Assay Detail
Functional
CHEMBL868084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 11 | 8.08 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212370 | — | — | 1 | 8.59 |
| CHEMBL212631 | — | — | 1 | 8.35 |
| CHEMBL240773 | QUINPIROLE | 2.0 | 1 | 7.31 |
| CHEMBL378680 | — | — | 1 | - |
| CHEMBL209034 | — | — | 1 | - |
| CHEMBL378515 | — | — | 1 | - |
| CHEMBL211135 | — | — | 1 | - |
| CHEMBL211164 | — | — | 1 | - |
| CHEMBL379125 | — | — | 1 | - |
| CHEMBL211590 | — | — | 1 | - |
| CHEMBL210341 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212370 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL212631 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL240773 | QUINPIROLE | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL378680 | — | EC50 | - | — | - | |
| CHEMBL209034 | — | EC50 | - | — | - | |
| CHEMBL378515 | — | EC50 | - | — | - | |
| CHEMBL211135 | — | EC50 | - | — | - | |
| CHEMBL211164 | — | EC50 | - | — | - | |
| CHEMBL379125 | — | EC50 | - | — | - | |
| CHEMBL211590 | — | EC50 | - | — | - | |
| CHEMBL210341 | — | EC50 | - | — | - |