Assay Detail
Binding
CHEMBL713109
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Inhibition of 2-[125I]iodomelatonin binding to Melatonin receptor 3 (MT3) of Syrian hamster brain membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Ribosyldihydronicotinamide dehydrogenase [quinone] (CHEMBL3959) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.29 | 10.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300056 | — | — | 1 | 10.06 |
| CHEMBL300728 | — | — | 1 | 9.89 |
| CHEMBL52559 | — | — | 1 | 9.74 |
| CHEMBL53622 | — | — | 1 | 9.51 |
| CHEMBL300195 | — | — | 1 | 8.96 |
| CHEMBL33700 | — | — | 1 | 8.55 |
| CHEMBL55084 | — | — | 1 | 8.21 |
| CHEMBL289233 | IODOMELATONIN | — | 1 | 8.19 |
| CHEMBL45 | MELATONIN | 4.0 | 1 | 7.25 |
| CHEMBL52755 | — | — | 1 | 7.16 |
| CHEMBL300729 | — | — | 1 | 6.00 |
| CHEMBL298335 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300056 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL300728 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL52559 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL53622 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL300195 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL33700 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL55084 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL289233 | IODOMELATONIN | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL45 | MELATONIN | Ki | = | 56.9 | nM | 7.25 |
| CHEMBL52755 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL300729 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL298335 | — | Ki | = | 1000.0 | nM | 6.00 |