Assay Detail
Binding
CHEMBL5151497
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]diprenorphine from human mu-opioid receptor stably expressed in HEK293T cell membrane incubated for 2 hrs by scintillation counting analysis
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Abolishing Dopamine D<sub>2long</sub>/D<sub>3</sub> Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H<sub>2</sub> Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 5.41 | 5.99 |
| Kd | 4 | 10.05 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4860528 | — | — | 2 | 10.05 |
| CHEMBL5207281 | — | — | 2 | 10.05 |
| CHEMBL5206565 | — | — | 2 | 10.05 |
| CHEMBL5201074 | — | — | 2 | 10.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4860528 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL5207281 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL5206565 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL5201074 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL4860528 | — | EC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL5207281 | — | EC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL5206565 | — | EC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL5201074 | — | EC50 | = | 17378.01 | nM | 4.76 |