Basic Information
ID: ALA3706003
Type: Binding
Description: Competition Binding Assay: The rat H3 receptor was cloned and expressed in cells, and competition binding assays carried out, according to methods previously described (see Esbenshade, et al. Journal of Pharmacology and Experimental Therapeutics 2005, 313, 165-175; Esbenshade et al., Biochemical Pharmacology 2004, 68, 933-945; and Krueger, et al. Journal of Pharmacology and Experimental Therapeutics 2005, 314, 271-281). Membranes were prepared from C6 or HEK293 cells, expressing the rat histamine H3 receptor, by homogenization on ice in TE buffer (50 mM Tris-HCl buffer, pH 7.4, containing 5 mM EDTA), 1 mM benzamidine, 2 ug/ml aprotinin, 1 ug/ml leupeptin, and 1 ug/ml pepstatin. The homogenate was centrifuged at 40,000 g for 20 minutes at 4 C. This step was repeated, and the resulting pellet was resuspended in TE buffer. Aliquots were frozen at -70 C. until needed. On the day of assay, membranes were thawed and diluted with TE buffer.
Organism: Homo sapiens
Cell type: HEK293
Activity Charts
Bioactivity
Activity Types for Assay ALA3706003
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 193.25 | -0.19 | -0.19 |
| 195.27 | 0.06 | 0.06 |
| 167.22 | -0.18 | -0.18 |
| 181.24 | 0.08 | 0.08 |
| 181.24 | -0.16 | -0.16 |
| 195.27 | 0.60 | 0.60 |
| 195.27 | 0.46 | 0.46 |
| 279.34 | 1.12 | 1.12 |
| 307.40 | 2.12 | 2.12 |
| 207.28 | 0.74 | 0.74 |
| 279.34 | 1.48 | 1.48 |
| 179.23 | -0.17 | -0.17 |
| 295.39 | 1.63 | 1.63 |
| 193.25 | -0.01 | -0.01 |
| 297.41 | 2.16 | 2.16 |
| 165.20 | -0.56 | -0.56 |
| 219.29 | 0.25 | 0.25 |
| 193.25 | 0.22 | 0.22 |
| 179.23 | -0.53 | -0.53 |
| 181.24 | 0.03 | 0.03 |
| 167.22 | -0.18 | -0.18 |
| 181.24 | 0.21 | 0.21 |
| 283.38 | 2.14 | 2.14 |