Assay Detail
Binding
CHEMBL751847
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Inhibition of [3H]-nicotinic acid (20 nM) binding to nicotinic acid receptor in rat spleen membrane.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Spleen |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Hydroxycarboxylic acid receptor 2 (CHEMBL4731) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Pyrazole derivatives as partial agonists for the nicotinic acid receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 5.70 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573 | NIACIN | 4.0 | 1 | 7.48 |
| CHEMBL428730 | — | — | 1 | 7.14 |
| CHEMBL237788 | — | — | 1 | 6.84 |
| CHEMBL128604 | — | — | 1 | 6.81 |
| CHEMBL394441 | — | — | 1 | 6.30 |
| CHEMBL128679 | — | — | 1 | 6.23 |
| CHEMBL238002 | — | — | 1 | 6.17 |
| CHEMBL247317 | — | — | 1 | 5.90 |
| CHEMBL129385 | — | — | 1 | 5.80 |
| CHEMBL338405 | — | — | 1 | 5.45 |
| CHEMBL341520 | — | — | 1 | 5.44 |
| CHEMBL129326 | — | — | 1 | 5.20 |
| CHEMBL128949 | — | — | 1 | 4.69 |
| CHEMBL128077 | — | — | 1 | 4.67 |
| CHEMBL341154 | — | — | 1 | 4.42 |
| CHEMBL338017 | — | — | 1 | 4.20 |
| CHEMBL127387 | — | — | 1 | 4.18 |
| CHEMBL397785 | — | — | 1 | - |
| CHEMBL338071 | — | — | 1 | - |
| CHEMBL129261 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573 | NIACIN | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL428730 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL237788 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL128604 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL394441 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL128679 | — | Ki | = | 594.0 | nM | 6.23 |
| CHEMBL238002 | — | Ki | = | 683.0 | nM | 6.17 |
| CHEMBL247317 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL129385 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL338405 | — | Ki | = | 3540.0 | nM | 5.45 |
| CHEMBL341520 | — | Ki | = | 3610.0 | nM | 5.44 |
| CHEMBL129326 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL128949 | — | Ki | = | 20300.0 | nM | 4.69 |
| CHEMBL128077 | — | Ki | = | 21400.0 | nM | 4.67 |
| CHEMBL341154 | — | Ki | = | 37900.0 | nM | 4.42 |
| CHEMBL338017 | — | Ki | = | 63700.0 | nM | 4.20 |
| CHEMBL127387 | — | Ki | = | 66000.0 | nM | 4.18 |
| CHEMBL397785 | — | Ki | = | 101000.0 | nM | - |
| CHEMBL338071 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL129261 | — | Ki | = | 107000.0 | nM | - |