Assay Detail
Binding
CHEMBL1105987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NA from cloned human GPR109A receptor expressed in CHO-K1 cells by spectrophotometry
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.85 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1084657 | — | — | 1 | 8.85 |
| CHEMBL1087302 | — | — | 1 | 8.52 |
| CHEMBL237248 | — | — | 1 | 8.40 |
| CHEMBL1086656 | — | — | 2 | 8.40 |
| CHEMBL1086657 | — | — | 1 | 8.40 |
| CHEMBL1086658 | — | — | 1 | 7.96 |
| CHEMBL1088213 | — | — | 1 | 7.66 |
| CHEMBL1084393 | — | — | 1 | 7.54 |
| CHEMBL573 | NIACIN | 4.0 | 1 | 7.09 |
| CHEMBL1084394 | — | — | 1 | 6.89 |
| CHEMBL1088074 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1084657 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1087302 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL237248 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1086656 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1086657 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1086656 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1086658 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1088213 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1084393 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL573 | NIACIN | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL1084394 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL1088074 | — | Ki | = | 360.0 | nM | 6.44 |