Assay Detail
Functional
CHEMBL2166532
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 8.01 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165642 | — | — | 1 | 8.75 |
| CHEMBL2165628 | — | — | 1 | 8.54 |
| CHEMBL2165641 | — | — | 1 | 8.38 |
| CHEMBL2165644 | — | — | 1 | 6.35 |
| CHEMBL2165643 | — | — | 1 | - |
| CHEMBL2165640 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165642 | — | EC50 | = | 1.778 | nM | 8.75 |
| CHEMBL2165628 | — | EC50 | = | 2.884 | nM | 8.54 |
| CHEMBL2165641 | — | EC50 | = | 4.169 | nM | 8.38 |
| CHEMBL2165644 | — | EC50 | = | 446.68 | nM | 6.35 |
| CHEMBL2165643 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL2165640 | — | EC50 | > | 10000.0 | nM | - |