Basic Information
ID: ALA3887280
Type: Binding
Description: null: A commercially available P450-GLO Assay kit (Promega Corporation, Madison Wis.) is used to screen various compounds for CYP3A4A inhibition activity. CYP3A4A is thought to be one of the primary CYP isoforms responsible for retinoic acid metabolism in the skin. Three benchmark agents, liarozole, climbazole, and ketoconazole, were assessed for CYP3A4 inhibition to confirm that the inhibition activity (the IC50 for CYP3A4 inhibition) measured by the assay corresponds to the activity reported by the published literature. The results show that the substituted azole compounds having the specific structure set forth herein are CYP inhibitors, and thus function as RAMBAs.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3887280
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 232.24 | 1.42 | 1.42 |
| 331.35 | 1.58 | 1.58 |
| 252.35 | 0.60 | 0.60 |
| 416.13 | 6.45 | 6.45 |
| 144.18 | 2.08 | 2.08 |
| 68.08 | 0.41 | 0.41 |
| 144.18 | 2.08 | 2.08 |
| 144.18 | 1.87 | 1.87 |
| 82.11 | 0.42 | 0.42 |
| 344.85 | 5.38 | 5.38 |
| 306.28 | 0.74 | 0.74 |
| 236.27 | 3.39 | 3.39 |
| 155.16 | -0.64 | -0.64 |
| 470.02 | 3.55 | 3.55 |
| 354.45 | 3.27 | 3.27 |
| 268.36 | 5.55 | 5.55 |
| 1202.63 | ||
| 204.23 | 1.12 | 1.12 |
| 146.15 | -1.34 | -1.34 |
| 132.12 | -1.73 | -1.73 |
| 226.28 | 2.64 | 2.64 |
| 96.13 | 0.97 | 0.97 |
| 82.11 | 0.72 | 0.72 |
| 118.14 | 1.56 | 1.56 |
| 290.32 | 2.57 | 2.57 |
| 154.56 | 1.01 | 1.01 |
| 165.24 | 0.95 | 0.95 |
| 194.24 | 3.23 | 3.23 |
| 531.44 | 4.21 | 4.21 |
| 184.20 | 2.82 | 2.82 |
| 308.77 | 4.05 | 4.05 |
| 135.13 | -0.11 | -0.11 |
| 180.17 | -1.04 | -1.04 |
| 215.22 | 1.56 | 1.56 |
| 136.11 | 0.06 | 0.06 |
| 84.08 | -0.61 | -0.61 |
| 174.20 | -1.34 | -1.34 |
| 114.17 | 0.71 | 0.71 |
| 272.31 | 3.69 | 3.69 |
| 228.68 | 3.88 | 3.88 |
| 186.21 | 2.07 | 2.07 |
| 192.30 | 3.66 | 3.66 |
| 338.44 | 3.72 | 3.72 |
| 142.16 | -0.15 | -0.15 |
| 146.15 | -1.34 | -1.34 |
| 110.16 | 1.28 | 1.28 |
| 292.77 | 3.73 | 3.73 |
| 110.12 | 0.54 | 0.54 |
| 274.30 | 2.48 | 2.48 |
| 277.75 | 2.73 | 2.73 |
| 747.96 | 2.44 | 2.44 |
| 287.36 | 3.24 | 3.24 |
| 162.15 | 0.60 | 0.60 |
| 225.25 | 1.53 | 1.53 |
| 392.89 | 4.77 | 4.77 |
| 685.89 | 0.64 | 0.64 |
| 240.26 | -0.22 | -0.22 |
| 94.12 | 0.98 | 0.98 |
| 186.64 | 2.22 | 2.22 |
| 312.42 | 5.50 | 5.50 |
| 283.80 | 2.90 | 2.90 |
| 125.17 | 0.23 | 0.23 |
| 414.53 | 3.71 | 3.71 |
| 739.99 | 2.07 | 2.07 |
| 822.95 | 3.93 | 3.93 |