| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3268497 | B | Displacement of [9-methyl-3H]BRL-43694 from human 5-HT3A receptor after overnight incubation by scintillation proximity assay | Homo sapiens | 11 | single protein format | Scientific Literature | ||
| 2. | ALA3268498 | B | Partial agonist activity at human 5-HT3A receptor expressed in HEK293 cells assessed as change in Ca2+ level measured as intrinsic activity at 1 uM relative to 5-HT in presence of carbachol | Homo sapiens | 6 | cell-based format | Scientific Literature | ||
| 3. | ALA3268499 | B | Partial agonist activity at mouse 5-HT3A receptor expressed in HEK293 cells assessed as change in Ca2+ level measured as intrinsic activity at 1 uM relative to 5-HT in presence of carbachol | Mus musculus | 4 | cell-based format | Scientific Literature | ||
| 4. | ALA3268500 | B | Agonist activity at human 5-HT3A receptor expressed in HEK293 cells in presence of carbachol | Homo sapiens | 6 | cell-based format | Scientific Literature | ||
| 5. | ALA3268501 | B | Agonist activity at mouse 5-HT3A receptor expressed in HEK293 cells in presence of carbachol | Mus musculus | 4 | cell-based format | Scientific Literature | ||
| 6. | ALA3268502 | A | Inhibition of CYP1A2 (unknown origin) | Homo sapiens | 7 | single protein format | Scientific Literature | ||
| 7. | ALA3268503 | A | Inhibition of CYP2B6 (unknown origin) | Homo sapiens | 6 | single protein format | Scientific Literature | ||
| 8. | ALA3268874 | A | Inhibition of CYP2C9 (unknown origin) | Homo sapiens | 6 | single protein format | Scientific Literature | ||
| 9. | ALA3268875 | A | Inhibition of CYP2C19 (unknown origin) | Homo sapiens | 6 | single protein format | Scientific Literature | ||
| 10. | ALA3268876 | A | Inhibition of CYP2D6 (unknown origin) | Homo sapiens | 6 | single protein format | Scientific Literature | ||
| 11. | ALA3268877 | A | Inhibition of CYP3A4 (unknown origin) | Homo sapiens | 7 | single protein format | Scientific Literature | ||
| 12. | ALA3268878 | A | Intrinsic clearance in human liver microsomes | Homo sapiens | 8 | assay format | Scientific Literature | ||
| 13. | ALA3268879 | F | Inhibition of 5-HT induced-bradycardia in ICR mouse von Bezold-Jarisch reflex model at 3 mg/kg, po after 60 mins relative to control | Mus musculus | 1 | organism-based format | Scientific Literature | ||
| 14. | ALA3706294 | B | 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. | Homo sapiens | 26 | assay format | BindingDB Database |
The page will load shortly, Thanks for your patience!