Assay Detail
Functional
CHEMBL4154377
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR109a expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
17
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 9 | 7.72 | 7.97 |
| Inhibition | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4164140 | — | — | 3 | 7.97 |
| CHEMBL573 | NIACIN | 4.0 | 2 | 7.68 |
| CHEMBL4174798 | — | — | 3 | 7.52 |
| CHEMBL4163670 | — | — | 1 | - |
| CHEMBL4170912 | — | — | 1 | - |
| CHEMBL4160302 | — | — | 1 | - |
| CHEMBL4167537 | — | — | 1 | - |
| CHEMBL4175406 | — | — | 1 | - |
| CHEMBL4170967 | — | — | 1 | - |
| CHEMBL4163051 | — | — | 1 | - |
| CHEMBL4167588 | — | — | 1 | - |
| CHEMBL4159670 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4164140 | — | EC50 | = | 10.6 | nM | 7.97 |
| CHEMBL4164140 | — | EC50 | = | 10.59 | nM | 7.97 |
| CHEMBL573 | NIACIN | EC50 | = | 20.75 | nM | 7.68 |
| CHEMBL573 | NIACIN | EC50 | = | 20.7 | nM | 7.68 |
| CHEMBL4174798 | — | EC50 | = | 30.48 | nM | 7.52 |
| CHEMBL4174798 | — | EC50 | = | 30.5 | nM | 7.52 |
| CHEMBL4164140 | — | Inhibition | - | % | - | |
| CHEMBL4174798 | — | Inhibition | - | % | - | |
| CHEMBL4163670 | — | Inhibition | - | % | - | |
| CHEMBL4159670 | — | EC50 | >= | 10000.0 | nM | - |
| CHEMBL4167588 | — | EC50 | >= | 10000.0 | nM | - |
| CHEMBL4163051 | — | EC50 | >= | 10000.0 | nM | - |
| CHEMBL4170967 | — | Inhibition | - | % | - | |
| CHEMBL4175406 | — | Inhibition | - | % | - | |
| CHEMBL4167537 | — | Inhibition | - | % | - | |
| CHEMBL4160302 | — | Inhibition | - | % | - | |
| CHEMBL4170912 | — | Inhibition | - | % | - |