Basic Information
ID: ALA3705828
Type: Binding
Description: Homogeneous Time Resolved Fluorescence Assay: The assay below is used to test the modulatory activity of compounds against FLAP. Human and mouse FLAP-encoding DNA was amplified by polymerase chain reaction and cloned into pFastBac1 (Invitrogen) with a NH2-terminal 6-His tag for expression in Spodoptera frugiperda (Sf-9) cells. FLAP-containing membranes were prepared as was a FITC-labeled FLAP modulator (3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid). The FLAP binding assay is performed in HTRF format (homogeneous time resolved fluorescence). FLAP-containing membranes (1 ug/well final for human) are incubated in the presence of the HTRF ligand, [5-[({[2-(2-{3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropanoyl}hydrazino)-2-oxoethyl]sulfanyl}acetyl)amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid] (25 nM final), a terbium labeled anti-His tag antibody (0.5 ng/well final, from Cisbio) and compounds.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705828
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 337.36 | 3.71 | 3.71 |
| 315.39 | 4.31 | 4.31 |
| 387.46 | 6.00 | 6.00 |
| 333.44 | 4.60 | 4.60 |
| 329.76 | 4.10 | 4.10 |
| 331.42 | 4.57 | 4.57 |
| 298.32 | 3.01 | 3.01 |
| 273.31 | 3.14 | 3.14 |
| 282.32 | 4.34 | 4.34 |
| 283.31 | 3.74 | 3.74 |
| 284.29 | 2.71 | 2.71 |
| 259.28 | 2.84 | 2.84 |
| 594.63 | 6.95 | 6.95 |
| 378.41 | 4.54 | 4.54 |
| 393.42 | 4.12 | 4.12 |
| 408.43 | 4.55 | 4.55 |
| 390.42 | 5.23 | 5.23 |
| 391.41 | 4.62 | 4.62 |
| 361.38 | 4.61 | 4.61 |
| 337.36 | 3.71 | 3.71 |
| 367.38 | 3.72 | 3.72 |
| 353.36 | 3.42 | 3.42 |
| 362.37 | 3.59 | 3.59 |
| 394.45 | 4.09 | 4.09 |
| 394.45 | 4.09 | 4.09 |
| 380.43 | 3.78 | 3.78 |
| 435.43 | 5.24 | 5.24 |
| 414.46 | 3.72 | 3.72 |
| 408.48 | 4.59 | 4.59 |
| 492.56 | 4.45 | 4.45 |
| 408.48 | 4.50 | 4.50 |
| 296.35 | 4.65 | 4.65 |
| 380.45 | 2.06 | 2.06 |
| 372.44 | 2.84 | 2.84 |
| 373.43 | 3.85 | 3.85 |
| 428.51 | 4.38 | 4.38 |
| 442.54 | 4.77 | 4.77 |
| 442.54 | 4.91 | 4.91 |
| 456.56 | 5.16 | 5.16 |
| 303.34 | 2.50 | 2.50 |
| 345.37 | 3.38 | 3.38 |
| 343.40 | 3.69 | 3.69 |
| 388.49 | 3.12 | 3.12 |
| 333.36 | 1.86 | 1.86 |
| 402.47 | 2.20 | 2.20 |
| 450.54 | 1.60 | 1.60 |
| 337.36 | 3.71 | 3.71 |
| 352.37 | 3.30 | 3.30 |
| 337.36 | 3.71 | 3.71 |
| 337.36 | 3.71 | 3.71 |
| 408.48 | 4.78 | 4.78 |
| 448.45 | 4.64 | 4.64 |
| 466.47 | 3.64 | 3.64 |
| 357.43 | 3.94 | 3.94 |
| 438.48 | 4.20 | 4.20 |
| 471.38 | 6.96 | 6.96 |
| 344.43 | 3.46 | 3.46 |
| 330.41 | 3.07 | 3.07 |
| 380.43 | 4.06 | 4.06 |
| 376.39 | 4.20 | 4.20 |
| 423.40 | 5.15 | 5.15 |
| 402.43 | 4.45 | 4.45 |
| 377.38 | 3.17 | 3.17 |
| 298.32 | 3.03 | 3.03 |
| 337.36 | 3.71 | 3.71 |
| 323.33 | 3.32 | 3.32 |
| 338.35 | 2.91 | 2.91 |
| 353.40 | 3.44 | 3.44 |
