Assay Detail
Binding
CHEMBL853360
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Displacement of [3H]histamine from human histamine H4 receptor transfected in SK-N-MC cells
27
Total Activities
23
Compounds Tested
3
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
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 |
|---|---|---|---|
| Ki | 23 | 6.65 | 7.80 |
| Kd | 2 | 7.95 | 7.97 |
| Bmax | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL213912 | — | — | 3 | 7.97 |
| CHEMBL42 | CLOZAPINE | 4.0 | 3 | 7.92 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.80 |
| CHEMBL209758 | — | — | 1 | 7.56 |
| CHEMBL209628 | — | — | 1 | 7.51 |
| CHEMBL387054 | — | — | 1 | 7.41 |
| CHEMBL7828 | ISOLOXAPINE | — | 1 | 7.37 |
| CHEMBL211170 | — | — | 1 | 7.34 |
| CHEMBL211242 | — | — | 1 | 7.10 |
| CHEMBL339414 | — | — | 1 | 6.88 |
| CHEMBL379102 | — | — | 1 | 6.72 |
| CHEMBL1795042 | — | — | 1 | 6.54 |
| CHEMBL378788 | — | — | 1 | 6.51 |
| CHEMBL1794919 | — | — | 1 | 6.49 |
| CHEMBL377985 | — | — | 1 | 5.97 |
| CHEMBL266723 | — | — | 1 | 5.85 |
| CHEMBL67284 | ISOCLOTHIAPINE | — | 1 | 5.69 |
| CHEMBL831 | LOXAPINE | 4.0 | 1 | 5.34 |
| CHEMBL386333 | — | — | 1 | 5.33 |
| CHEMBL340801 | PERLAPINE | 2.0 | 1 | 5.32 |
| CHEMBL377765 | — | — | 1 | - |
| CHEMBL209680 | — | — | 1 | - |
| CHEMBL90882 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL213912 | — | Kd | = | 10.7 | nM | 7.97 |
| CHEMBL42 | CLOZAPINE | Kd | = | 11.9 | nM | 7.92 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL209758 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL213912 | — | Ki | = | 28.18 | nM | 7.55 |
| CHEMBL209628 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL387054 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL7828 | ISOLOXAPINE | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL211170 | — | Ki | = | 45.71 | nM | 7.34 |
| CHEMBL211242 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL339414 | — | Ki | = | 131.83 | nM | 6.88 |
| CHEMBL42 | CLOZAPINE | Ki | = | 177.83 | nM | 6.75 |
| CHEMBL379102 | — | Ki | = | 190.55 | nM | 6.72 |
| CHEMBL1795042 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL378788 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL1794919 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL377985 | — | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL266723 | — | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL67284 | ISOCLOTHIAPINE | Ki | = | 2041.74 | nM | 5.69 |
| CHEMBL831 | LOXAPINE | Ki | = | 4570.88 | nM | 5.34 |
| CHEMBL386333 | — | Ki | = | 4677.35 | nM | 5.33 |
| CHEMBL340801 | PERLAPINE | Ki | = | 4786.3 | nM | 5.32 |
| CHEMBL90882 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL377765 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL209680 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL42 | CLOZAPINE | Bmax | = | 1011.0 | fmol/mg | - |
| CHEMBL213912 | — | Bmax | = | 1034.0 | fmol/mg | - |