Assay Detail
Functional
CHEMBL1912710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 |
|---|---|---|---|
| Kd | 12 | 7.99 | 9.07 |
| pA2 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 9.07 |
| CHEMBL1910386 | — | — | 1 | 8.42 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 8.42 |
| CHEMBL1910381 | — | — | 1 | 8.31 |
| CHEMBL1910380 | — | — | 1 | 8.14 |
| CHEMBL1910382 | — | — | 1 | 8.12 |
| CHEMBL1910384 | — | — | 1 | 8.07 |
| CHEMBL1910378 | — | — | 1 | 7.97 |
| CHEMBL657 | DIPHENHYDRAMINE | 4.0 | 1 | 7.93 |
| CHEMBL1910385 | — | — | 1 | 7.90 |
| CHEMBL1910379 | — | — | 1 | 7.69 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 5.80 |
| CHEMBL1910383 | — | — | 1 | - |
| CHEMBL382276 | — | — | 1 | - |
| CHEMBL129199 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511 | PYRILAMINE | Kd | = | 0.8511 | nM | 9.07 |
| CHEMBL1910386 | — | Kd | = | 3.802 | nM | 8.42 |
| CHEMBL296419 | ASTEMIZOLE | Kd | = | 3.802 | nM | 8.42 |
| CHEMBL1910381 | — | Kd | = | 4.898 | nM | 8.31 |
| CHEMBL1910380 | — | Kd | = | 7.244 | nM | 8.14 |
| CHEMBL1910382 | — | Kd | = | 7.586 | nM | 8.12 |
| CHEMBL1910384 | — | Kd | = | 8.511 | nM | 8.07 |
| CHEMBL1910378 | — | Kd | = | 10.72 | nM | 7.97 |
| CHEMBL657 | DIPHENHYDRAMINE | Kd | = | 11.75 | nM | 7.93 |
| CHEMBL1910385 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL1910379 | — | Kd | = | 20.42 | nM | 7.69 |
| CHEMBL129198 | JNJ-7777120 | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL1910383 | — | pA2 | - | — | - | |
| CHEMBL382276 | — | pA2 | - | — | - | |
| CHEMBL129199 | — | pA2 | - | — | - |