Assay Detail
Functional
CHEMBL1102912
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Antagonist activity at human CRTH2 receptor expressed in HEK385-7 cells assessed as inhibition of PGD2-mediated beta-arrestin translocation preincubated 5 mins prior to PGD2 challenge measured after 5 mins by BRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK385-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.67 | 10.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088284 | — | — | 1 | 10.92 |
| CHEMBL1081033 | — | — | 1 | 10.14 |
| CHEMBL1087029 | — | — | 1 | 10.10 |
| CHEMBL1087622 | — | — | 1 | 10.07 |
| CHEMBL1080695 | — | — | 1 | 10.01 |
| CHEMBL1086856 | — | — | 1 | 9.70 |
| CHEMBL1087030 | — | — | 1 | 9.62 |
| CHEMBL1087031 | — | — | 1 | 9.59 |
| CHEMBL1087500 | — | — | 1 | 9.34 |
| CHEMBL1088727 | — | — | 1 | 9.00 |
| CHEMBL1087501 | — | — | 1 | 8.82 |
| CHEMBL1076716 | — | — | 1 | 8.70 |
| CHEMBL1086857 | — | — | 1 | - |
| CHEMBL1088285 | — | — | 1 | - |
| CHEMBL1080393 | — | — | 1 | - |
| CHEMBL1080560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088284 | — | IC50 | = | 0.012 | nM | 10.92 |
| CHEMBL1081033 | — | IC50 | = | 0.072 | nM | 10.14 |
| CHEMBL1087029 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL1087622 | — | IC50 | = | 0.085 | nM | 10.07 |
| CHEMBL1080695 | — | IC50 | = | 0.098 | nM | 10.01 |
| CHEMBL1086856 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1087030 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL1087031 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL1087500 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL1088727 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1087501 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1076716 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1086857 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL1088285 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL1080393 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL1080560 | — | IC50 | > | 100.0 | nM | - |