Assay Detail
Functional
CHEMBL4178741
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Antagonist activity at human GPR4 expressed in human HeLa cells assessed as inhibition of IBMX-induced cAMP accumulation after 15 mins by HTRF assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.27 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3639746 | — | — | 1 | 7.70 |
| CHEMBL4217603 | — | — | 1 | 7.68 |
| CHEMBL4208267 | — | — | 1 | 7.62 |
| CHEMBL4210921 | — | — | 1 | 7.57 |
| CHEMBL4209248 | — | — | 1 | 7.37 |
| CHEMBL4213196 | — | — | 1 | 7.30 |
| CHEMBL4212656 | — | — | 1 | 7.28 |
| CHEMBL4211343 | — | — | 1 | 7.20 |
| CHEMBL3675743 | — | — | 1 | 7.16 |
| CHEMBL4207309 | — | — | 1 | 7.14 |
| CHEMBL4205308 | — | — | 1 | 7.13 |
| CHEMBL3675746 | — | — | 1 | 6.94 |
| CHEMBL4204864 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3639746 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4217603 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4208267 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4210921 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4209248 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4213196 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4212656 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4211343 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3675743 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4207309 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4205308 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3675746 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4204864 | — | IC50 | = | 368.0 | nM | 6.43 |