Assay Detail
Binding
CHEMBL4606555
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Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes
15
Total Activities
15
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 | 15 | 6.53 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4597218 | — | — | 1 | 8.30 |
| CHEMBL4595327 | — | — | 1 | 7.90 |
| CHEMBL4635634 | — | — | 1 | 7.85 |
| CHEMBL4642520 | — | — | 1 | 7.47 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | 4.0 | 1 | 7.20 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.20 |
| CHEMBL4646286 | — | — | 1 | 6.53 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 6.30 |
| CHEMBL4636487 | — | — | 1 | 6.23 |
| CHEMBL4634235 | — | — | 1 | 6.03 |
| CHEMBL4634728 | — | — | 1 | 5.85 |
| CHEMBL4633688 | — | — | 1 | 5.74 |
| CHEMBL4640263 | — | — | 1 | 5.71 |
| CHEMBL4639472 | — | — | 1 | 5.15 |
| CHEMBL4634631 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4597218 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL4595327 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL4635634 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL4642520 | — | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4646286 | — | Ki | = | 295.12 | nM | 6.53 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4636487 | — | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL4634235 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL4634728 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL4633688 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL4640263 | — | Ki | = | 1949.84 | nM | 5.71 |
| CHEMBL4639472 | — | Ki | = | 7079.46 | nM | 5.15 |
| CHEMBL4634631 | — | Ki | = | 28183.83 | nM | 4.55 |