Assay Detail
Functional
CHEMBL908865
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against CRTH2 receptor measured as inhibition of PGD2-induced beta-arrestin translocation in HEK293 cells by BRET assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.11 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384979 | — | — | 1 | 7.92 |
| CHEMBL218561 | — | — | 1 | 7.89 |
| CHEMBL217393 | — | — | 1 | 7.77 |
| CHEMBL217053 | — | — | 1 | 7.62 |
| CHEMBL385472 | — | — | 1 | 7.51 |
| CHEMBL216367 | — | — | 1 | 7.28 |
| CHEMBL214668 | — | — | 1 | 6.83 |
| CHEMBL412381 | — | — | 1 | 6.73 |
| CHEMBL217420 | — | — | 1 | 6.63 |
| CHEMBL386348 | — | — | 1 | 6.37 |
| CHEMBL217591 | — | — | 1 | 6.36 |
| CHEMBL217624 | — | — | 1 | 6.35 |
| CHEMBL385009 | — | — | 1 | 6.32 |
| CHEMBL216907 | — | — | 1 | 6.31 |
| CHEMBL385624 | — | — | 1 | 6.23 |
| CHEMBL217167 | — | — | 1 | 6.19 |
| CHEMBL217352 | — | — | 1 | 5.88 |
| CHEMBL386370 | — | — | 1 | 5.58 |
| CHEMBL216366 | — | — | 1 | 5.52 |
| CHEMBL216189 | — | — | 1 | 5.49 |
| CHEMBL386358 | — | — | 1 | 5.46 |
| CHEMBL386606 | — | — | 1 | 5.38 |
| CHEMBL384130 | — | — | 1 | 5.34 |
| CHEMBL213657 | — | — | 1 | 5.27 |
| CHEMBL217709 | — | — | 1 | 5.20 |
| CHEMBL214655 | — | — | 1 | 5.16 |
| CHEMBL384289 | — | — | 1 | 4.30 |
| CHEMBL216175 | — | — | 1 | 4.22 |
| CHEMBL216122 | — | — | 1 | 4.09 |
| CHEMBL217287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384979 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL218561 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL217393 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL217053 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL385472 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL216367 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL214668 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL412381 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL217420 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL386348 | — | IC50 | = | 423.0 | nM | 6.37 |
| CHEMBL217591 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL217624 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL385009 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL216907 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL385624 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL217167 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL217352 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL386370 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL216366 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL216189 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL386358 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL386606 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL384130 | — | IC50 | = | 4520.0 | nM | 5.34 |
| CHEMBL213657 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL217709 | — | IC50 | = | 6320.0 | nM | 5.20 |
| CHEMBL214655 | — | IC50 | = | 6870.0 | nM | 5.16 |
| CHEMBL384289 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL216175 | — | IC50 | = | 60200.0 | nM | 4.22 |
| CHEMBL216122 | — | IC50 | = | 81700.0 | nM | 4.09 |
| CHEMBL217287 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL214620 | — | IC50 | > | 100000.0 | nM | - |