Assay Detail
Binding
CHEMBL4606596
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Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay
6
Total Activities
6
Compounds Tested
2
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 | 4 | 8.15 | 9.47 |
| pKi | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.47 |
| CHEMBL4597218 | — | — | 1 | 9.27 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.36 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | 4.0 | 1 | 6.50 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | - |
| CHEMBL4595327 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.3388 | nM | 9.47 |
| CHEMBL4597218 | — | Ki | = | 0.537 | nM | 9.27 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL129198 | JNJ-7777120 | pKi | - | — | - | |
| CHEMBL4595327 | — | pKi | - | — | - |