Assay Detail
Binding
CHEMBL4606604
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method
4
Total Activities
4
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
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H3 and H4 Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.00 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 7.30 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | 4.0 | 1 | 7.20 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.20 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 501.19 | nM | 6.30 |