Assay Detail
Binding
CHEMBL4042616
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Agonist activity at TEV protease cleavage site linked GAL4-VP16-fused GPR35 in human Tango GPR35-bla U2OS cells assessed as induction of TEV protease-tagged beta-arrestin recruitment incubated for 5 hrs by beta-lactamase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.78 | 6.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100677 | — | — | 1 | 6.71 |
| CHEMBL4079816 | — | — | 1 | 6.54 |
| CHEMBL4082281 | — | — | 1 | 6.32 |
| CHEMBL4092954 | — | — | 1 | 5.81 |
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 5.45 |
| CHEMBL4081238 | — | — | 1 | 5.44 |
| CHEMBL4065291 | — | — | 1 | 5.15 |
| CHEMBL4103143 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100677 | — | EC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4079816 | — | EC50 | = | 288.0 | nM | 6.54 |
| CHEMBL4082281 | — | EC50 | = | 479.0 | nM | 6.32 |
| CHEMBL4092954 | — | EC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL28079 | ZAPRINAST | EC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL4081238 | — | EC50 | = | 3630.0 | nM | 5.44 |
| CHEMBL4065291 | — | EC50 | = | 7050.0 | nM | 5.15 |
| CHEMBL4103143 | — | EC50 | = | 14060.0 | nM | 4.85 |