Assay Detail
Binding
CHEMBL1646946
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Displacement of radioligand from human CRTH2 expressed in HEK293 cells by competitive binding assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Azaindoles as potent CRTH2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.85 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1641809 | — | — | 1 | 8.74 |
| CHEMBL1641810 | — | — | 1 | 8.72 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.60 |
| CHEMBL1641808 | — | — | 1 | 8.48 |
| CHEMBL1641811 | — | — | 1 | 8.47 |
| CHEMBL1641816 | — | — | 1 | 8.47 |
| CHEMBL1641814 | — | — | 1 | 8.44 |
| CHEMBL1641817 | — | — | 1 | 8.41 |
| CHEMBL1641813 | — | — | 1 | 8.33 |
| CHEMBL1641815 | — | — | 1 | 8.29 |
| CHEMBL1641818 | — | — | 1 | 7.94 |
| CHEMBL1641812 | — | — | 1 | 7.68 |
| CHEMBL1641807 | — | — | 1 | 6.86 |
| CHEMBL1641806 | — | — | 1 | 5.17 |
| CHEMBL557117 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1641809 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1641810 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL561132 | MK-7246 | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1641808 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL1641811 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1641816 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1641814 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1641817 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1641813 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL1641815 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL1641818 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL1641812 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL1641807 | — | Ki | = | 139.0 | nM | 6.86 |
| CHEMBL1641806 | — | Ki | = | 6725.0 | nM | 5.17 |
| CHEMBL557117 | — | Ki | = | 7189.0 | nM | 5.14 |