Assay Detail
Binding
CHEMBL3887789
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Dose-Displacement Binding Assay: Radioligand dose-displacement binding assays for t-opioid receptors used 0.3 nM [3H]-diprenorphine (Perkin Elmer, Shelton, Conn.), with 5 mg membrane protein/well in a final volume of 500 ul binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Perkin Elmer, Shelton, Conn.), presoaked in 0.5% polyethylenimine using a 96-well tissue harvester (Perkin Elmer, Shelton, Conn.) followed by performing three filtration washes with 500 ul of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Perkin Elmer, Shelton, Conn.) was added (50 ul/well), and plates were counted using a Packard Top-Count.
90
Total Activities
90
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 | 90 | 7.39 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3927136 | — | — | 1 | 9.82 |
| CHEMBL4115222 | — | — | 1 | 9.72 |
| CHEMBL4106746 | — | — | 1 | 9.47 |
| CHEMBL4110639 | — | — | 1 | 9.03 |
| CHEMBL4115153 | — | — | 1 | 8.93 |
| CHEMBL4111231 | — | — | 1 | 8.88 |
| CHEMBL3939745 | — | — | 1 | 8.85 |
| CHEMBL3916122 | — | — | 1 | 8.82 |
| CHEMBL4112287 | — | — | 1 | 8.75 |
| CHEMBL4107680 | — | — | 1 | 8.69 |
| CHEMBL4106722 | — | — | 1 | 8.48 |
| CHEMBL4111224 | — | — | 1 | 8.38 |
| CHEMBL4107906 | — | — | 1 | 8.36 |
| CHEMBL4107918 | — | — | 1 | 8.33 |
| CHEMBL3908063 | — | — | 1 | 8.27 |
| CHEMBL4106985 | — | — | 1 | 8.20 |
| CHEMBL4111124 | — | — | 1 | 8.17 |
| CHEMBL4111594 | — | — | 1 | 8.14 |
| CHEMBL4107821 | — | — | 1 | 8.12 |
| CHEMBL4109653 | — | — | 1 | 8.11 |
| CHEMBL4109061 | — | — | 1 | 8.06 |
| CHEMBL4113058 | — | — | 1 | 8.04 |
| CHEMBL4112771 | — | — | 1 | 7.93 |
| CHEMBL4110146 | — | — | 1 | 7.88 |
| CHEMBL4108066 | — | — | 1 | 7.85 |
| CHEMBL4107627 | — | — | 1 | 7.84 |
| CHEMBL4109267 | — | — | 1 | 7.82 |
| CHEMBL3969293 | — | — | 1 | 7.82 |
| CHEMBL4113804 | — | — | 1 | 7.80 |
| CHEMBL4115338 | — | — | 1 | 7.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3927136 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4115222 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL4106746 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL4110639 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL4115153 | — | Ki | = | 1.17 | nM | 8.93 |
| CHEMBL4111231 | — | Ki | = | 1.33 | nM | 8.88 |
| CHEMBL3939745 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3916122 | — | Ki | = | 1.52 | nM | 8.82 |
| CHEMBL4112287 | — | Ki | = | 1.76 | nM | 8.75 |
| CHEMBL4107680 | — | Ki | = | 2.05 | nM | 8.69 |
| CHEMBL4106722 | — | Ki | = | 3.32 | nM | 8.48 |
| CHEMBL4111224 | — | Ki | = | 4.16 | nM | 8.38 |
| CHEMBL4107906 | — | Ki | = | 4.41 | nM | 8.36 |
| CHEMBL4107918 | — | Ki | = | 4.69 | nM | 8.33 |
| CHEMBL3908063 | — | Ki | = | 5.42 | nM | 8.27 |
| CHEMBL4106985 | — | Ki | = | 6.29 | nM | 8.20 |
| CHEMBL4111124 | — | Ki | = | 6.72 | nM | 8.17 |
| CHEMBL4111594 | — | Ki | = | 7.29 | nM | 8.14 |
| CHEMBL4107821 | — | Ki | = | 7.65 | nM | 8.12 |
| CHEMBL4109653 | — | Ki | = | 7.79 | nM | 8.11 |
| CHEMBL4109061 | — | Ki | = | 8.69 | nM | 8.06 |
| CHEMBL4113058 | — | Ki | = | 9.01 | nM | 8.04 |
| CHEMBL4112771 | — | Ki | = | 11.79 | nM | 7.93 |
| CHEMBL4110146 | — | Ki | = | 13.09 | nM | 7.88 |
| CHEMBL4108066 | — | Ki | = | 14.02 | nM | 7.85 |
| CHEMBL4107627 | — | Ki | = | 14.29 | nM | 7.84 |
| CHEMBL3969293 | — | Ki | = | 15.09 | nM | 7.82 |
| CHEMBL4109267 | — | Ki | = | 14.98 | nM | 7.82 |
| CHEMBL4113804 | — | Ki | = | 15.83 | nM | 7.80 |
| CHEMBL4115338 | — | Ki | = | 16.36 | nM | 7.79 |
| CHEMBL4114477 | — | Ki | = | 17.25 | nM | 7.76 |
| CHEMBL4108017 | — | Ki | = | 17.42 | nM | 7.76 |
| CHEMBL4111803 | — | Ki | = | 19.04 | nM | 7.72 |
| CHEMBL4112051 | — | Ki | = | 19.39 | nM | 7.71 |
| CHEMBL4109142 | — | Ki | = | 20.39 | nM | 7.69 |
| CHEMBL4112656 | — | Ki | = | 20.7 | nM | 7.68 |
| CHEMBL4111233 | — | Ki | = | 20.74 | nM | 7.68 |
| CHEMBL3930729 | — | Ki | = | 24.41 | nM | 7.61 |
| CHEMBL4110312 | — | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL4111717 | — | Ki | = | 29.33 | nM | 7.53 |
| CHEMBL4107537 | — | Ki | = | 32.04 | nM | 7.49 |
| CHEMBL4110056 | — | Ki | = | 35.79 | nM | 7.45 |
| CHEMBL4115091 | — | Ki | = | 36.46 | nM | 7.44 |
| CHEMBL4112358 | — | Ki | = | 37.54 | nM | 7.43 |
| CHEMBL4109652 | — | Ki | = | 49.26 | nM | 7.31 |
| CHEMBL4106544 | — | Ki | = | 49.98 | nM | 7.30 |
| CHEMBL4113830 | — | Ki | = | 51.1 | nM | 7.29 |
| CHEMBL4109258 | — | Ki | = | 54.23 | nM | 7.27 |
| CHEMBL4109220 | — | Ki | = | 54.83 | nM | 7.26 |
| CHEMBL4114486 | — | Ki | = | 55.53 | nM | 7.25 |