Assay Detail
Functional
CHEMBL3405600
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Antagonist activity at human S1P2 receptor overexpressed in CHO cells assessed as increase in intracellular calcium ion concentration incubated 3 mins prior to S1P challenge by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.46 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3401382 | — | — | 1 | 7.68 |
| CHEMBL3401386 | — | — | 1 | 7.57 |
| CHEMBL3401383 | — | — | 1 | 7.41 |
| CHEMBL3401387 | — | — | 1 | 7.37 |
| CHEMBL3401381 | — | — | 1 | 7.24 |
| CHEMBL3401380 | — | — | 1 | 7.08 |
| CHEMBL3401385 | — | — | 1 | 7.06 |
| CHEMBL3401388 | — | — | 1 | 7.03 |
| CHEMBL3401384 | — | — | 1 | 6.82 |
| CHEMBL3401389 | — | — | 1 | 6.68 |
| CHEMBL3401390 | — | — | 1 | 6.58 |
| CHEMBL3401376 | — | — | 1 | 6.30 |
| CHEMBL3401373 | — | — | 1 | 6.09 |
| CHEMBL3401377 | — | — | 1 | 6.07 |
| CHEMBL3401379 | — | — | 1 | 6.01 |
| CHEMBL3401375 | — | — | 1 | 5.92 |
| CHEMBL3400193 | — | — | 1 | 5.92 |
| CHEMBL3400191 | — | — | 1 | 5.92 |
| CHEMBL3400192 | — | — | 1 | 5.89 |
| CHEMBL3401378 | — | — | 1 | 5.85 |
| CHEMBL3401374 | — | — | 1 | 5.82 |
| CHEMBL3400190 | — | — | 1 | 5.66 |
| CHEMBL3400194 | — | — | 1 | 4.68 |
| CHEMBL3400195 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3401382 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3401386 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3401383 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3401387 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3401381 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3401380 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3401385 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3401388 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3401384 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3401389 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3401390 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3401376 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3401373 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3401377 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3401379 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3401375 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3400193 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3400191 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3400192 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3401378 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3401374 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3400190 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3400194 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3400195 | — | IC50 | > | 25000.0 | nM | - |