Assay Detail
Binding
CHEMBL912002
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Displacement of [125]metastin from metastin receptor
43
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 43 | 7.09 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375982 | — | — | 1 | 9.10 |
| CHEMBL373467 | — | — | 2 | 8.96 |
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 8.89 |
| CHEMBL262577 | — | — | 1 | 8.80 |
| CHEMBL221602 | — | — | 1 | 8.74 |
| CHEMBL220855 | — | — | 1 | 8.70 |
| CHEMBL414073 | — | — | 2 | 8.66 |
| CHEMBL435315 | — | — | 1 | 8.33 |
| CHEMBL221761 | — | — | 1 | 8.30 |
| CHEMBL434382 | — | — | 1 | 8.11 |
| CHEMBL375432 | — | — | 1 | 8.03 |
| CHEMBL374260 | — | — | 1 | 8.03 |
| CHEMBL375395 | — | — | 1 | 7.96 |
| CHEMBL220759 | — | — | 1 | 7.80 |
| CHEMBL434379 | — | — | 1 | 7.79 |
| CHEMBL375450 | — | — | 1 | 7.68 |
| CHEMBL386958 | — | — | 1 | 7.53 |
| CHEMBL373676 | — | — | 1 | 7.48 |
| CHEMBL439094 | — | — | 1 | 7.29 |
| CHEMBL385105 | — | — | 1 | 7.08 |
| CHEMBL221764 | — | — | 1 | 7.05 |
| CHEMBL374077 | — | — | 1 | 7.02 |
| CHEMBL375006 | — | — | 1 | 6.96 |
| CHEMBL441935 | — | — | 1 | 6.85 |
| CHEMBL221816 | — | — | 1 | 6.79 |
| CHEMBL435922 | — | — | 1 | 6.71 |
| CHEMBL375983 | — | — | 1 | 6.70 |
| CHEMBL373714 | — | — | 1 | 6.62 |
| CHEMBL374246 | — | — | 1 | 6.53 |
| CHEMBL221817 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375982 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL373467 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL376756 | KISSPEPTIN-10 | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL262577 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL221602 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL220855 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL414073 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL435315 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL221761 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL434382 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL374260 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL375432 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL373467 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL375395 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL220759 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL434379 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL375450 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL386958 | — | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL373676 | — | Ki | = | 33.4 | nM | 7.48 |
| CHEMBL439094 | — | Ki | = | 51.5 | nM | 7.29 |
| CHEMBL414073 | — | Ki | = | 80.8 | nM | 7.09 |
| CHEMBL385105 | — | Ki | = | 82.7 | nM | 7.08 |
| CHEMBL221764 | — | Ki | = | 88.1 | nM | 7.05 |
| CHEMBL374077 | — | Ki | = | 94.8 | nM | 7.02 |
| CHEMBL375006 | — | Ki | = | 109.6 | nM | 6.96 |
| CHEMBL441935 | — | Ki | = | 141.8 | nM | 6.85 |
| CHEMBL221816 | — | Ki | = | 161.8 | nM | 6.79 |
| CHEMBL435922 | — | Ki | = | 196.7 | nM | 6.71 |
| CHEMBL375983 | — | Ki | = | 198.3 | nM | 6.70 |
| CHEMBL373714 | — | Ki | = | 240.2 | nM | 6.62 |
| CHEMBL374246 | — | Ki | = | 298.2 | nM | 6.53 |
| CHEMBL221817 | — | Ki | = | 494.9 | nM | 6.30 |
| CHEMBL220853 | — | Ki | = | 551.8 | nM | 6.26 |
| CHEMBL218690 | — | Ki | = | 708.0 | nM | 6.15 |
| CHEMBL414811 | — | Ki | = | 775.2 | nM | 6.11 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL426552 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL374748 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL221141 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL262316 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL410741 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL374295 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL373854 | — | Ki | = | 10000.0 | nM | 5.00 |