Assay Detail
Binding
CHEMBL2379695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells by competitive kinetic analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: comparison of hERG binding and target residence time with PF-3893787.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 7.86 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.40 |
| CHEMBL2376800 | — | — | 1 | 8.07 |
| CHEMBL2376803 | — | — | 1 | 7.99 |
| CHEMBL2376804 | — | — | 1 | 7.87 |
| CHEMBL2376801 | — | — | 1 | 7.67 |
| CHEMBL1915540 | ADRIFORANT | 2.0 | 1 | 7.60 |
| CHEMBL1935574 | — | — | 1 | 7.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL2376800 | — | Kd | = | 8.511 | nM | 8.07 |
| CHEMBL2376803 | — | Kd | = | 10.23 | nM | 7.99 |
| CHEMBL2376804 | — | Kd | = | 13.49 | nM | 7.87 |
| CHEMBL2376801 | — | Kd | = | 21.38 | nM | 7.67 |
| CHEMBL1915540 | ADRIFORANT | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL1935574 | — | Kd | = | 40.74 | nM | 7.39 |