Assay Detail
Binding
CHEMBL1781769
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Binding affinity to human CRTH2 receptor expressed in HEK293-EBNA cells by radioligand competition binding assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293-EBNA |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
New indole amide derivatives as potent CRTH2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.39 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1778388 | — | — | 1 | 8.77 |
| CHEMBL1778524 | — | — | 1 | 8.74 |
| CHEMBL1778523 | — | — | 1 | 8.70 |
| CHEMBL561132 | MK-7246 | 1.0 | 1 | 8.60 |
| CHEMBL1778522 | — | — | 1 | 8.52 |
| CHEMBL1778387 | — | — | 1 | 8.40 |
| CHEMBL1778525 | — | — | 1 | 8.37 |
| CHEMBL1778506 | — | — | 1 | 8.13 |
| CHEMBL1778518 | — | — | 1 | 7.85 |
| CHEMBL1778505 | — | — | 1 | 7.82 |
| CHEMBL1778516 | — | — | 1 | 7.72 |
| CHEMBL1778514 | — | — | 1 | 7.66 |
| CHEMBL1778517 | — | — | 1 | 7.51 |
| CHEMBL1778521 | — | — | 1 | 7.41 |
| CHEMBL1778513 | — | — | 1 | 7.16 |
| CHEMBL1778508 | — | — | 1 | 6.96 |
| CHEMBL1778390 | — | — | 1 | 6.92 |
| CHEMBL1778515 | — | — | 1 | 6.90 |
| CHEMBL1778512 | — | — | 1 | 6.85 |
| CHEMBL1778511 | — | — | 1 | 6.74 |
| CHEMBL1778510 | — | — | 1 | 6.62 |
| CHEMBL1778389 | — | — | 1 | 6.47 |
| CHEMBL1778504 | — | — | 1 | 6.43 |
| CHEMBL1778519 | — | — | 1 | 6.39 |
| CHEMBL1778507 | — | — | 1 | 6.17 |
| CHEMBL1778520 | — | — | 1 | 5.91 |
| CHEMBL1778509 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1778388 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1778524 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1778523 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL561132 | MK-7246 | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1778522 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1778387 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1778525 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL1778506 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL1778518 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1778505 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1778516 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1778514 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1778517 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL1778521 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1778513 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL1778508 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1778390 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1778515 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL1778512 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL1778511 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL1778510 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL1778389 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL1778504 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL1778519 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL1778507 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL1778520 | — | Ki | = | 1220.0 | nM | 5.91 |
| CHEMBL1778509 | — | Ki | = | 1700.0 | nM | 5.77 |