Assay Detail
Functional
CHEMBL960690
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Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay
6
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 4 | - | - |
| IC50 | 2 | 7.00 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452847 | — | — | 2 | 7.16 |
| CHEMBL454890 | — | — | 2 | 6.84 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | - |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452847 | — | IC50 | = | 69.18 | nM | 7.16 |
| CHEMBL454890 | — | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL454890 | — | Activity | - | — | - | |
| CHEMBL452847 | — | Activity | - | — | - | |
| CHEMBL260374 | THIOPERAMIDE | Activity | - | — | - | |
| CHEMBL90 | HISTAMINE | Activity | - | — | - |