Assay Detail
Functional
CHEMBL2169534
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Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.87 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL908 | CHLORPROTHIXENE | 4.0 | 2 | 9.00 |
| CHEMBL511 | PYRILAMINE | 4.0 | 1 | 7.33 |
| CHEMBL564 | PROMAZINE | 4.0 | 1 | 5.61 |
| CHEMBL86715 | PROCYCLIDINE | 4.0 | 1 | 4.75 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 4.35 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 1 | 4.01 |
| CHEMBL597 | PHENTOLAMINE | 4.0 | 1 | - |
| CHEMBL596 | FENTANYL | 4.0 | 1 | - |
| CHEMBL353846 | ADIPHENINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL908 | CHLORPROTHIXENE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 46.77 | nM | 7.33 |
| CHEMBL908 | CHLORPROTHIXENE | IC50 | = | 870.96 | nM | 6.06 |
| CHEMBL564 | PROMAZINE | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL86715 | PROCYCLIDINE | IC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL122270 | LOBELINE | IC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL900 | ORPHENADRINE | IC50 | = | 97723.72 | nM | 4.01 |
| CHEMBL597 | PHENTOLAMINE | IC50 | = | 316227.77 | nM | - |
| CHEMBL596 | FENTANYL | IC50 | = | 147910.84 | nM | - |
| CHEMBL353846 | ADIPHENINE | IC50 | = | 112201.85 | nM | - |