Assay Detail
Binding
CHEMBL1912890
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting
15
Total Activities
15
Compounds Tested
2
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 | 13 | 7.03 | 8.68 |
| pKi | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.68 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 8.35 |
| CHEMBL1910386 | — | — | 1 | 8.26 |
| CHEMBL1910381 | — | — | 1 | 8.15 |
| CHEMBL657 | DIPHENHYDRAMINE | 4.0 | 1 | 7.83 |
| CHEMBL1910382 | — | — | 1 | 7.00 |
| CHEMBL1910378 | — | — | 1 | 6.77 |
| CHEMBL1910385 | — | — | 1 | 6.67 |
| CHEMBL1910383 | — | — | 1 | 6.65 |
| CHEMBL1910384 | — | — | 1 | 6.34 |
| CHEMBL1910380 | — | — | 1 | 6.22 |
| CHEMBL1910379 | — | — | 1 | 6.11 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 4.33 |
| CHEMBL382276 | — | — | 1 | - |
| CHEMBL129199 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 2.089 | nM | 8.68 |
| CHEMBL511 | PYRILAMINE | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL1910386 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL1910381 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL657 | DIPHENHYDRAMINE | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL1910382 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1910378 | — | Ki | = | 169.82 | nM | 6.77 |
| CHEMBL1910385 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL1910383 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL1910384 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL1910380 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL1910379 | — | Ki | = | 776.25 | nM | 6.11 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 46773.51 | nM | 4.33 |
| CHEMBL382276 | — | pKi | - | — | - | |
| CHEMBL129199 | — | pKi | - | — | - |