Assay Detail
Functional
CHEMBL4834975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR35 receptor expressed in HT-29 cells assessed as desensitization of zaprinast-induced DMR response preincubated for 1 hr followed by zaprinast stimulation by DMR desensitization assay
35
Total Activities
35
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
Structure-Activity Relationship Studies of Coumarin-like Diacid Derivatives as Human G Protein-Coupled Receptor-35 (hGPR35) Agonists and a Consequent New Design Principle.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.12 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3306990 | — | — | 1 | 8.70 |
| CHEMBL4870213 | — | — | 1 | 8.70 |
| CHEMBL4859764 | — | — | 1 | 8.52 |
| CHEMBL4869539 | — | — | 1 | 8.22 |
| CHEMBL4861414 | — | — | 1 | 8.22 |
| CHEMBL4856506 | — | — | 1 | 8.15 |
| CHEMBL4848109 | — | — | 1 | 8.10 |
| CHEMBL4857772 | — | — | 1 | 8.00 |
| CHEMBL4865638 | — | — | 1 | 7.82 |
| CHEMBL4876009 | — | — | 1 | 7.82 |
| CHEMBL4850743 | — | — | 1 | 7.82 |
| CHEMBL4856069 | — | — | 1 | 7.80 |
| CHEMBL4856029 | — | — | 1 | 7.75 |
| CHEMBL4865971 | — | — | 1 | 7.70 |
| CHEMBL4878979 | — | — | 1 | 7.66 |
| CHEMBL4848949 | — | — | 1 | 7.58 |
| CHEMBL4847100 | — | — | 1 | 7.58 |
| CHEMBL4875009 | — | — | 1 | 7.57 |
| CHEMBL4871203 | — | — | 1 | 7.57 |
| CHEMBL1235421 | PYRROLOQUINOLINE QUINONE | — | 1 | 7.52 |
| CHEMBL4862654 | — | — | 1 | 7.38 |
| CHEMBL4852667 | — | — | 1 | 7.19 |
| CHEMBL4870255 | — | — | 1 | 6.60 |
| CHEMBL4879017 | — | — | 1 | 6.52 |
| CHEMBL4860550 | — | — | 1 | 6.14 |
| CHEMBL4859675 | — | — | 1 | 5.99 |
| CHEMBL4856916 | — | — | 1 | 5.96 |
| CHEMBL4875771 | — | — | 1 | 5.88 |
| CHEMBL4878047 | — | — | 1 | 5.86 |
| CHEMBL4847144 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3306990 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4870213 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4859764 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4869539 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4861414 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4856506 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4848109 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4857772 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4865638 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4876009 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4850743 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4856069 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4856029 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4865971 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4878979 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4848949 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4847100 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4875009 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4871203 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1235421 | PYRROLOQUINOLINE QUINONE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4862654 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4852667 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4870255 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4879017 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4860550 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4859675 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4856916 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL4875771 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4878047 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL4847144 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4853043 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4875041 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL4077503 | — | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL4872368 | — | IC50 | = | 5410.0 | nM | 5.27 |
| CHEMBL4854346 | — | IC50 | = | 17580.0 | nM | 4.75 |