Assay Detail
Functional
CHEMBL5159686
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Antagonist activity at human GPR84 expressed in HEK293 cells co-expressing Galpha16 assessed as right shift in 3-OH-C12-induced calcium response curve by measuring agonist EC50 at 10 nM preincubated for 10 mins and measured after 1 min of agonist stimulation by schild plot analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 4.61 | 4.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3716365 | GLPG-1205 | 2.0 | 1 | 4.66 |
| CHEMBL5179395 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3716365 | GLPG-1205 | EC50 | = | 22100.0 | nM | 4.66 |
| CHEMBL5179395 | — | EC50 | = | 28430.0 | nM | 4.55 |