Basic Information
ID: ALA3706064
Type: Binding
Description: Inhibition Assay: The PDE 4 (phosphodiesterase IV) inhibiting effect of the compounds of the present invention was performed by the following method, which was modified assay method described in Biochemical. Pharmacol. 48(6), 1219-1223 (1994). (1) The active fraction of PDE 4 (phosphodiesterase IV) was obtained. That is, the livers obtained from three Balb/c mice (male, 12 weeks: obtainable from CLEA Japan, Inc.) were suspended with 30 mL of buffer solution B [20 mM of bis-tris, 5 mM of 2-mercaptoethnol, 2 mM of benzamidine, 2 mM of EDTA, 0.1 mM of 4-(2-aminoethyl)benzensulfonyl hydrochloride, 50 mM of sodium acetate; pH 6.5], then homogenized by Polytron homogenizer. The homogenate were centrifuged under 25,000xG for 10 minutes at 4 C. The supernatant was separated and thus obtained supernatant was further centrifuged under 100,000xG for 60 minutes at 4° C., and then filtrated with 0.2 um filter to obtain the soluble fraction.
Format: BAO_0000019
Target: Phosphodiesterase 4B(ALA2272)
Document: ALA3638901
BindingDB Source: 6586
Activity Charts
Bioactivity
Activity Types for Assay ALA3706064
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 426.54 | 5.13 | 5.13 |
| 422.55 | 5.07 | 5.07 |
| 426.54 | 5.73 | 5.73 |
| 380.52 | 5.13 | 5.13 |
| 424.57 | 5.00 | 5.00 |
| 396.52 | 4.52 | 4.52 |
| 436.58 | 5.46 | 5.46 |
| 450.61 | 5.71 | 5.71 |
| 464.64 | 6.10 | 6.10 |
| 394.50 | 4.66 | 4.66 |
| 410.54 | 4.91 | 4.91 |
| 465.62 | 4.55 | 4.55 |
| 501.68 | 4.10 | 4.10 |
| 440.57 | 4.54 | 4.54 |
| 381.50 | 5.37 | 5.37 |
| 410.54 | 4.87 | 4.87 |
| 411.53 | 5.34 | 5.34 |
| 383.47 | 4.86 | 4.86 |
| 424.57 | 5.30 | 5.30 |
| 426.54 | 3.89 | 3.89 |
| 397.50 | 4.52 | 4.52 |
| 438.60 | 5.69 | 5.69 |
| 382.49 | 4.73 | 4.73 |
| 448.59 | 5.46 | 5.46 |
| 458.61 | 4.49 | 4.49 |
| 420.54 | 5.78 | 5.78 |
| 426.54 | 4.29 | 4.29 |
| 410.54 | 4.45 | 4.45 |
| 423.59 | 4.57 | 4.57 |
| 465.62 | 4.83 | 4.83 |
| 361.51 | 3.94 | 3.94 |
| 495.65 | 4.32 | 4.32 |
| 440.57 | 4.63 | 4.63 |
| 402.56 | 4.09 | 4.09 |
| 410.54 | 5.51 | 5.51 |
| 354.48 | 4.75 | 4.75 |
| 396.52 | 5.12 | 5.12 |
| 426.54 | 4.75 | 4.75 |
| 398.49 | 4.35 | 4.35 |
| 397.50 | 3.92 | 3.92 |
| 437.61 | 4.92 | 4.92 |
| 438.60 | 4.31 | 4.31 |
| 501.68 | 4.10 | 4.10 |
| 432.57 | 4.07 | 4.07 |
| 451.64 | 5.31 | 5.31 |
| 438.60 | 5.12 | 5.12 |
| 440.57 | 5.52 | 5.52 |
| 430.55 | 4.73 | 4.73 |
| 430.62 | 4.28 | 4.28 |
| 422.60 | 5.63 | 5.63 |
| 436.63 | 5.97 | 5.97 |
| 495.65 | 4.56 | 4.56 |
| 496.63 | 4.77 | 4.77 |
| 456.57 | 3.89 | 3.89 |
| 426.54 | 4.53 | 4.53 |
| 455.60 | 5.05 | 5.05 |
| 472.06 | 5.57 | 5.57 |
| 456.59 | 5.26 | 5.26 |
| 473.04 | 5.78 | 5.78 |
| 469.63 | 5.49 | 5.49 |
| 486.09 | 6.01 | 6.01 |
| 443.66 | 4.20 | 4.20 |
| 457.69 | 4.59 | 4.59 |
| 458.67 | 5.06 | 5.06 |
| 443.66 | 4.25 | 4.25 |
| 485.70 | 4.51 | 4.51 |
| 432.63 | 4.53 | 4.53 |
| 444.65 | 4.41 | 4.41 |
| 458.67 | 5.06 | 5.06 |
| 457.69 | 4.64 | 4.64 |
| 499.73 | 4.90 | 4.90 |
| 471.72 | 4.98 | 4.98 |
| 443.66 | 4.38 | 4.38 |
| 429.63 | 3.86 | 3.86 |
| 471.67 | 4.12 | 4.12 |
| 469.63 | 5.44 | 5.44 |
| 439.59 | 3.76 | 3.76 |
| 457.58 | 3.90 | 3.90 |
| 438.60 | 5.00 | 5.00 |
| 410.59 | 5.27 | 5.27 |
| 452.62 | 5.04 | 5.04 |
| 465.58 | 4.56 | 4.56 |
| 451.55 | 4.56 | 4.56 |
| 375.49 | 3.89 | 3.89 |
| 417.54 | 1.94 | 1.94 |
| 402.56 | 3.90 | 3.90 |
| 402.56 | 3.90 | 3.90 |
| 417.58 | 3.79 | 3.79 |
| 403.55 | 3.40 | 3.40 |
| 446.62 | 3.65 | 3.65 |
| 360.53 | 3.91 | 3.91 |
| 471.67 | 3.97 | 3.97 |
| 472.66 | 4.18 | 4.18 |
| 370.52 | 4.72 | 4.72 |
| 428.60 | 4.48 | 4.48 |
| 389.52 | 4.28 | 4.28 |
| 458.63 | 4.06 | 4.06 |
| 416.59 | 4.29 | 4.29 |
| 430.62 | 4.28 | 4.28 |
| 375.54 | 4.19 | 4.19 |