Assay Detail
Binding
CHEMBL872558
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | NIH3T3 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 8.14 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10009 | — | — | 1 | 10.30 |
| CHEMBL9772 | — | — | 1 | 10.22 |
| CHEMBL9997 | — | — | 1 | 9.92 |
| CHEMBL9590 | — | — | 1 | 9.80 |
| CHEMBL274317 | — | — | 1 | 9.77 |
| CHEMBL10099 | — | — | 1 | 9.70 |
| CHEMBL274896 | — | — | 1 | 9.68 |
| CHEMBL9630 | — | — | 1 | 9.59 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 9.48 |
| CHEMBL274438 | — | — | 1 | 9.30 |
| CHEMBL274842 | — | — | 1 | 9.29 |
| CHEMBL10110 | — | — | 1 | 9.02 |
| CHEMBL10293 | — | — | 1 | 8.85 |
| CHEMBL9605 | — | — | 1 | 8.43 |
| CHEMBL274630 | — | — | 1 | 8.30 |
| CHEMBL9600 | — | — | 1 | 8.26 |
| CHEMBL275529 | — | — | 1 | 8.20 |
| CHEMBL10007 | — | — | 1 | 8.19 |
| CHEMBL273897 | — | — | 1 | 8.03 |
| CHEMBL10124 | — | — | 1 | 7.92 |
| CHEMBL10328 | — | — | 1 | 7.92 |
| CHEMBL9765 | — | — | 1 | 7.77 |
| CHEMBL269175 | — | — | 1 | 7.76 |
| CHEMBL276005 | — | — | 1 | 7.66 |
| CHEMBL9917 | — | — | 1 | 7.50 |
| CHEMBL273624 | — | — | 1 | 7.47 |
| CHEMBL9634 | — | — | 1 | 7.44 |
| CHEMBL286615 | LUZINDOLE | — | 1 | 7.35 |
| CHEMBL9838 | — | — | 1 | 7.34 |
| CHEMBL9791 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10009 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL9772 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL9997 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL9590 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL274317 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL10099 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL274896 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL9630 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL45 | MELATONIN | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL274438 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL274842 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL10110 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL10293 | — | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL9605 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL274630 | — | Ki | = | 5.01 | nM | 8.30 |
| CHEMBL9600 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL275529 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL10007 | — | Ki | = | 6.46 | nM | 8.19 |
| CHEMBL273897 | — | Ki | = | 9.33 | nM | 8.03 |
| CHEMBL10124 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL10328 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL9765 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL269175 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL276005 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL9917 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL273624 | — | Ki | = | 33.9 | nM | 7.47 |
| CHEMBL9634 | — | Ki | = | 36.3 | nM | 7.44 |
| CHEMBL286615 | LUZINDOLE | Ki | = | 44.7 | nM | 7.35 |
| CHEMBL9838 | — | Ki | = | 45.7 | nM | 7.34 |
| CHEMBL9791 | — | Ki | = | 52.5 | nM | 7.28 |
| CHEMBL9815 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL9935 | — | Ki | = | 85.1 | nM | 7.07 |
| CHEMBL274995 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL273623 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL10043 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL269670 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL276490 | — | Ki | = | 324.0 | nM | 6.49 |
| CHEMBL9950 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL9934 | — | Ki | = | 1120.0 | nM | 5.95 |