Assay Detail
Functional
CHEMBL3755810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting
5
Total Activities
5
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
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.62 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.10 |
| CHEMBL494093 | — | — | 1 | 6.53 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 6.38 |
| CHEMBL3752085 | — | — | 1 | 6.04 |
| CHEMBL3752270 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL494093 | — | EC50 | = | 295.12 | nM | 6.53 |
| CHEMBL260374 | THIOPERAMIDE | EC50 | = | 416.87 | nM | 6.38 |
| CHEMBL3752085 | — | EC50 | = | 912.01 | nM | 6.04 |
| CHEMBL3752270 | — | EC50 | = | 933.25 | nM | 6.03 |