Assay Detail
Functional
CHEMBL1019891
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human cloned kappa opioid receptor expressed in CHO cells assessed as inhibition of U50488-induced [35S]GTPgammaS binding
34
Total Activities
17
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 20 | - | - |
| IC50 | 7 | 6.95 | 7.82 |
| Imax | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 2 | 7.82 |
| CHEMBL517567 | — | — | 2 | 6.85 |
| CHEMBL464230 | — | — | 2 | 6.19 |
| CHEMBL517779 | — | — | 2 | - |
| CHEMBL33986 | BUTORPHANOL | 4.0 | 2 | - |
| CHEMBL511691 | — | — | 2 | - |
| CHEMBL2107292 | KETAZOCINE | 2.0 | 2 | - |
| CHEMBL459746 | — | — | 2 | - |
| CHEMBL464071 | — | — | 2 | - |
| CHEMBL517166 | — | — | 2 | - |
| CHEMBL2367604 | — | — | 2 | - |
| CHEMBL3275494 | — | — | 2 | - |
| CHEMBL511884 | — | — | 2 | - |
| CHEMBL257661 | METAZOCINE | 2.0 | 2 | - |
| CHEMBL297428 | — | — | 2 | - |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 2 | - |
| CHEMBL290543 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511142 | BUPRENORPHINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL517567 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL464230 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL464071 | — | IC50 | - | — | - | |
| CHEMBL517567 | — | Imax | = | 59.0 | % | - |
| CHEMBL464071 | — | Imax | - | — | - | |
| CHEMBL459746 | — | IC50 | - | — | - | |
| CHEMBL459746 | — | Imax | - | — | - | |
| CHEMBL2107292 | KETAZOCINE | Activity | - | — | - | |
| CHEMBL2107292 | KETAZOCINE | Activity | - | — | - | |
| CHEMBL511691 | — | Activity | - | — | - | |
| CHEMBL511691 | — | Activity | - | — | - | |
| CHEMBL33986 | BUTORPHANOL | Activity | - | — | - | |
| CHEMBL33986 | BUTORPHANOL | Activity | - | — | - | |
| CHEMBL517779 | — | Activity | - | — | - | |
| CHEMBL517779 | — | Activity | - | — | - | |
| CHEMBL464230 | — | Imax | = | 49.0 | % | - |
| CHEMBL511142 | BUPRENORPHINE | Imax | = | 24.0 | % | - |
| CHEMBL517166 | — | Imax | - | — | - | |
| CHEMBL290543 | — | Activity | - | — | - | |
| CHEMBL56585 | CYCLAZOCINE | Activity | - | — | - | |
| CHEMBL56585 | CYCLAZOCINE | Activity | - | — | - | |
| CHEMBL297428 | — | Activity | - | — | - | |
| CHEMBL297428 | — | Activity | - | — | - | |
| CHEMBL257661 | METAZOCINE | Activity | - | — | - | |
| CHEMBL257661 | METAZOCINE | Activity | - | — | - | |
| CHEMBL511884 | — | IC50 | - | — | - | |
| CHEMBL511884 | — | Imax | - | — | - | |
| CHEMBL3275494 | — | Activity | - | — | - | |
| CHEMBL3275494 | — | Activity | - | — | - | |
| CHEMBL2367604 | — | Activity | - | — | - | |
| CHEMBL2367604 | — | Activity | - | — | - | |
| CHEMBL290543 | — | Activity | - | — | - | |
| CHEMBL517166 | — | IC50 | - | — | - |