Assay Detail
Functional
CHEMBL853363
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Activity at human histamine H4 receptor transfected in SK-N-MC cells by cAMP assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.30 | 7.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL211170 | — | — | 1 | 7.83 |
| CHEMBL209758 | — | — | 1 | 7.83 |
| CHEMBL213912 | — | — | 1 | 7.70 |
| CHEMBL209628 | — | — | 1 | 7.69 |
| CHEMBL7828 | ISOLOXAPINE | — | 1 | 7.55 |
| CHEMBL387054 | — | — | 1 | 7.41 |
| CHEMBL379102 | — | — | 1 | 7.09 |
| CHEMBL378788 | — | — | 1 | 6.99 |
| CHEMBL211242 | — | — | 1 | 6.98 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 6.66 |
| CHEMBL339414 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL211170 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL209758 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL213912 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL209628 | — | EC50 | = | 20.42 | nM | 7.69 |
| CHEMBL7828 | ISOLOXAPINE | EC50 | = | 28.18 | nM | 7.55 |
| CHEMBL387054 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL379102 | — | EC50 | = | 81.28 | nM | 7.09 |
| CHEMBL378788 | — | EC50 | = | 102.33 | nM | 6.99 |
| CHEMBL211242 | — | EC50 | = | 104.71 | nM | 6.98 |
| CHEMBL831 | LOXAPINE | EC50 | = | 218.78 | nM | 6.66 |
| CHEMBL339414 | — | EC50 | = | 302.0 | nM | 6.52 |