Assay Detail
Functional
CHEMBL866223
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.85 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379125 | — | — | 1 | 9.28 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 8.85 |
| CHEMBL212370 | — | — | 1 | 8.74 |
| CHEMBL212631 | — | — | 1 | 8.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379125 | — | EC50 | = | 0.52 | nM | 9.28 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL212370 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL212631 | — | EC50 | = | 3.0 | nM | 8.52 |