Assay Detail
Binding
CHEMBL937683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.84 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502339 | — | — | 1 | 8.20 |
| CHEMBL471413 | — | — | 1 | 8.07 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.94 |
| CHEMBL483406 | — | — | 1 | 7.82 |
| CHEMBL472441 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502339 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL471413 | — | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL90 | HISTAMINE | EC50 | = | 11.6 | nM | 7.94 |
| CHEMBL483406 | — | EC50 | = | 15.3 | nM | 7.82 |
| CHEMBL472441 | — | EC50 | = | 66.3 | nM | 7.18 |