Assay Detail
Functional
CHEMBL4337406
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Agonist activity at rat H4R expressed in HEK293-SF-rH4R-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 | Rattus norvegicus |
| 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 | 8.49 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454158 | — | — | 1 | 10.30 |
| CHEMBL4443126 | — | — | 1 | 9.21 |
| CHEMBL4439142 | — | — | 1 | 9.19 |
| CHEMBL4543119 | — | — | 1 | 8.93 |
| CHEMBL4445423 | — | — | 1 | 8.86 |
| CHEMBL4455324 | — | — | 1 | 8.75 |
| CHEMBL4437371 | — | — | 1 | 7.64 |
| CHEMBL4518374 | — | — | 1 | 7.03 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454158 | — | EC50 | = | 0.05012 | nM | 10.30 |
| CHEMBL4443126 | — | EC50 | = | 0.6166 | nM | 9.21 |
| CHEMBL4439142 | — | EC50 | = | 0.6457 | nM | 9.19 |
| CHEMBL4543119 | — | EC50 | = | 1.175 | nM | 8.93 |
| CHEMBL4445423 | — | EC50 | = | 1.38 | nM | 8.86 |
| CHEMBL4455324 | — | EC50 | = | 1.778 | nM | 8.75 |
| CHEMBL4437371 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL4518374 | — | EC50 | = | 93.33 | nM | 7.03 |
| CHEMBL90 | HISTAMINE | EC50 | = | 295.12 | nM | 6.53 |