Assay Detail
Functional
CHEMBL900198
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Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
20
Total Activities
20
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 | Intermediate |
Publication
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 6.49 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL236162 | — | — | 1 | 8.22 |
| CHEMBL237248 | — | — | 1 | 7.57 |
| CHEMBL235256 | — | — | 1 | 7.35 |
| CHEMBL235954 | — | — | 1 | 7.11 |
| CHEMBL235952 | — | — | 1 | 7.07 |
| CHEMBL236163 | — | — | 1 | 7.03 |
| CHEMBL391813 | — | — | 1 | 6.92 |
| CHEMBL237036 | — | — | 1 | 6.62 |
| CHEMBL237037 | — | — | 1 | 6.37 |
| CHEMBL235741 | — | — | 1 | 6.23 |
| CHEMBL237247 | — | — | 1 | 6.03 |
| CHEMBL391603 | — | — | 1 | 6.01 |
| CHEMBL235740 | — | — | 1 | 6.00 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 6.00 |
| CHEMBL237543 | — | — | 1 | 5.89 |
| CHEMBL428724 | — | — | 1 | 5.68 |
| CHEMBL391812 | — | — | 1 | 5.47 |
| CHEMBL228244 | — | — | 1 | 5.22 |
| CHEMBL235953 | — | — | 1 | - |
| CHEMBL236164 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL236162 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL237248 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL235256 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL235954 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL235952 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL236163 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL391813 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL237036 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL237037 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL235741 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL237247 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL391603 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL235740 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL573 | NIACIN | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL237543 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL428724 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL391812 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL228244 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL235953 | — | EC50 | > | 20000.0 | nM | - |
| CHEMBL236164 | — | EC50 | > | 20000.0 | nM | - |