Assay Detail
Functional
CHEMBL3386099
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 9.48 | 10.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3358545 | — | — | 1 | 10.38 |
| CHEMBL3358549 | — | — | 1 | 10.35 |
| CHEMBL3358541 | — | — | 1 | 10.29 |
| CHEMBL3358552 | — | — | 1 | 10.15 |
| CHEMBL3358539 | — | — | 1 | 10.07 |
| CHEMBL3358540 | — | — | 1 | 9.89 |
| CHEMBL3358546 | — | — | 1 | 9.89 |
| CHEMBL3358535 | — | — | 1 | 9.89 |
| CHEMBL3358551 | — | — | 1 | 9.82 |
| CHEMBL3358550 | — | — | 1 | 9.82 |
| CHEMBL3358536 | — | — | 1 | 9.74 |
| CHEMBL430239 | MELATONAN | — | 1 | 9.72 |
| CHEMBL3352878 | — | — | 1 | 9.64 |
| CHEMBL3358544 | — | — | 1 | 9.47 |
| CHEMBL3358547 | — | — | 1 | 8.75 |
| CHEMBL3358548 | — | — | 1 | 8.73 |
| CHEMBL3358537 | — | — | 1 | 8.72 |
| CHEMBL3358543 | — | — | 1 | 8.71 |
| CHEMBL3358533 | — | — | 1 | 8.49 |
| CHEMBL3358538 | — | — | 1 | 8.30 |
| CHEMBL3358534 | — | — | 1 | 8.27 |
| CHEMBL441738 | AFAMELANOTIDE | 4.0 | 1 | - |
| CHEMBL2372859 | — | — | 1 | - |
| CHEMBL3358542 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3358545 | — | EC50 | = | 0.042 | nM | 10.38 |
| CHEMBL3358549 | — | EC50 | = | 0.045 | nM | 10.35 |
| CHEMBL3358541 | — | EC50 | = | 0.051 | nM | 10.29 |
| CHEMBL3358552 | — | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3358539 | — | EC50 | = | 0.086 | nM | 10.07 |
| CHEMBL3358540 | — | EC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3358546 | — | EC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3358535 | — | EC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3358551 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3358550 | — | EC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3358536 | — | EC50 | = | 0.18 | nM | 9.74 |
| CHEMBL430239 | MELATONAN | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL3352878 | — | EC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3358544 | — | EC50 | = | 0.34 | nM | 9.47 |
| CHEMBL3358547 | — | EC50 | = | 1.76 | nM | 8.75 |
| CHEMBL3358548 | — | EC50 | = | 1.88 | nM | 8.73 |
| CHEMBL3358537 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3358543 | — | EC50 | = | 1.93 | nM | 8.71 |
| CHEMBL3358533 | — | EC50 | = | 3.22 | nM | 8.49 |
| CHEMBL3358538 | — | EC50 | = | 5.04 | nM | 8.30 |
| CHEMBL3358534 | — | EC50 | = | 5.33 | nM | 8.27 |
| CHEMBL441738 | AFAMELANOTIDE | EC50 | - | — | - | |
| CHEMBL2372859 | — | EC50 | - | — | - | |
| CHEMBL3358542 | — | EC50 | - | — | - |