Assay Detail
Binding
CHEMBL1925206
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Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
20
Total Activities
20
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 | 20 | 8.05 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.30 |
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 9.20 |
| CHEMBL1923026 | — | — | 1 | 8.99 |
| CHEMBL43934 | — | — | 1 | 8.98 |
| CHEMBL1923034 | — | — | 1 | 8.94 |
| CHEMBL19439 | IMETIT | — | 1 | 8.80 |
| CHEMBL1923033 | — | — | 1 | 8.79 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 8.55 |
| CHEMBL1923032 | — | — | 1 | 8.33 |
| CHEMBL1923027 | — | — | 1 | 8.31 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.20 |
| CHEMBL1923024 | — | — | 1 | 8.01 |
| CHEMBL1923028 | — | — | 1 | 7.77 |
| CHEMBL1923030 | — | — | 1 | 7.73 |
| CHEMBL1923029 | — | — | 1 | 7.49 |
| CHEMBL1923023 | — | — | 1 | 7.37 |
| CHEMBL1923025 | — | — | 1 | 7.33 |
| CHEMBL1923031 | — | — | 1 | 7.17 |
| CHEMBL1196470 | — | — | 1 | 6.50 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL19010 | IODOPROXYFAN | Ki | = | 0.631 | nM | 9.20 |
| CHEMBL1923026 | — | Ki | = | 1.023 | nM | 8.99 |
| CHEMBL43934 | — | Ki | = | 1.047 | nM | 8.98 |
| CHEMBL1923034 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL19439 | IMETIT | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1923033 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL1923032 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL1923027 | — | Ki | = | 4.898 | nM | 8.31 |
| CHEMBL90 | HISTAMINE | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1923024 | — | Ki | = | 9.772 | nM | 8.01 |
| CHEMBL1923028 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL1923030 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL1923029 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL1923023 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL1923025 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL1923031 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL1196470 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 5011.87 | nM | 5.30 |