Assay Detail
Functional
CHEMBL971522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.73 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483139 | — | — | 1 | 8.19 |
| CHEMBL485196 | — | — | 1 | 7.72 |
| CHEMBL483140 | — | — | 1 | 7.62 |
| CHEMBL483352 | — | — | 1 | 7.47 |
| CHEMBL521326 | — | — | 1 | 7.40 |
| CHEMBL483336 | — | — | 1 | 7.37 |
| CHEMBL483337 | — | — | 1 | 7.32 |
| CHEMBL483353 | — | — | 1 | 7.30 |
| CHEMBL520299 | — | — | 1 | 7.29 |
| CHEMBL482768 | — | — | 1 | 7.19 |
| CHEMBL520136 | — | — | 1 | 7.13 |
| CHEMBL520513 | — | — | 1 | 7.12 |
| CHEMBL485326 | — | — | 1 | 6.96 |
| CHEMBL484783 | — | — | 1 | 6.92 |
| CHEMBL482963 | — | — | 1 | 6.77 |
| CHEMBL485185 | — | — | 1 | 6.57 |
| CHEMBL522649 | — | — | 1 | 6.47 |
| CHEMBL235740 | — | — | 1 | 6.30 |
| CHEMBL235741 | — | — | 1 | 6.23 |
| CHEMBL485327 | — | — | 1 | 6.21 |
| CHEMBL520620 | — | — | 1 | 6.16 |
| CHEMBL483160 | — | — | 1 | 6.08 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 6.00 |
| CHEMBL483153 | — | — | 1 | 6.00 |
| CHEMBL485184 | — | — | 1 | 5.58 |
| CHEMBL228244 | — | — | 1 | 5.22 |
| CHEMBL483996 | — | — | 1 | 5.14 |
| CHEMBL482980 | — | — | 1 | - |
| CHEMBL484605 | — | — | 1 | - |
| CHEMBL484604 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483139 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL485196 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL483140 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL483352 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL521326 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL483336 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL483337 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL483353 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL520299 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL482768 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL520136 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL520513 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL485326 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL484783 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL482963 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL485185 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL522649 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL235740 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL235741 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL485327 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL520620 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL483160 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL573 | NIACIN | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL483153 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL485184 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL228244 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL483996 | — | EC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL482980 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL484605 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL484604 | — | EC50 | - | — | - |