Assay Detail
Functional
CHEMBL912003
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Activity at metastin receptor expressed in HEK293 cells by measuring calcium release
41
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| EC50 | 41 | 6.74 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221602 | — | — | 1 | 7.95 |
| CHEMBL435315 | — | — | 1 | 7.93 |
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 7.76 |
| CHEMBL220855 | — | — | 1 | 7.75 |
| CHEMBL221761 | — | — | 1 | 7.65 |
| CHEMBL373467 | — | — | 2 | 7.64 |
| CHEMBL434382 | — | — | 1 | 7.60 |
| CHEMBL220759 | — | — | 1 | 7.59 |
| CHEMBL375982 | — | — | 1 | 7.53 |
| CHEMBL375450 | — | — | 1 | 7.52 |
| CHEMBL262577 | — | — | 1 | 7.47 |
| CHEMBL373676 | — | — | 1 | 7.40 |
| CHEMBL414073 | — | — | 2 | 7.33 |
| CHEMBL375432 | — | — | 1 | 7.16 |
| CHEMBL434379 | — | — | 1 | 7.15 |
| CHEMBL385105 | — | — | 1 | 7.06 |
| CHEMBL435922 | — | — | 1 | 7.06 |
| CHEMBL375395 | — | — | 1 | 7.04 |
| CHEMBL374260 | — | — | 1 | 6.99 |
| CHEMBL375006 | — | — | 1 | 6.99 |
| CHEMBL439094 | — | — | 1 | 6.96 |
| CHEMBL386958 | — | — | 1 | 6.96 |
| CHEMBL374246 | — | — | 1 | 6.67 |
| CHEMBL221764 | — | — | 1 | 6.67 |
| CHEMBL375983 | — | — | 1 | 6.54 |
| CHEMBL441935 | — | — | 1 | 6.54 |
| CHEMBL374077 | — | — | 1 | 6.54 |
| CHEMBL373714 | — | — | 1 | 6.46 |
| CHEMBL221816 | — | — | 1 | 6.41 |
| CHEMBL374295 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221602 | — | EC50 | = | 11.3 | nM | 7.95 |
| CHEMBL435315 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL376756 | KISSPEPTIN-10 | EC50 | = | 17.3 | nM | 7.76 |
| CHEMBL220855 | — | EC50 | = | 17.6 | nM | 7.75 |
| CHEMBL221761 | — | EC50 | = | 22.2 | nM | 7.65 |
| CHEMBL373467 | — | EC50 | = | 22.8 | nM | 7.64 |
| CHEMBL434382 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL220759 | — | EC50 | = | 25.8 | nM | 7.59 |
| CHEMBL375982 | — | EC50 | = | 29.4 | nM | 7.53 |
| CHEMBL375450 | — | EC50 | = | 30.3 | nM | 7.52 |
| CHEMBL373467 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL262577 | — | EC50 | = | 33.8 | nM | 7.47 |
| CHEMBL373676 | — | EC50 | = | 39.5 | nM | 7.40 |
| CHEMBL414073 | — | EC50 | = | 46.3 | nM | 7.33 |
| CHEMBL375432 | — | EC50 | = | 69.8 | nM | 7.16 |
| CHEMBL434379 | — | EC50 | = | 70.8 | nM | 7.15 |
| CHEMBL385105 | — | EC50 | = | 87.8 | nM | 7.06 |
| CHEMBL435922 | — | EC50 | = | 86.7 | nM | 7.06 |
| CHEMBL375395 | — | EC50 | = | 91.7 | nM | 7.04 |
| CHEMBL375006 | — | EC50 | = | 101.4 | nM | 6.99 |
| CHEMBL374260 | — | EC50 | = | 102.9 | nM | 6.99 |
| CHEMBL439094 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL386958 | — | EC50 | = | 108.3 | nM | 6.96 |
| CHEMBL374246 | — | EC50 | = | 215.2 | nM | 6.67 |
| CHEMBL221764 | — | EC50 | = | 213.7 | nM | 6.67 |
| CHEMBL441935 | — | EC50 | = | 290.3 | nM | 6.54 |
| CHEMBL375983 | — | EC50 | = | 285.0 | nM | 6.54 |
| CHEMBL374077 | — | EC50 | = | 290.2 | nM | 6.54 |
| CHEMBL373714 | — | EC50 | = | 347.5 | nM | 6.46 |
| CHEMBL221816 | — | EC50 | = | 385.2 | nM | 6.41 |
| CHEMBL414073 | — | EC50 | = | 392.8 | nM | 6.41 |
| CHEMBL374295 | — | EC50 | = | 644.8 | nM | 6.19 |
| CHEMBL414811 | — | EC50 | = | 791.8 | nM | 6.10 |
| CHEMBL220853 | — | EC50 | = | 1068.5 | nM | 5.97 |
| CHEMBL221817 | — | EC50 | = | 2097.3 | nM | 5.68 |
| CHEMBL410741 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL262316 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL221141 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL374748 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL373854 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL426552 | — | EC50 | = | 10000.0 | nM | 5.00 |