Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 5.7 10'-3 ug/ml | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions at 0.1 mg/ml | ChEMBL. | 18789706 |
EC50 (functional) | = 6.2 10'-3 ug/ml | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions at 0.5 mg/ml | ChEMBL. | 18789706 |
EC50 (functional) | = 8.9 10'-3 ug/ml | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions at 1.0 mg/ml | ChEMBL. | 18789706 |
Emax (functional) | = 52 % | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions at 1.0 mg/ml relative to control | ChEMBL. | 18789706 |
Emax (functional) | = 96 % | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions at 0.5 mg/ml relative to control | ChEMBL. | 18789706 |
Emax (functional) | = 100 % | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced contractions at 0.1 mg/ml relative to control | ChEMBL. | 18789706 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.