Assay Detail
Binding
CHEMBL4606597
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Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| 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 | 6 | 7.64 | 8.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4597218 | — | — | 1 | 8.93 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.38 |
| CHEMBL4595327 | — | — | 1 | 7.92 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 7.11 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 6.81 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | 4.0 | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4597218 | — | Ki | = | 1.175 | nM | 8.93 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL4595327 | — | Ki | = | 12.02 | nM | 7.92 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 77.62 | nM | 7.11 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | Ki | = | 218.78 | nM | 6.66 |