Assay Detail
Binding
CHEMBL971505
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Displacement of [3H]nicotinic acid from mouse GPR109a receptor
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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 | 6.24 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL520137 | — | — | 2 | 7.40 |
| CHEMBL509541 | — | — | 2 | 7.22 |
| CHEMBL507182 | — | — | 1 | 7.16 |
| CHEMBL519966 | — | — | 1 | 7.10 |
| CHEMBL520676 | — | — | 1 | 7.05 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 6.85 |
| CHEMBL502716 | — | — | 1 | 6.85 |
| CHEMBL500239 | — | — | 1 | 6.58 |
| CHEMBL520675 | — | — | 1 | 6.51 |
| CHEMBL504980 | — | — | 1 | 6.47 |
| CHEMBL519811 | — | — | 1 | 6.28 |
| CHEMBL484172 | — | — | 1 | 6.10 |
| CHEMBL483142 | — | — | 1 | 6.07 |
| CHEMBL456145 | — | — | 1 | 5.92 |
| CHEMBL519338 | — | — | 1 | 5.89 |
| CHEMBL483141 | — | — | 1 | 5.80 |
| CHEMBL482943 | — | — | 1 | 5.77 |
| CHEMBL501585 | — | — | 1 | 5.60 |
| CHEMBL447050 | — | — | 1 | 5.51 |
| CHEMBL482979 | — | — | 1 | 5.44 |
| CHEMBL485195 | — | — | 1 | 5.40 |
| CHEMBL485194 | — | — | 1 | 5.38 |
| CHEMBL520159 | — | — | 1 | 5.05 |
| CHEMBL519689 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL520137 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL509541 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL507182 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL520137 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL519966 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL520676 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL573 | NIACIN | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL502716 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL509541 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL500239 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL520675 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL504980 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL519811 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL484172 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL483142 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL456145 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL519338 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL483141 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL482943 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL501585 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL447050 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL482979 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL485195 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL485194 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL520159 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL519689 | — | IC50 | = | 11000.0 | nM | 4.96 |