Assay Detail
Functional
CHEMBL1918600
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Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcriptional activation after 5 hrs by tango beta-arrestin translocation reporter assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 4.96 | 5.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 5.38 |
| CHEMBL1914576 | — | — | 1 | 4.99 |
| CHEMBL1914588 | — | — | 1 | 4.82 |
| CHEMBL1914590 | — | — | 1 | 4.64 |
| CHEMBL1914592 | — | — | 1 | - |
| CHEMBL1914591 | — | — | 1 | - |
| CHEMBL1914589 | — | — | 1 | - |
| CHEMBL1914587 | — | — | 1 | - |
| CHEMBL1914586 | — | — | 1 | - |
| CHEMBL1914585 | — | — | 1 | - |
| CHEMBL1173787 | — | — | 1 | - |
| CHEMBL1914593 | — | — | 1 | - |
| CHEMBL1914583 | — | — | 1 | - |
| CHEMBL1914582 | — | — | 1 | - |
| CHEMBL1914581 | — | — | 1 | - |
| CHEMBL1914580 | — | — | 1 | - |
| CHEMBL1914579 | — | — | 1 | - |
| CHEMBL1914578 | — | — | 1 | - |
| CHEMBL1914577 | — | — | 1 | - |
| CHEMBL1914584 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28079 | ZAPRINAST | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1914576 | — | EC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL1914588 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1914590 | — | EC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL1914592 | — | EC50 | - | — | - | |
| CHEMBL1914591 | — | EC50 | - | — | - | |
| CHEMBL1914589 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL1914587 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL1914586 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL1914585 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL1173787 | — | EC50 | - | — | - | |
| CHEMBL1914593 | — | EC50 | - | — | - | |
| CHEMBL1914583 | — | EC50 | - | — | - | |
| CHEMBL1914582 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL1914581 | — | EC50 | - | — | - | |
| CHEMBL1914580 | — | EC50 | - | — | - | |
| CHEMBL1914579 | — | EC50 | - | — | - | |
| CHEMBL1914578 | — | EC50 | > | 50000.0 | nM | - |
| CHEMBL1914577 | — | EC50 | - | — | - | |
| CHEMBL1914584 | — | EC50 | > | 50000.0 | nM | - |