Assay Detail
Functional
CHEMBL3376866
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Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 9.07 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3314223 | — | — | 1 | 9.52 |
| CHEMBL3314217 | — | — | 1 | 9.51 |
| CHEMBL3314224 | — | — | 1 | 9.48 |
| CHEMBL3314227 | — | — | 1 | 9.36 |
| CHEMBL3315315 | — | — | 1 | 9.36 |
| CHEMBL3314220 | — | — | 1 | 9.31 |
| CHEMBL3314215 | — | — | 1 | 9.29 |
| CHEMBL3314212 | — | — | 1 | 9.23 |
| CHEMBL3314221 | — | — | 1 | 9.20 |
| CHEMBL3314222 | — | — | 1 | 9.19 |
| CHEMBL3314218 | — | — | 1 | 9.15 |
| CHEMBL3314228 | — | — | 1 | 9.12 |
| CHEMBL3314225 | — | — | 1 | 9.10 |
| CHEMBL3314226 | — | — | 1 | 9.09 |
| CHEMBL3314207 | — | — | 1 | 9.06 |
| CHEMBL3314229 | — | — | 1 | 9.03 |
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 9.02 |
| CHEMBL3314216 | — | — | 1 | 9.00 |
| CHEMBL3314213 | — | — | 1 | 8.92 |
| CHEMBL3314219 | — | — | 1 | 8.89 |
| CHEMBL3314211 | — | — | 1 | 8.82 |
| CHEMBL3314208 | — | — | 1 | 8.80 |
| CHEMBL3314209 | — | — | 1 | 8.74 |
| CHEMBL3086284 | KISS1-305 | — | 1 | 8.59 |
| CHEMBL3314214 | — | — | 1 | 8.55 |
| CHEMBL3314210 | — | — | 1 | 8.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3314223 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3314217 | — | EC50 | = | 0.31 | nM | 9.51 |
| CHEMBL3314224 | — | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL3314227 | — | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL3315315 | — | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL3314220 | — | EC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3314215 | — | EC50 | = | 0.51 | nM | 9.29 |
| CHEMBL3314212 | — | EC50 | = | 0.59 | nM | 9.23 |
| CHEMBL3314221 | — | EC50 | = | 0.63 | nM | 9.20 |
| CHEMBL3314222 | — | EC50 | = | 0.64 | nM | 9.19 |
| CHEMBL3314218 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3314228 | — | EC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3314225 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3314226 | — | EC50 | = | 0.82 | nM | 9.09 |
| CHEMBL3314207 | — | EC50 | = | 0.87 | nM | 9.06 |
| CHEMBL3314229 | — | EC50 | = | 0.94 | nM | 9.03 |
| CHEMBL376756 | KISSPEPTIN-10 | EC50 | = | 0.96 | nM | 9.02 |
| CHEMBL3314216 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3314213 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3314219 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3314211 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3314208 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3314209 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3086284 | KISS1-305 | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3314214 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3314210 | — | EC50 | = | 4.4 | nM | 8.36 |