Assay Detail
Binding
CHEMBL4000101
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Antagonist activity at DP2 receptor in human whole assessed as inhibition of DK-PGD2-induced eosinophils shape change preincubated for 5 mins followed by DK-PGD2 addition measured after 5 mins by flow cytometry
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.74 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137332 | FEVIPIPRANT | 3.0 | 1 | 9.40 |
| CHEMBL3932668 | — | — | 1 | 8.40 |
| CHEMBL3931906 | — | — | 1 | 8.15 |
| CHEMBL3983909 | — | — | 1 | 7.96 |
| CHEMBL2442750 | QAV680 | 2.0 | 1 | 7.51 |
| CHEMBL3975922 | — | — | 1 | 7.50 |
| CHEMBL3981414 | — | — | 1 | 7.33 |
| CHEMBL4094939 | — | — | 1 | 6.73 |
| CHEMBL3912535 | — | — | 1 | 6.67 |
| CHEMBL3922383 | — | — | 1 | - |
| CHEMBL4073398 | — | — | 1 | - |
| CHEMBL4086277 | — | — | 1 | - |
| CHEMBL4064804 | — | — | 1 | - |
| CHEMBL4078419 | — | — | 1 | - |
| CHEMBL4102679 | — | — | 1 | - |
| CHEMBL4067518 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137332 | FEVIPIPRANT | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3932668 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3931906 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3983909 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2442750 | QAV680 | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3975922 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3981414 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4094939 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL3912535 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL3922383 | — | IC50 | - | — | - | |
| CHEMBL4073398 | — | IC50 | - | — | - | |
| CHEMBL4086277 | — | IC50 | - | — | - | |
| CHEMBL4064804 | — | IC50 | - | — | - | |
| CHEMBL4078419 | — | IC50 | - | — | - | |
| CHEMBL4102679 | — | IC50 | - | — | - | |
| CHEMBL4067518 | — | IC50 | - | — | - |