Basic Information
ID: ALA3705781
Type: Functional
Description: In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
Organism: Homo sapiens
Cell type: CHO
Activity Charts
Bioactivity
Activity Types for Assay ALA3705781
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 425.88 | 5.46 | 5.46 |
| 425.88 | 5.46 | 5.46 |
| 413.37 | 4.86 | 4.86 |
| 455.86 | 4.85 | 4.85 |
| 468.95 | 5.22 | 5.22 |
| 508.95 | 6.53 | 6.53 |
| 431.91 | 5.52 | 5.52 |
| 439.91 | 5.77 | 5.77 |
| 425.88 | 5.46 | 5.46 |
| 425.88 | 5.46 | 5.46 |
| 445.31 | 6.41 | 6.41 |
| 491.94 | 6.09 | 6.09 |
| 445.94 | 5.83 | 5.83 |
| 494.92 | 6.29 | 6.29 |
| 442.91 | 5.44 | 5.44 |
| 442.91 | 5.61 | 5.61 |
| 411.86 | 5.15 | 5.15 |
| 410.87 | 5.76 | 5.76 |
| 392.96 | 4.52 | 4.52 |
| 469.90 | 4.07 | 4.07 |
| 413.87 | 5.16 | 5.16 |
| 440.90 | 5.36 | 5.36 |
| 428.86 | 5.90 | 5.90 |
| 425.88 | 5.46 | 5.46 |
| 471.43 | 5.80 | 5.80 |
| 342.87 | 4.74 | 4.74 |
| 427.47 | 5.65 | 5.65 |
| 494.92 | 6.29 | 6.29 |
| 425.88 | 5.46 | 5.46 |
| 424.89 | 6.15 | 6.15 |
| 424.89 | 6.01 | 6.01 |
| 374.92 | 4.15 | 4.15 |
| 429.85 | 5.29 | 5.29 |
| 429.85 | 5.29 | 5.29 |
| 443.87 | 5.60 | 5.60 |
| 454.92 | 5.36 | 5.36 |
| 439.91 | 5.72 | 5.72 |
| 390.89 | 4.29 | 4.29 |
| 401.94 | 4.05 | 4.05 |
| 455.91 | 5.47 | 5.47 |
| 451.88 | 5.03 | 5.03 |
| 464.92 | 5.94 | 5.94 |
| 468.88 | 5.77 | 5.77 |
| 468.88 | 5.77 | 5.77 |
| 464.92 | 5.94 | 5.94 |
| 485.34 | 6.29 | 6.29 |
| 480.92 | 5.64 | 5.64 |
| 460.33 | 6.12 | 6.12 |
| 464.92 | 5.65 | 5.65 |
| 490.96 | 6.46 | 6.46 |
| 460.33 | 6.12 | 6.12 |
| 465.91 | 5.34 | 5.34 |
| 521.81 | 6.20 | 6.20 |
| 490.96 | 6.46 | 6.46 |
| 511.38 | 6.80 | 6.80 |
| 407.35 | 4.80 | 4.80 |
| 525.40 | 7.11 | 7.11 |
| 451.88 | 5.03 | 5.03 |
| 476.93 | 6.15 | 6.15 |
| 476.33 | 5.82 | 5.82 |
| 478.91 | 4.74 | 4.74 |
| 490.96 | 6.16 | 6.16 |
| 429.87 | 5.36 | 5.36 |
| 477.92 | 5.54 | 5.54 |
| 415.85 | 4.19 | 4.19 |
| 376.86 | 3.98 | 3.98 |
| 389.93 | 4.12 | 4.12 |
| 476.33 | 5.82 | 5.82 |
| 449.30 | 5.44 | 5.44 |
| 525.40 | 6.91 | 6.91 |
| 442.91 | 5.35 | 5.35 |
| 435.88 | 5.70 | 5.70 |
| 435.88 | 5.70 | 5.70 |
| 414.86 | 4.56 | 4.56 |
| 483.92 | 4.38 | 4.38 |
| 448.32 | 5.81 | 5.81 |
| 427.90 | 5.47 | 5.47 |
| 461.92 | 6.21 | 6.21 |
| 414.86 | 4.56 | 4.56 |
| 460.33 | 6.12 | 6.12 |
| 395.33 | 4.50 | 4.50 |
| 360.89 | 3.85 | 3.85 |