Assay Detail
Binding
CHEMBL1005955
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Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
13
Total Activities
13
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 | Autocuration |
Publication
Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.10 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19439 | IMETIT | — | 1 | 8.44 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 8.30 |
| CHEMBL498770 | IODOPHENPROPIT | — | 1 | 8.11 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 7.87 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.77 |
| CHEMBL1162351 | — | — | 1 | 7.07 |
| CHEMBL12344 | DIMAPRIT | — | 1 | 7.05 |
| CHEMBL268229 | — | — | 1 | 6.74 |
| CHEMBL1162352 | — | — | 1 | 6.66 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 6.48 |
| CHEMBL1162347 | — | — | 1 | 6.05 |
| CHEMBL1162346 | — | — | 1 | 5.91 |
| CHEMBL1162345 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19439 | IMETIT | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL498770 | IODOPHENPROPIT | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL90 | HISTAMINE | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1162351 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL12344 | DIMAPRIT | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL268229 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL1162352 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 328.0 | nM | 6.48 |
| CHEMBL1162347 | — | Ki | = | 897.0 | nM | 6.05 |
| CHEMBL1162346 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL1162345 | — | Ki | = | 1480.0 | nM | 5.83 |