Basic Information
ID: ALA3706272
Type: Binding
Description: Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
Format: BAO_0000219
Organism: Homo sapiens
Target: Metabotropic glutamate receptor 5(ALA3227)
Document: ALA3638809
BindingDB Source: 6523
Activity Charts
Bioactivity
Activity Types for Assay ALA3706272
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 368.39 | 3.38 | 3.38 |
| 350.40 | 2.92 | 2.92 |
| 381.41 | 2.13 | 2.13 |
| 432.43 | 3.18 | 3.18 |
| 415.52 | 3.88 | 3.88 |
| 385.43 | 3.10 | 3.10 |
| 385.45 | 2.67 | 2.67 |
| 370.42 | 2.33 | 2.33 |
| 445.45 | 1.99 | 1.99 |
| 400.44 | 2.80 | 2.80 |
| 414.47 | 3.20 | 3.20 |
| 404.51 | 3.72 | 3.72 |
| 350.42 | 2.18 | 2.18 |
| 334.38 | 2.08 | 2.08 |
| 374.44 | 3.04 | 3.04 |
| 388.47 | 3.28 | 3.28 |
| 376.46 | 3.15 | 3.15 |
| 385.43 | 3.10 | 3.10 |
| 359.43 | 2.72 | 2.72 |
| 349.39 | 1.85 | 1.85 |
| 386.38 | 3.47 | 3.47 |
| 395.47 | 3.51 | 3.51 |
| 388.47 | 3.43 | 3.43 |
| 362.43 | 1.98 | 1.98 |
| 376.42 | 2.23 | 2.23 |
| 414.44 | 3.04 | 3.04 |
| 414.44 | 3.04 | 3.04 |
| 385.43 | 2.03 | 2.03 |
| 432.43 | 3.18 | 3.18 |
| 414.44 | 3.04 | 3.04 |
| 348.40 | 2.93 | 2.93 |
| 350.42 | 2.36 | 2.36 |
| 410.48 | 3.21 | 3.21 |
| 414.44 | 3.04 | 3.04 |
| 362.43 | 2.59 | 2.59 |
| 362.43 | 2.50 | 2.50 |
| 416.40 | 3.48 | 3.48 |
| 409.49 | 3.82 | 3.82 |
| 328.82 | 3.63 | 3.63 |
| 349.39 | 2.33 | 2.33 |
| 362.38 | 4.00 | 4.00 |
| 324.40 | 2.99 | 2.99 |
| 322.36 | 2.83 | 2.83 |
| 349.39 | 2.33 | 2.33 |
| 322.37 | 1.66 | 1.66 |
| 392.46 | 2.95 | 2.95 |
| 382.85 | 3.59 | 3.59 |
| 348.40 | 2.93 | 2.93 |
| 362.43 | 3.24 | 3.24 |
| 312.37 | 3.12 | 3.12 |
| 397.27 | 3.69 | 3.69 |
| 404.47 | 2.16 | 2.16 |
| 377.44 | 2.65 | 2.65 |
| 377.45 | 1.49 | 1.49 |
| 355.40 | 3.57 | 3.57 |
| 373.28 | 3.74 | 3.74 |
| 444.27 | 3.53 | 3.53 |
| 445.26 | 2.92 | 2.92 |
| 404.21 | 3.11 | 3.11 |
| 418.24 | 2.25 | 2.25 |
| 403.48 | 2.76 | 2.76 |
| 322.37 | 1.14 | 1.14 |
| 322.37 | 1.14 | 1.14 |
| 360.41 | 3.13 | 3.13 |
| 394.47 | 4.59 | 4.59 |
| 396.45 | 3.38 | 3.38 |
| 397.44 | 2.78 | 2.78 |
| 326.79 | 2.53 | 2.53 |
| 434.24 | 1.67 | 1.67 |
| 432.26 | 2.79 | 2.79 |
| 476.27 | 2.35 | 2.35 |
| 388.43 | 2.11 | 2.11 |
| 400.49 | 3.09 | 3.09 |
| 400.49 | 3.09 | 3.09 |
| 373.42 | 2.79 | 2.79 |
| 419.51 | 2.88 | 2.88 |
| 387.42 | 3.08 | 3.08 |
| 375.46 | 3.00 | 3.00 |
| 400.46 | 3.94 | 3.94 |
| 399.45 | 3.41 | 3.41 |
| 401.50 | 3.57 | 3.57 |
| 396.45 | 2.90 | 2.90 |
| 402.48 | 2.97 | 2.97 |
| 419.51 | 3.23 | 3.23 |
| 413.46 | 3.65 | 3.65 |
| 348.45 | 3.25 | 3.25 |
| 336.44 | 2.67 | 2.67 |
| 376.46 | 2.98 | 2.98 |
| 347.42 | 2.54 | 2.54 |
| 363.42 | 1.99 | 1.99 |
| 413.46 | 3.65 | 3.65 |
| 427.48 | 4.04 | 4.04 |
| 431.45 | 3.79 | 3.79 |
| 425.49 | 3.52 | 3.52 |
| 384.44 | 2.84 | 2.84 |
| 414.44 | 3.04 | 3.04 |
| 413.46 | 3.65 | 3.65 |
| 428.47 | 3.43 | 3.43 |
| 380.42 | 2.73 | 2.73 |
| 394.45 | 3.29 | 3.29 |