Assay Detail
Functional
CHEMBL2444574
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Antagonist activity at human CRTh2 receptor expressed in CHO cells assessed as inhibition of prostaglandin D2 and forskolin-induced cAMP accumulation after 45 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.72 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2442750 | QAV680 | 2.0 | 1 | 7.43 |
| CHEMBL563949 | — | — | 1 | 7.22 |
| CHEMBL2442751 | — | — | 1 | 6.84 |
| CHEMBL2442752 | — | — | 1 | 6.83 |
| CHEMBL2442748 | — | — | 1 | 6.63 |
| CHEMBL2442736 | — | — | 1 | 6.32 |
| CHEMBL2442749 | — | — | 1 | 6.26 |
| CHEMBL561539 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2442750 | QAV680 | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL563949 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2442751 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL2442752 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL2442748 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL2442736 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL2442749 | — | IC50 | = | 554.0 | nM | 6.26 |
| CHEMBL561539 | — | IC50 | = | 565.0 | nM | 6.25 |