Assay Detail
Binding
CHEMBL856874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human DP receptor expressed in HEK293 cells
8
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.63 | 9.24 |
| Kd | 1 | 10.52 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL426559 | LAROPIPRANT | 4.0 | 2 | 10.52 |
| CHEMBL385126 | — | — | 1 | 8.96 |
| CHEMBL426387 | — | — | 1 | 8.82 |
| CHEMBL207203 | — | — | 1 | 8.74 |
| CHEMBL383484 | — | — | 1 | 8.59 |
| CHEMBL221007 | DIASTEREOMER 2 | — | 1 | 8.05 |
| CHEMBL387477 | — | — | 1 | 8.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL426559 | LAROPIPRANT | Kd | = | 0.03 | nM | 10.52 |
| CHEMBL426559 | LAROPIPRANT | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL385126 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL426387 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL207203 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL383484 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL221007 | DIASTEREOMER 2 | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL387477 | — | Ki | = | 9.6 | nM | 8.02 |