Assay Detail
Binding
CHEMBL971506
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Displacement of [3H]nicotinic acid from human GPR109a receptor
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.12 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL520137 | — | — | 2 | 7.40 |
| CHEMBL507182 | — | — | 1 | 7.16 |
| CHEMBL509541 | — | — | 2 | 7.10 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 6.85 |
| CHEMBL519966 | — | — | 1 | 6.85 |
| CHEMBL520676 | — | — | 1 | 6.85 |
| CHEMBL502716 | — | — | 1 | 6.54 |
| CHEMBL504980 | — | — | 1 | 6.39 |
| CHEMBL520675 | — | — | 1 | 6.37 |
| CHEMBL519811 | — | — | 1 | 6.21 |
| CHEMBL500239 | — | — | 1 | 6.16 |
| CHEMBL483142 | — | — | 1 | 6.12 |
| CHEMBL484172 | — | — | 1 | 6.06 |
| CHEMBL456145 | — | — | 1 | 5.82 |
| CHEMBL447050 | — | — | 1 | 5.72 |
| CHEMBL483141 | — | — | 1 | 5.62 |
| CHEMBL520159 | — | — | 1 | 5.60 |
| CHEMBL482943 | — | — | 1 | 5.57 |
| CHEMBL519338 | — | — | 1 | 5.34 |
| CHEMBL482979 | — | — | 1 | 5.32 |
| CHEMBL485195 | — | — | 1 | 5.30 |
| CHEMBL501585 | — | — | 1 | 5.28 |
| CHEMBL485194 | — | — | 1 | 5.11 |
| CHEMBL519689 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL520137 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL507182 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL509541 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL520137 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL573 | NIACIN | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL519966 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL520676 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL502716 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL509541 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL504980 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL520675 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL519811 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL500239 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL483142 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL484172 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL456145 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL447050 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL483141 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL520159 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL482943 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL519338 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL482979 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL485195 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL501585 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL485194 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL519689 | — | IC50 | = | 16000.0 | nM | 4.80 |