Assay Detail
Functional
CHEMBL910350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 53 | 7.20 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212648 | — | — | 1 | 9.12 |
| CHEMBL445332 | SALVINORIN A | 1.0 | 2 | 8.66 |
| CHEMBL212647 | — | — | 1 | 8.62 |
| CHEMBL290543 | — | — | 1 | 8.35 |
| CHEMBL386883 | — | — | 1 | 8.14 |
| CHEMBL379138 | — | — | 1 | 8.00 |
| CHEMBL386665 | — | — | 1 | 7.90 |
| CHEMBL378635 | DEOXY SALVINORIN A | — | 1 | 7.73 |
| CHEMBL212435 | — | — | 1 | 7.72 |
| CHEMBL370272 | — | — | 1 | 7.69 |
| CHEMBL213074 | — | — | 1 | 7.68 |
| CHEMBL424902 | — | — | 1 | 7.60 |
| CHEMBL215389 | — | — | 1 | 7.43 |
| CHEMBL384411 | — | — | 1 | 7.16 |
| CHEMBL385548 | — | — | 1 | 7.14 |
| CHEMBL213155 | — | — | 1 | 6.73 |
| CHEMBL212483 | — | — | 1 | 6.62 |
| CHEMBL378767 | — | — | 1 | 6.51 |
| CHEMBL213399 | — | — | 1 | 6.47 |
| CHEMBL213567 | — | — | 1 | 6.46 |
| CHEMBL424698 | SALVINORIN B | — | 1 | 6.43 |
| CHEMBL413774 | — | — | 1 | 6.41 |
| CHEMBL212022 | — | — | 1 | 6.35 |
| CHEMBL435108 | SALVINORIN A (ESTER) | — | 1 | 6.28 |
| CHEMBL214144 | — | — | 1 | 6.19 |
| CHEMBL215301 | — | — | 1 | 6.14 |
| CHEMBL215560 | — | — | 1 | 6.08 |
| CHEMBL384403 | — | — | 1 | 6.07 |
| CHEMBL212714 | — | — | 1 | 5.86 |
| CHEMBL379954 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212648 | — | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL445332 | SALVINORIN A | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL212647 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL445332 | SALVINORIN A | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL290543 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL386883 | — | EC50 | = | 7.2 | nM | 8.14 |
| CHEMBL379138 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL386665 | — | EC50 | = | 12.6 | nM | 7.90 |
| CHEMBL378635 | DEOXY SALVINORIN A | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL212435 | — | EC50 | = | 18.9 | nM | 7.72 |
| CHEMBL370272 | — | EC50 | = | 20.4 | nM | 7.69 |
| CHEMBL213074 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL424902 | — | EC50 | = | 25.2 | nM | 7.60 |
| CHEMBL215389 | — | EC50 | = | 37.2 | nM | 7.43 |
| CHEMBL384411 | — | EC50 | = | 68.9 | nM | 7.16 |
| CHEMBL385548 | — | EC50 | = | 72.8 | nM | 7.14 |
| CHEMBL213155 | — | EC50 | = | 188.0 | nM | 6.73 |
| CHEMBL212483 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL378767 | — | EC50 | = | 306.0 | nM | 6.51 |
| CHEMBL213399 | — | EC50 | = | 339.0 | nM | 6.47 |
| CHEMBL213567 | — | EC50 | = | 343.0 | nM | 6.46 |
| CHEMBL424698 | SALVINORIN B | EC50 | = | 371.0 | nM | 6.43 |
| CHEMBL413774 | — | EC50 | = | 389.0 | nM | 6.41 |
| CHEMBL212022 | — | EC50 | = | 444.0 | nM | 6.35 |
| CHEMBL435108 | SALVINORIN A (ESTER) | EC50 | = | 531.0 | nM | 6.28 |
| CHEMBL214144 | — | EC50 | = | 641.0 | nM | 6.19 |
| CHEMBL215301 | — | EC50 | = | 718.0 | nM | 6.14 |
| CHEMBL215560 | — | EC50 | = | 825.0 | nM | 6.08 |
| CHEMBL384403 | — | EC50 | = | 857.0 | nM | 6.07 |
| CHEMBL212714 | — | EC50 | = | 1373.0 | nM | 5.86 |
| CHEMBL215938 | — | EC50 | - | — | - | |
| CHEMBL426689 | — | EC50 | - | — | - | |
| CHEMBL212704 | — | EC50 | - | — | - | |
| CHEMBL378716 | — | EC50 | - | — | - | |
| CHEMBL385591 | — | EC50 | - | — | - | |
| CHEMBL385846 | — | EC50 | - | — | - | |
| CHEMBL214491 | — | EC50 | - | — | - | |
| CHEMBL212385 | — | EC50 | - | — | - | |
| CHEMBL214528 | — | EC50 | - | — | - | |
| CHEMBL438617 | — | EC50 | - | — | - | |
| CHEMBL215076 | — | EC50 | - | — | - | |
| CHEMBL214018 | — | EC50 | - | — | - | |
| CHEMBL212702 | — | EC50 | - | — | - | |
| CHEMBL425249 | — | EC50 | - | — | - | |
| CHEMBL215882 | — | EC50 | - | — | - | |
| CHEMBL212562 | — | EC50 | - | — | - | |
| CHEMBL384860 | — | EC50 | - | — | - | |
| CHEMBL410682 | — | EC50 | - | — | - | |
| CHEMBL379954 | — | EC50 | - | — | - | |
| CHEMBL378690 | — | EC50 | - | — | - |