Basic Information
ID: ALA3706294
Type: Binding
Description: Radioligand Binding Assay: The relative affinity of the various compounds for the human 5-HT3 receptor was measured in a radioligand binding assay, using a scintillation proximity assay (SPA) format. Test compounds were dissolved to 10 mM in 100% DMSO, then serially diluted at 10x assay concentrations in 100% DMSO in 96-well polypropylene plates and further diluted to 4x assay concentrations with the assay buffer. Samples were incubated in 50 mM Tris-HCl, pH 7.5, 3 mM MgCl2, 1 mM EDTA and 10% DMSO with 10 nM [9-methyl-3H]BRL-43694 (Perkin Elmer), 3 ug of human 5-HT3 receptor membranes (Perkin Elmer) and 0.5 mg/mL SPA beads (WGA PVT, Amersham Biosciences) in a final volume of 0.2 mL. Binding reactions were set up in wells of PicoPlates-96 (Perkin Elmer) by adding consecutively 50 uL of each competing compound or buffer, SPA beads, the radioligand and 5-HT3 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3706294
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 294.36 | 2.41 | 2.41 |
| 279.34 | 2.89 | 2.89 |
| 295.39 | 2.19 | 2.19 |
| 295.39 | 2.19 | 2.19 |
| 343.86 | 3.15 | 3.15 |
| 296.37 | 1.59 | 1.59 |
| 330.82 | 2.24 | 2.24 |
| 312.37 | 0.88 | 0.88 |
| 348.43 | 0.71 | 0.71 |
| 309.41 | 2.50 | 2.50 |
| 309.41 | 2.58 | 2.58 |
| 309.41 | 2.58 | 2.58 |
| 314.36 | 1.73 | 1.73 |
| 326.40 | 1.08 | 1.08 |
| 310.40 | 1.89 | 1.89 |
| 312.37 | 1.29 | 1.29 |
| 296.37 | 1.59 | 1.59 |
| 324.43 | 2.15 | 2.15 |
| 372.47 | 3.25 | 3.25 |
| 406.92 | 3.91 | 3.91 |
| 429.56 | 3.67 | 3.67 |
| 309.41 | 2.65 | 2.65 |
| 296.37 | 2.00 | 2.00 |
| 296.37 | 1.86 | 1.86 |
| 310.40 | 1.98 | 1.98 |
| 310.40 | 1.90 | 1.90 |