Assay Detail
Functional
CHEMBL2039371
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Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
15
Total Activities
15
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 Natural Phenols as G Protein-Coupled Receptor-35 (GPR35) Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 4.85 | 5.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6246 | ELLAGIC ACID | 2.0 | 1 | 5.53 |
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 5.50 |
| CHEMBL1360563 | HEMATEIN | — | 1 | 5.33 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 5.23 |
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 5.21 |
| CHEMBL28626 | MORIN | — | 1 | 4.95 |
| CHEMBL559337 | 7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID | — | 1 | 4.91 |
| CHEMBL164 | MYRICETIN | — | 1 | 4.83 |
| CHEMBL1914588 | — | — | 1 | 4.75 |
| CHEMBL551842 | LOBARIC ACID | — | 1 | 4.75 |
| CHEMBL8260 | BAICALEIN | 2.0 | 1 | 4.64 |
| CHEMBL63323 | NIFLUMIC ACID | 2.0 | 1 | 4.40 |
| CHEMBL15193 | LAPACHOL | — | 1 | 4.32 |
| CHEMBL2037378 | LACCACID ACID A | — | 1 | 4.29 |
| CHEMBL76602 | alpha-CYANO-4-HYDROXYCINNAMIC ACID | — | 1 | 4.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6246 | ELLAGIC ACID | EC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL151 | LUTEOLIN | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1360563 | HEMATEIN | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL50 | QUERCETIN | EC50 | = | 5930.0 | nM | 5.23 |
| CHEMBL28079 | ZAPRINAST | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL28626 | MORIN | EC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL559337 | 7-DESHYDROXYPYROGALLIN-4-CARBOXYLIC ACID | EC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL164 | MYRICETIN | EC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL1914588 | — | EC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL551842 | LOBARIC ACID | EC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL8260 | BAICALEIN | EC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL63323 | NIFLUMIC ACID | EC50 | = | 40200.0 | nM | 4.40 |
| CHEMBL15193 | LAPACHOL | EC50 | = | 47900.0 | nM | 4.32 |
| CHEMBL2037378 | LACCACID ACID A | EC50 | = | 51500.0 | nM | 4.29 |
| CHEMBL76602 | alpha-CYANO-4-HYDROXYCINNAMIC ACID | EC50 | = | 70700.0 | nM | 4.15 |