Assay Detail
Binding
CHEMBL3887216
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: The receptor affinity for the human mu-opiate receptor was determined in a homogeneous batch in microtitre plates. For this, dilution series of the particular spirocyclic cyclohexane derivative to be tested were incubated in a total volume of 250 ul for 90 minutes at room temperature with a receptor membrane preparation (15-40 ug protein per 250 ul incubation batch) of CHO-K1 cells, which express the human mu-opiate receptor (RB-HOM receptor membrane preparation of NEN, Zaventem, Belgium), in the presence of 1 nmol/l of the radioactive ligand [3H]-naloxone (NET719, NEN, Zaventem, Belgium) and of 1 mg WGA-SPA beads (wheat germ agglutinin SPA beads from Amersham/Pharmacia, Freiburg, Germany). 50 mmoles/l Tris-HCl supplemented with 0.05 wt. % sodium azide and with 0.06 wt. % bovine serum albumin was used as the incubation buffer. 25 umoles/l naloxone was additionally added for determination of the non-specific binding.
34
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Process for preparing spirocyclic cyclohexane compounds, compositions containing such compounds and method of using such compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 8.32 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3894898 | — | — | 2 | 9.44 |
| CHEMBL3894557 | — | — | 1 | 9.30 |
| CHEMBL3959398 | — | — | 3 | 9.22 |
| CHEMBL3966641 | — | — | 1 | 9.22 |
| CHEMBL3954763 | — | — | 1 | 9.15 |
| CHEMBL3959597 | — | — | 1 | 8.96 |
| CHEMBL3953613 | — | — | 1 | 8.92 |
| CHEMBL3962932 | — | — | 2 | 8.82 |
| CHEMBL3890825 | — | — | 1 | 8.77 |
| CHEMBL3924497 | — | — | 1 | 8.70 |
| CHEMBL3961861 | — | — | 1 | 8.68 |
| CHEMBL3919062 | — | — | 2 | 8.66 |
| CHEMBL3892859 | — | — | 1 | 8.64 |
| CHEMBL3958404 | — | — | 1 | 8.57 |
| CHEMBL3914982 | — | — | 1 | 8.57 |
| CHEMBL3980449 | — | — | 1 | 8.51 |
| CHEMBL3942233 | — | — | 2 | 8.18 |
| CHEMBL3909973 | — | — | 1 | 8.17 |
| CHEMBL3909755 | — | — | 1 | 8.14 |
| CHEMBL3909041 | — | — | 2 | 7.92 |
| CHEMBL3892273 | — | — | 1 | 7.85 |
| CHEMBL3973336 | — | — | 1 | 7.85 |
| CHEMBL3979202 | — | — | 1 | 7.82 |
| CHEMBL3899983 | — | — | 1 | 7.77 |
| CHEMBL3895920 | — | — | 1 | 7.72 |
| CHEMBL3936891 | — | — | 1 | 7.24 |
| CHEMBL3983394 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3894898 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL3894557 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3966641 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3959398 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3954763 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3959597 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3953613 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3959398 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3962932 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3890825 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3924497 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3961861 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3919062 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3892859 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL3958404 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3914982 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3980449 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3919062 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL3894898 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL3942233 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL3909973 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL3909755 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL3962932 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3909041 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3892273 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3973336 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3979202 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3899983 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3895920 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3942233 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3909041 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3936891 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3983394 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL3959398 | — | Ki | = | 310.0 | nM | 6.51 |