Assay Detail
Functional
CHEMBL4332252
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Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay
28
Total Activities
28
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
A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 9.54 | 10.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4539775 | — | — | 1 | 10.66 |
| CHEMBL4533110 | — | — | 1 | 10.62 |
| CHEMBL4462883 | — | — | 1 | 10.55 |
| CHEMBL4528114 | — | — | 1 | 10.43 |
| CHEMBL4451244 | — | — | 1 | 10.24 |
| CHEMBL3085809 | — | — | 1 | 10.24 |
| CHEMBL4541289 | — | — | 1 | 10.17 |
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 10.06 |
| CHEMBL4473151 | — | — | 1 | 9.96 |
| CHEMBL4584512 | — | — | 1 | 9.92 |
| CHEMBL4563528 | — | — | 1 | 9.89 |
| CHEMBL4459547 | — | — | 1 | 9.89 |
| CHEMBL4536531 | — | — | 1 | 9.80 |
| CHEMBL4439387 | — | — | 1 | 9.77 |
| CHEMBL4470916 | — | — | 1 | 9.64 |
| CHEMBL4538305 | — | — | 1 | 9.62 |
| CHEMBL4468499 | — | — | 1 | 9.57 |
| CHEMBL3086284 | KISS1-305 | — | 1 | 9.57 |
| CHEMBL4557192 | — | — | 1 | 9.48 |
| CHEMBL4476438 | — | — | 1 | 9.22 |
| CHEMBL4463349 | — | — | 1 | 9.21 |
| CHEMBL4446920 | — | — | 1 | 9.05 |
| CHEMBL4472672 | — | — | 1 | 8.85 |
| CHEMBL4518378 | — | — | 1 | 8.82 |
| CHEMBL4549804 | — | — | 1 | 8.68 |
| CHEMBL4470482 | — | — | 1 | 8.11 |
| CHEMBL4562955 | — | — | 1 | 8.09 |
| CHEMBL4535825 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4539775 | — | EC50 | = | 0.022 | nM | 10.66 |
| CHEMBL4533110 | — | EC50 | = | 0.024 | nM | 10.62 |
| CHEMBL4462883 | — | EC50 | = | 0.028 | nM | 10.55 |
| CHEMBL4528114 | — | EC50 | = | 0.037 | nM | 10.43 |
| CHEMBL4451244 | — | EC50 | = | 0.058 | nM | 10.24 |
| CHEMBL3085809 | — | EC50 | = | 0.057 | nM | 10.24 |
| CHEMBL4541289 | — | EC50 | = | 0.068 | nM | 10.17 |
| CHEMBL376756 | KISSPEPTIN-10 | EC50 | = | 0.087 | nM | 10.06 |
| CHEMBL4473151 | — | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4584512 | — | EC50 | = | 0.12 | nM | 9.92 |
| CHEMBL4563528 | — | EC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4459547 | — | EC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4536531 | — | EC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4439387 | — | EC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4470916 | — | EC50 | = | 0.23 | nM | 9.64 |
| CHEMBL4538305 | — | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4468499 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3086284 | KISS1-305 | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL4557192 | — | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4476438 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4463349 | — | EC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4446920 | — | EC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4472672 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4518378 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4549804 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4470482 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4562955 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4535825 | — | EC50 | = | 130.0 | nM | 6.89 |