Assay Detail
Functional
CHEMBL4337398
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Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
[<sup>3</sup>H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H<sub>4</sub> Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.28 | 9.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454158 | — | — | 1 | 9.91 |
| CHEMBL4443126 | — | — | 1 | 9.22 |
| CHEMBL4439142 | — | — | 1 | 8.72 |
| CHEMBL4455324 | — | — | 1 | 8.45 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.77 |
| CHEMBL4518374 | — | — | 1 | 7.74 |
| CHEMBL4543119 | — | — | 1 | 7.71 |
| CHEMBL4437371 | — | — | 1 | 7.53 |
| CHEMBL4445423 | — | — | 1 | 7.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454158 | — | EC50 | = | 0.123 | nM | 9.91 |
| CHEMBL4443126 | — | EC50 | = | 0.6026 | nM | 9.22 |
| CHEMBL4439142 | — | EC50 | = | 1.905 | nM | 8.72 |
| CHEMBL4455324 | — | EC50 | = | 3.548 | nM | 8.45 |
| CHEMBL90 | HISTAMINE | EC50 | = | 16.98 | nM | 7.77 |
| CHEMBL4518374 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL4543119 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4437371 | — | EC50 | = | 29.51 | nM | 7.53 |
| CHEMBL4445423 | — | EC50 | = | 35.48 | nM | 7.45 |