Assay Detail
Functional
CHEMBL3137174
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPR17 receptor transfected in 1321N1 astrocytoma cells assessed as induction of intracellular calcium mobilization by fluorimetric assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Uracil nucleotide/cysteinyl leukotriene receptor (CHEMBL1075162) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Improved synthesis of 4-/6-substituted 2-carboxy-1H-indole-3-propionic acid derivatives and structureactivity relationships as GPR17 agonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 5.35 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3132880 | — | — | 1 | 6.70 |
| CHEMBL31344 | — | — | 1 | 6.48 |
| CHEMBL3132887 | — | — | 1 | 6.15 |
| CHEMBL3132885 | — | — | 1 | 5.65 |
| CHEMBL3132881 | — | — | 1 | 5.32 |
| CHEMBL3132882 | — | — | 1 | 4.77 |
| CHEMBL3132886 | — | — | 1 | 4.43 |
| CHEMBL3132884 | — | — | 1 | 4.34 |
| CHEMBL3132883 | — | — | 1 | 4.28 |
| CHEMBL50976 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3132880 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL31344 | — | EC50 | = | 331.0 | nM | 6.48 |
| CHEMBL3132887 | — | EC50 | = | 715.0 | nM | 6.15 |
| CHEMBL3132885 | — | EC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL3132881 | — | EC50 | = | 4790.0 | nM | 5.32 |
| CHEMBL3132882 | — | EC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL3132886 | — | EC50 | = | 36800.0 | nM | 4.43 |
| CHEMBL3132884 | — | EC50 | = | 45500.0 | nM | 4.34 |
| CHEMBL3132883 | — | EC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL50976 | — | EC50 | > | 100000.0 | nM | - |