Assay Detail
Binding
CHEMBL1105988
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 in presence of 4% human serum albumin
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 | 6.17 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573 | NIACIN | 4.0 | 1 | 6.98 |
| CHEMBL237248 | — | — | 1 | 6.92 |
| CHEMBL1087302 | — | — | 1 | 6.82 |
| CHEMBL1086656 | — | — | 2 | 6.64 |
| CHEMBL1086657 | — | — | 1 | 6.22 |
| CHEMBL1088213 | — | — | 1 | 6.18 |
| CHEMBL1084657 | — | — | 1 | 6.08 |
| CHEMBL1088074 | — | — | 1 | 5.97 |
| CHEMBL1084393 | — | — | 1 | 5.96 |
| CHEMBL1086658 | — | — | 1 | 5.04 |
| CHEMBL1084394 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573 | NIACIN | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL237248 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1087302 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL1086656 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL1086656 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL1086657 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL1088213 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL1084657 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL1088074 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL1084393 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1086658 | — | Ki | = | 9130.0 | nM | 5.04 |
| CHEMBL1084394 | — | Ki | = | 24700.0 | nM | 4.61 |