Assay Detail
Binding
CHEMBL1912709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.33 | 7.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.73 |
| CHEMBL129199 | — | — | 1 | 6.86 |
| CHEMBL382276 | — | — | 1 | 6.54 |
| CHEMBL1910378 | — | — | 1 | 5.23 |
| CHEMBL1910382 | — | — | 1 | 5.17 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 5.10 |
| CHEMBL1910381 | — | — | 1 | 5.05 |
| CHEMBL1910386 | — | — | 1 | 4.98 |
| CHEMBL1910385 | — | — | 1 | 4.85 |
| CHEMBL1910379 | — | — | 1 | 4.80 |
| CHEMBL1910383 | — | — | 1 | 4.75 |
| CHEMBL1910380 | — | — | 1 | 4.65 |
| CHEMBL1910384 | — | — | 1 | 4.56 |
| CHEMBL657 | DIPHENHYDRAMINE | 4.0 | 1 | 4.37 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL129199 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL382276 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL1910378 | — | Ki | = | 5888.44 | nM | 5.23 |
| CHEMBL1910382 | — | Ki | = | 6760.83 | nM | 5.17 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL1910381 | — | Ki | = | 8912.51 | nM | 5.05 |
| CHEMBL1910386 | — | Ki | = | 10471.29 | nM | 4.98 |
| CHEMBL1910385 | — | Ki | = | 14125.38 | nM | 4.85 |
| CHEMBL1910379 | — | Ki | = | 15848.93 | nM | 4.80 |
| CHEMBL1910383 | — | Ki | = | 17782.79 | nM | 4.75 |
| CHEMBL1910380 | — | Ki | = | 22387.21 | nM | 4.65 |
| CHEMBL1910384 | — | Ki | = | 27542.29 | nM | 4.56 |
| CHEMBL657 | DIPHENHYDRAMINE | Ki | = | 42657.95 | nM | 4.37 |
| CHEMBL511 | PYRILAMINE | Ki | < | 47.0 | nM | - |