Assay Detail
Binding
CHEMBL2444575
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Displacement of [3H]-prostaglandin D2 from human CRTh2 receptor expressed in CHO cells after 2 hrs
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 19 | 6.56 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL563949 | — | — | 1 | 7.51 |
| CHEMBL2442750 | QAV680 | 2.0 | 1 | 7.44 |
| CHEMBL561539 | — | — | 1 | 6.99 |
| CHEMBL2442743 | — | — | 1 | 6.96 |
| CHEMBL2442742 | — | — | 1 | 6.84 |
| CHEMBL2442736 | — | — | 1 | 6.83 |
| CHEMBL2442751 | — | — | 1 | 6.83 |
| CHEMBL2442752 | — | — | 1 | 6.68 |
| CHEMBL2442748 | — | — | 1 | 6.60 |
| CHEMBL2442737 | — | — | 1 | 6.57 |
| CHEMBL2442744 | — | — | 1 | 6.56 |
| CHEMBL2442741 | — | — | 1 | 6.52 |
| CHEMBL2442749 | — | — | 1 | 6.42 |
| CHEMBL2442740 | — | — | 1 | 6.30 |
| CHEMBL2442739 | — | — | 1 | 6.23 |
| CHEMBL2442738 | — | — | 1 | 6.21 |
| CHEMBL2442745 | — | — | 1 | 5.97 |
| CHEMBL2442746 | — | — | 1 | 5.65 |
| CHEMBL2442747 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL563949 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2442750 | QAV680 | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL561539 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL2442743 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL2442742 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL2442736 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL2442751 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL2442752 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL2442748 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL2442737 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2442744 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL2442741 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL2442749 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL2442740 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL2442739 | — | Ki | = | 588.0 | nM | 6.23 |
| CHEMBL2442738 | — | Ki | = | 624.0 | nM | 6.21 |
| CHEMBL2442745 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL2442746 | — | Ki | = | 2230.0 | nM | 5.65 |
| CHEMBL2442747 | — | Ki | = | 2940.0 | nM | 5.53 |