Assay Detail
Binding
CHEMBL3887791
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Dose-Displacement Binding Assay: Delta-opioid Receptor Binding Assay Procedures were conducted as follows. Radioligand dose-displacement assays used 0.3 nM [3H]-Naltrindole (Perkin Elmer, Shelton, Conn.; 33.0 Ci/mmole) with 5 ug membrane protein (Perkin Elmer, Shelton, Conn.) in a final volume of 500 ul binding buffer (5 mM MgCl2, 5% DMSO, 50 mM Trizma base, pH 7.4). Non-specific binding was determined in the presence of 25 uM unlabeled naloxone. All reactions were performed in 96-deep 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 500 ul ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 1-2 hours.
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Buprenorphine analogs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 54 | 6.37 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4115222 | — | — | 1 | 8.91 |
| CHEMBL4110639 | — | — | 1 | 8.62 |
| CHEMBL4111231 | — | — | 1 | 7.86 |
| CHEMBL3916122 | — | — | 1 | 7.82 |
| CHEMBL4111124 | — | — | 1 | 7.60 |
| CHEMBL4111224 | — | — | 1 | 7.49 |
| CHEMBL4115091 | — | — | 1 | 7.37 |
| CHEMBL4111717 | — | — | 1 | 7.20 |
| CHEMBL4107918 | — | — | 1 | 7.09 |
| CHEMBL4107906 | — | — | 1 | 7.03 |
| CHEMBL4107681 | — | — | 1 | 6.92 |
| CHEMBL4107627 | — | — | 1 | 6.86 |
| CHEMBL4107821 | — | — | 1 | 6.82 |
| CHEMBL4109061 | — | — | 1 | 6.78 |
| CHEMBL4115338 | — | — | 1 | 6.76 |
| CHEMBL4112472 | — | — | 1 | 6.74 |
| CHEMBL4114477 | — | — | 1 | 6.73 |
| CHEMBL4108017 | — | — | 1 | 6.71 |
| CHEMBL4113804 | — | — | 1 | 6.68 |
| CHEMBL4110312 | — | — | 1 | 6.57 |
| CHEMBL4106985 | — | — | 1 | 6.56 |
| CHEMBL4107470 | — | — | 1 | 6.50 |
| CHEMBL4112656 | — | — | 1 | 6.47 |
| CHEMBL4111244 | — | — | 1 | 6.45 |
| CHEMBL4108066 | — | — | 1 | 6.42 |
| CHEMBL4112771 | — | — | 1 | 6.41 |
| CHEMBL4107680 | — | — | 1 | 6.39 |
| CHEMBL4106544 | — | — | 1 | 6.33 |
| CHEMBL4109142 | — | — | 1 | 6.33 |
| CHEMBL4113058 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4115222 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL4110639 | — | Ki | = | 2.38 | nM | 8.62 |
| CHEMBL4111231 | — | Ki | = | 13.81 | nM | 7.86 |
| CHEMBL3916122 | — | Ki | = | 15.01 | nM | 7.82 |
| CHEMBL4111124 | — | Ki | = | 25.38 | nM | 7.60 |
| CHEMBL4111224 | — | Ki | = | 32.24 | nM | 7.49 |
| CHEMBL4115091 | — | Ki | = | 43.05 | nM | 7.37 |
| CHEMBL4111717 | — | Ki | = | 63.02 | nM | 7.20 |
| CHEMBL4107918 | — | Ki | = | 81.93 | nM | 7.09 |
| CHEMBL4107906 | — | Ki | = | 92.5 | nM | 7.03 |
| CHEMBL4107681 | — | Ki | = | 118.99 | nM | 6.92 |
| CHEMBL4107627 | — | Ki | = | 138.07 | nM | 6.86 |
| CHEMBL4107821 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL4109061 | — | Ki | = | 165.88 | nM | 6.78 |
| CHEMBL4115338 | — | Ki | = | 174.45 | nM | 6.76 |
| CHEMBL4112472 | — | Ki | = | 180.4 | nM | 6.74 |
| CHEMBL4114477 | — | Ki | = | 184.83 | nM | 6.73 |
| CHEMBL4108017 | — | Ki | = | 194.89 | nM | 6.71 |
| CHEMBL4113804 | — | Ki | = | 211.03 | nM | 6.68 |
| CHEMBL4110312 | — | Ki | = | 269.62 | nM | 6.57 |
| CHEMBL4106985 | — | Ki | = | 277.58 | nM | 6.56 |
| CHEMBL4107470 | — | Ki | = | 317.88 | nM | 6.50 |
| CHEMBL4112656 | — | Ki | = | 341.52 | nM | 6.47 |
| CHEMBL4111244 | — | Ki | = | 355.13 | nM | 6.45 |
| CHEMBL4108066 | — | Ki | = | 380.74 | nM | 6.42 |
| CHEMBL4112771 | — | Ki | = | 387.09 | nM | 6.41 |
| CHEMBL4107680 | — | Ki | = | 410.59 | nM | 6.39 |
| CHEMBL4106544 | — | Ki | = | 468.09 | nM | 6.33 |
| CHEMBL4109142 | — | Ki | = | 469.9 | nM | 6.33 |
| CHEMBL4113058 | — | Ki | = | 493.55 | nM | 6.31 |
| CHEMBL4109220 | — | Ki | = | 517.28 | nM | 6.29 |
| CHEMBL4111378 | — | Ki | = | 617.83 | nM | 6.21 |
| CHEMBL4114002 | — | Ki | = | 667.33 | nM | 6.18 |
| CHEMBL4112051 | — | Ki | = | 729.1 | nM | 6.14 |
| CHEMBL4111803 | — | Ki | = | 739.45 | nM | 6.13 |
| CHEMBL4111233 | — | Ki | = | 743.43 | nM | 6.13 |
| CHEMBL4115652 | — | Ki | = | 1004.92 | nM | 6.00 |
| CHEMBL4109778 | — | Ki | = | 1054.82 | nM | 5.98 |
| CHEMBL4112155 | — | Ki | = | 1479.53 | nM | 5.83 |
| CHEMBL3930597 | — | Ki | = | 1704.16 | nM | 5.77 |
| CHEMBL4108301 | — | Ki | = | 1732.46 | nM | 5.76 |
| CHEMBL4109389 | — | Ki | = | 1983.26 | nM | 5.70 |
| CHEMBL4112358 | — | Ki | = | 2425.67 | nM | 5.62 |
| CHEMBL4113830 | — | Ki | = | 3024.75 | nM | 5.52 |
| CHEMBL4114523 | — | Ki | = | 3001.22 | nM | 5.52 |
| CHEMBL4113221 | — | Ki | = | 3254.47 | nM | 5.49 |
| CHEMBL4107537 | — | Ki | = | 3615.75 | nM | 5.44 |
| CHEMBL4107210 | — | Ki | = | 3710.17 | nM | 5.43 |
| CHEMBL4110440 | — | Ki | = | 4096.83 | nM | 5.39 |
| CHEMBL4106700 | — | Ki | = | 5530.06 | nM | 5.26 |