Assay Detail
Functional
CHEMBL1918596
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Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| 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 |
|---|---|---|---|
| IC50 | 19 | 5.46 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1914576 | — | — | 1 | 7.22 |
| CHEMBL1914588 | — | — | 1 | 6.96 |
| CHEMBL1914590 | — | — | 1 | 6.24 |
| CHEMBL1914589 | — | — | 1 | 5.98 |
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 5.91 |
| CHEMBL1914585 | — | — | 1 | 5.83 |
| CHEMBL1914591 | — | — | 1 | 5.73 |
| CHEMBL1914578 | — | — | 1 | 5.71 |
| CHEMBL1914577 | — | — | 1 | 5.35 |
| CHEMBL1914586 | — | — | 1 | 5.33 |
| CHEMBL1914592 | — | — | 1 | 5.23 |
| CHEMBL1914587 | — | — | 1 | 5.22 |
| CHEMBL1914581 | — | — | 1 | 5.19 |
| CHEMBL1914580 | — | — | 1 | 4.99 |
| CHEMBL1914584 | — | — | 1 | 4.92 |
| CHEMBL1914582 | — | — | 1 | 4.79 |
| CHEMBL1914579 | — | — | 1 | 4.67 |
| CHEMBL1914583 | — | — | 1 | 4.31 |
| CHEMBL1173787 | — | — | 1 | 4.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1914576 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1914588 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1914590 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL1914589 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL1914585 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL1914591 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL1914578 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL1914577 | — | IC50 | = | 4480.0 | nM | 5.35 |
| CHEMBL1914586 | — | IC50 | = | 4690.0 | nM | 5.33 |
| CHEMBL1914592 | — | IC50 | = | 5920.0 | nM | 5.23 |
| CHEMBL1914587 | — | IC50 | = | 6070.0 | nM | 5.22 |
| CHEMBL1914581 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1914580 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL1914584 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL1914582 | — | IC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL1914579 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL1914583 | — | IC50 | = | 48900.0 | nM | 4.31 |
| CHEMBL1173787 | — | IC50 | = | 57000.0 | nM | 4.24 |