVINORIN A (ESTER) | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL213155 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL424698 | SALVINORIN B | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL212483 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL413774 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL212714 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL214144 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL215560 | — | Ki | = | 328.0 | nM | 6.48 |
| CHEMBL213399 | — | Ki | = | 332.0 | nM | 6.48 |
| CHEMBL212022 | — | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL384403 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL378767 | — | Ki | = | 424.0 | nM | 6.37 |
| CHEMBL385846 | — | Ki | = | 641.0 | nM | 6.19 |
| CHEMBL214491 | — | Ki | = | 665.0 | nM | 6.18 |
| CHEMBL385591 | — | Ki | = | 769.0 | nM | 6.11 |
| CHEMBL215938 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL215319 | — | Ki | = | 1392.0 | nM | 5.86 |
| CHEMBL426689 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL212702 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL410682 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL215076 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL438617 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL214528 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL212385 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL425249 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL212704 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL215882 | — | Ki | - | — | - | |
| CHEMBL379268 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL379954 | — | Ki | - | — | - | |
| CHEMBL212838 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL214018 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL378716 | — | Ki | > | 10000.0 | nM | - |