Assay Detail
Functional
CHEMBL1638837
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Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay
7
Total Activities
7
Compounds Tested
2
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
Histamine H4 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.18 | 6.70 |
| pKb | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 6.70 |
| CHEMBL26116 | — | — | 1 | 6.70 |
| CHEMBL24665 | — | — | 1 | 6.60 |
| CHEMBL12620 | 2-METHYLHISTAMINE | — | 1 | 6.10 |
| CHEMBL293762 | AMTHAMINE | — | 1 | 4.80 |
| CHEMBL483406 | — | — | 1 | - |
| CHEMBL471413 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL26116 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL24665 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL12620 | 2-METHYLHISTAMINE | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL293762 | AMTHAMINE | EC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL483406 | — | pKb | = | 4.8 | — | - |
| CHEMBL471413 | — | pKb | = | 5.5 | — | - |