Assay Detail
Binding
CHEMBL953176
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Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells 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 | 6.82 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483406 | — | — | 1 | 7.17 |
| CHEMBL471413 | — | — | 1 | 7.11 |
| CHEMBL502339 | — | — | 1 | 6.96 |
| CHEMBL472441 | — | — | 1 | 6.92 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483406 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL471413 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL502339 | — | EC50 | = | 109.0 | nM | 6.96 |
| CHEMBL472441 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL90 | HISTAMINE | EC50 | = | 1200.0 | nM | 5.92 |