Assay Detail
Binding
CHEMBL852182
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Binding affinity towards human histamine H4 receptor was determined by [3H]Na-methylhistamine binding to SK-N-MC cell membranes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.05 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.10 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.70 |
| CHEMBL128613 | — | — | 1 | 7.50 |
| CHEMBL186108 | — | — | 1 | 7.20 |
| CHEMBL185951 | — | — | 1 | 7.10 |
| CHEMBL186456 | — | — | 1 | 6.70 |
| CHEMBL187210 | — | — | 1 | 6.00 |
| CHEMBL185842 | — | — | 1 | 5.50 |
| CHEMBL362163 | — | — | 1 | 5.30 |
| CHEMBL365257 | — | — | 1 | 5.10 |
| CHEMBL186640 | — | — | 1 | 4.70 |
| CHEMBL185948 | — | — | 1 | 4.60 |
| CHEMBL364629 | — | — | 1 | 4.60 |
| CHEMBL185546 | — | — | 1 | 4.60 |
| CHEMBL185680 | — | — | 1 | - |
| CHEMBL363089 | — | — | 1 | - |
| CHEMBL186575 | — | — | 1 | - |
| CHEMBL187106 | — | — | 1 | - |
| CHEMBL188020 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL128613 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL186108 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL185951 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL186456 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL187210 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL185842 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL362163 | — | Ki | = | 5011.87 | nM | 5.30 |
| CHEMBL365257 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL186640 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL185948 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL364629 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL185546 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL185680 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL363089 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL186575 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL187106 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL188020 | — | Ki | < | 100000.0 | nM | - |