Assay Detail
Binding
CHEMBL1925207
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Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
21
Total Activities
21
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
Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.33 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19439 | IMETIT | — | 1 | 8.20 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 8.00 |
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 7.90 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.80 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.80 |
| CHEMBL1923025 | — | — | 1 | 7.79 |
| CHEMBL18661 | IMMEPIP | — | 1 | 7.70 |
| CHEMBL1923031 | — | — | 1 | 7.53 |
| CHEMBL1196470 | — | — | 1 | 7.50 |
| CHEMBL1923030 | — | — | 1 | 7.50 |
| CHEMBL1923023 | — | — | 1 | 7.37 |
| CHEMBL43934 | — | — | 1 | 7.32 |
| CHEMBL1923024 | — | — | 1 | 7.12 |
| CHEMBL1923027 | — | — | 1 | 7.05 |
| CHEMBL1923032 | — | — | 1 | 7.05 |
| CHEMBL1923033 | — | — | 1 | 6.90 |
| CHEMBL1923034 | — | — | 1 | 6.87 |
| CHEMBL1923026 | — | — | 1 | 6.83 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 6.70 |
| CHEMBL1923028 | — | — | 1 | 6.64 |
| CHEMBL1923029 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19439 | IMETIT | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL19010 | IODOPROXYFAN | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL90 | HISTAMINE | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1923025 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL18661 | IMMEPIP | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1923031 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL1196470 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1923030 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1923023 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL43934 | — | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL1923024 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL1923027 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL1923032 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL1923033 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1923034 | — | Ki | = | 134.9 | nM | 6.87 |
| CHEMBL1923026 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL42 | CLOZAPINE | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1923028 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL1923029 | — | Ki | = | 380.19 | nM | 6.42 |