Assay Detail
Functional
CHEMBL4154378
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR109a expressed in HTLA cells assessed as increase in beta-arrestin2 recruitment after overnight incubation by Tango assay
17
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.14 | 6.63 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4174798 | — | — | 3 | 6.63 |
| CHEMBL4163051 | — | — | 3 | 6.56 |
| CHEMBL4159670 | — | — | 3 | 6.34 |
| CHEMBL4167588 | — | — | 3 | 6.00 |
| CHEMBL4164140 | — | — | 3 | 5.77 |
| CHEMBL573 | NIACIN | 4.0 | 2 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4174798 | — | EC50 | = | 232.0 | nM | 6.63 |
| CHEMBL4174798 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL4163051 | — | EC50 | = | 275.42 | nM | 6.56 |
| CHEMBL4163051 | — | EC50 | = | 276.0 | nM | 6.56 |
| CHEMBL4159670 | — | EC50 | = | 457.09 | nM | 6.34 |
| CHEMBL4159670 | — | EC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4167588 | — | EC50 | = | 1005.0 | nM | 6.00 |
| CHEMBL4167588 | — | EC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL4164140 | — | EC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL4164140 | — | EC50 | = | 1686.0 | nM | 5.77 |
| CHEMBL573 | NIACIN | EC50 | = | 2727.0 | nM | 5.56 |
| CHEMBL573 | NIACIN | EC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL4174798 | — | Activity | - | — | - | |
| CHEMBL4164140 | — | Activity | - | — | - | |
| CHEMBL4159670 | — | Activity | - | — | - | |
| CHEMBL4167588 | — | Activity | - | — | - | |
| CHEMBL4163051 | — | Activity | - | — | - |