Assay Detail
Functional
CHEMBL3860802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at rat KISS1R expressed in CHO/dhfr cells assessed as increase in intracellular Ca2+ levels measured for 180 secs by Fluo 3-AM dye based FLIPR assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO/dhfr |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 7.96 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3949159 | — | — | 1 | 8.92 |
| CHEMBL3314224 | — | — | 1 | 8.89 |
| CHEMBL3928465 | — | — | 1 | 8.74 |
| CHEMBL3921327 | — | — | 1 | 8.55 |
| CHEMBL376756 | KISSPEPTIN-10 | 3.0 | 1 | 8.38 |
| CHEMBL3957784 | — | — | 1 | 8.33 |
| CHEMBL3985112 | — | — | 1 | 8.32 |
| CHEMBL3930297 | — | — | 1 | 8.32 |
| CHEMBL3915251 | — | — | 1 | 8.22 |
| CHEMBL3956437 | — | — | 1 | 8.17 |
| CHEMBL3964403 | — | — | 1 | 8.15 |
| CHEMBL3949224 | — | — | 1 | 8.15 |
| CHEMBL3968824 | — | — | 1 | 8.15 |
| CHEMBL3977235 | — | — | 1 | 8.14 |
| CHEMBL3939287 | — | — | 1 | 8.13 |
| CHEMBL3967782 | — | — | 1 | 8.07 |
| CHEMBL3911692 | — | — | 1 | 8.03 |
| CHEMBL3985323 | — | — | 1 | 7.96 |
| CHEMBL3958495 | — | — | 1 | 7.96 |
| CHEMBL3976038 | — | — | 1 | 7.92 |
| CHEMBL3931718 | — | — | 1 | 7.82 |
| CHEMBL3967058 | — | — | 1 | 7.80 |
| CHEMBL3904889 | — | — | 1 | 7.80 |
| CHEMBL3894943 | — | — | 1 | 7.77 |
| CHEMBL3964945 | — | — | 1 | 7.77 |
| CHEMBL3914238 | — | — | 1 | 7.75 |
| CHEMBL3956626 | — | — | 1 | 7.70 |
| CHEMBL3977314 | — | — | 1 | 7.70 |
| CHEMBL3956072 | — | — | 1 | 7.64 |
| CHEMBL3924151 | TAK-448 | 2.0 | 1 | 7.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3949159 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3314224 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3928465 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3921327 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL376756 | KISSPEPTIN-10 | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3957784 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3985112 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3930297 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3915251 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3956437 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3964403 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3949224 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3968824 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3977235 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3939287 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL3967782 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3911692 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL3958495 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3985323 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3976038 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3931718 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3967058 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3904889 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3894943 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3964945 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3914238 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3977314 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3956626 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3956072 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3924151 | TAK-448 | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3984058 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3947975 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3982675 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3896533 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3938759 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3966187 | — | EC50 | = | 110.0 | nM | 6.96 |