Assay Detail
Binding
CHEMBL3887790
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Dose-Displacement Binding Assay: Radioligand dose displacement assays used 0.4 nM [3H]-U69,593 (GE Healthcare, Piscataway, N.J.; 40 Ci/mmole) with 15 μg membrane protein (recombinant κ opioid receptor expressed in HEK 293 cells; in-house prep) in a final volume of 200 μl binding buffer (5% DMSO, 50 mM Trizma base, pH 7.4). Non-specific binding was determined in the presence of 10 μM unlabeled naloxone or U69,593. All reactions were performed in 96-well polypropylene plates for 1 hr at a temperature of about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Perkin Elmer, Shelton, Conn.) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by five filtration washes with 2001 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 1-2 hours.
94
Total Activities
94
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Buprenorphine analogs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 94 | 8.57 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4109154 | — | — | 1 | 10.85 |
| CHEMBL4108017 | — | — | 1 | 10.70 |
| CHEMBL4113058 | — | — | 1 | 10.40 |
| CHEMBL4112241 | — | — | 1 | 10.30 |
| CHEMBL3927136 | — | — | 1 | 10.22 |
| CHEMBL4115222 | — | — | 1 | 10.15 |
| CHEMBL4109954 | — | — | 1 | 10.15 |
| CHEMBL4111231 | — | — | 1 | 10.10 |
| CHEMBL4112656 | — | — | 1 | 10.10 |
| CHEMBL3916122 | — | — | 1 | 10.05 |
| CHEMBL4110639 | — | — | 1 | 10.05 |
| CHEMBL4106746 | — | — | 1 | 10.00 |
| CHEMBL4112294 | — | — | 1 | 9.96 |
| CHEMBL4112771 | — | — | 1 | 9.85 |
| CHEMBL3939745 | — | — | 1 | 9.85 |
| CHEMBL4107918 | — | — | 1 | 9.85 |
| CHEMBL4112472 | — | — | 1 | 9.82 |
| CHEMBL4114477 | — | — | 1 | 9.82 |
| CHEMBL4115153 | — | — | 1 | 9.82 |
| CHEMBL4107906 | — | — | 1 | 9.72 |
| CHEMBL4110449 | — | — | 1 | 9.70 |
| CHEMBL4115338 | — | — | 1 | 9.64 |
| CHEMBL4109652 | — | — | 1 | 9.62 |
| CHEMBL4107680 | — | — | 1 | 9.55 |
| CHEMBL4109061 | — | — | 1 | 9.54 |
| CHEMBL4112051 | — | — | 1 | 9.37 |
| CHEMBL4108066 | — | — | 1 | 9.37 |
| CHEMBL4111224 | — | — | 1 | 9.34 |
| CHEMBL4111233 | — | — | 1 | 9.28 |
| CHEMBL4110967 | — | — | 1 | 9.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4109154 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL4108017 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL4113058 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL4112241 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL3927136 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL4115222 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4109954 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4111231 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL4112656 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL3916122 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL4110639 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL4106746 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4112294 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL3939745 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4112771 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4107918 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4112472 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4114477 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4115153 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4107906 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL4110449 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4115338 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL4109652 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL4107680 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL4109061 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL4112051 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL4108066 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL4111224 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL4111233 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL4110967 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3908063 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL4112287 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL4108290 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL4110146 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL4106873 | — | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL4107821 | — | Ki | = | 1.16 | nM | 8.94 |
| CHEMBL4111717 | — | Ki | = | 1.37 | nM | 8.86 |
| CHEMBL4111594 | — | Ki | = | 1.39 | nM | 8.86 |
| CHEMBL4113221 | — | Ki | = | 1.57 | nM | 8.80 |
| CHEMBL4114523 | — | Ki | = | 1.58 | nM | 8.80 |
| CHEMBL4112155 | — | Ki | = | 1.71 | nM | 8.77 |
| CHEMBL4107210 | — | Ki | = | 1.76 | nM | 8.75 |
| CHEMBL4108301 | — | Ki | = | 2.43 | nM | 8.61 |
| CHEMBL4106985 | — | Ki | = | 2.51 | nM | 8.60 |
| CHEMBL4111124 | — | Ki | = | 2.55 | nM | 8.59 |
| CHEMBL3930729 | — | Ki | = | 2.55 | nM | 8.59 |
| CHEMBL4109220 | — | Ki | = | 2.75 | nM | 8.56 |
| CHEMBL4109818 | — | Ki | = | 2.76 | nM | 8.56 |
| CHEMBL4110056 | — | Ki | = | 2.86 | nM | 8.54 |
| CHEMBL4115091 | — | Ki | = | 4.18 | nM | 8.38 |