Assay Detail
Binding
CHEMBL4606598
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Inhibition of UR-DEBa242 binding to mouse 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 | Mus musculus |
| 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 | 7.35 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4597218 | — | — | 1 | 8.91 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.93 |
| CHEMBL4595327 | — | — | 1 | 7.51 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.18 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 6.91 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | 4.0 | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4597218 | — | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL4595327 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 123.03 | nM | 6.91 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | Ki | = | 2137.96 | nM | 5.67 |