| 398.39 | 3.49 | 3.49 |
| 384.37 | 3.40 | 3.40 |
| 406.49 | 5.32 | 5.32 |
| 353.40 | 3.44 | 3.44 |
| 353.40 | 3.44 | 3.44 |
| 351.38 | 3.50 | 3.50 |
| 384.84 | 4.76 | 4.76 |
| 375.41 | 3.98 | 3.98 |
| 354.39 | 4.01 | 4.01 |
| 375.41 | 3.98 | 3.98 |
| 432.46 | 3.81 | 3.81 |
| 302.35 | 2.47 | 2.47 |
| 380.43 | 3.41 | 3.41 |
| 380.43 | 3.41 | 3.41 |
| 380.43 | 3.41 | 3.41 |
| 356.45 | 3.51 | 3.51 |
| 356.45 | 3.51 | 3.51 |
| 342.42 | 3.12 | 3.12 |
| 328.39 | 2.73 | 2.73 |
| 342.42 | 3.26 | 3.26 |
| 400.50 | 3.36 | 3.36 |
| 346.41 | 2.09 | 2.09 |
| 374.46 | 2.87 | 2.87 |
| 386.47 | 2.97 | 2.97 |
| 360.43 | 2.43 | 2.43 |
| 402.47 | 1.94 | 1.94 |
| 401.49 | 1.78 | 1.78 |
| 411.44 | 2.13 | 2.13 |
| 449.49 | 3.22 | 3.22 |
| 401.44 | 1.90 | 1.90 |
| 430.45 | 3.75 | 3.75 |
| 297.29 | 2.76 | 2.76 |
| 312.31 | 2.34 | 2.34 |
| 311.32 | 3.01 | 3.01 |
| 326.34 | 2.59 | 2.59 |
| 325.35 | 3.57 | 3.57 |
| 325.35 | 3.40 | 3.40 |
| 365.41 | 4.49 | 4.49 |
| 379.44 | 4.57 | 4.57 |
| 353.40 | 4.04 | 4.04 |
| 339.37 | 3.65 | 3.65 |
| 353.40 | 4.04 | 4.04 |
| 380.43 | 4.08 | 4.08 |
| 394.45 | 4.15 | 4.15 |
| 368.42 | 3.62 | 3.62 |
| 354.39 | 3.23 | 3.23 |
| 380.38 | 2.81 | 2.81 |
| 393.45 | 4.93 | 4.93 |
| 407.47 | 5.24 | 5.24 |
| 395.44 | 3.00 | 3.00 |
| 273.31 | 3.14 | 3.14 |
| 259.28 | 2.84 | 2.84 |
| 417.41 | 5.73 | 5.73 |
| 417.41 | 5.73 | 5.73 |
| 417.41 | 5.73 | 5.73 |
| 393.42 | 4.41 | 4.41 |
| 393.42 | 4.41 | 4.41 |
| 427.50 | 4.11 | 4.11 |
| 427.50 | 4.11 | 4.11 |
| 433.40 | 5.61 | 5.61 |
| 433.40 | 5.61 | 5.61 |
| 433.40 | 5.61 | 5.61 |
| 461.95 | 4.77 | 4.77 |
| 391.45 | 4.91 | 4.91 |
| 350.40 | 4.11 | 4.11 |
| 350.40 | 4.11 | 4.11 |
| 374.42 | 4.58 | 4.58 |
| 374.42 | 4.58 | 4.58 |
| 392.43 | 3.81 | 3.81 |
| 374.42 | 4.58 | 4.58 |
| 392.43 | 3.81 | 3.81 |
| 417.45 | 3.89 | 3.89 |
| 417.45 | 3.89 | 3.89 |
| 417.45 | 3.89 | 3.89 |
| 407.45 | 4.34 | 4.34 |
| 350.40 | 4.11 | 4.11 |
| 456.54 | 3.96 | 3.96 |
| 428.49 | 3.36 | 3.36 |
| 442.52 | 3.62 | 3.62 |
| 367.40 | 4.85 | 4.85 |
| 367.40 | 4.85 | 4.85 |
| 367.40 | 4.85 | 4.85 |
| 385.39 | 4.99 | 4.99 |
| 385.39 | 4.99 | 4.99 |
| 385.39 | 4.99 | 4.99 |
| 383.85 | 5.36 | 5.36 |
| 383.85 | 5.36 | 5.36 |
| 383.85 | 5.36 | 5.36 |
| 418.30 | 6.02 | 6.02 |
| 418.30 | 6.02 | 6.02 |
| 418.30 | 6.02 | 6.02 |
| 418.30 | 6.02 | 6.02 |
| 377.46 | 5.33 | 5.33 |
| 451.85 | 6.38 | 6.38 |
| 451.85 | 6.38 | 6.38 |
| 435.40 | 5.87 | 5.87 |
| 401.84 | 5.50 | 5.50 |
| 393.42 | 4.41 | 4.41 |
| 353.40 | 3.44 | 3.44 |
| 381.41 | 3.97 | 3.97 |
| 373.43 | 3.85 | 3.85 |
| 317.32 | 2.60 | 2.60 |
| 410.45 | 2.73 | 2.73 |
| 411.44 | 2.13 | 2.13 |
| 411.44 | 2.13 | 2.13 |
| 411.44 | 2.13 | 2.13 |
| 410.45 | 2.77 | 2.77 |
| 410.45 | 2.77 | 2.77 |
| 410.45 | 2.77 | 2.77 |
| 425.47 | 2.36 | 2.36 |
| 425.47 | 2.36 | 2.36 |
| 383.43 | 2.77 | 2.77 |
| 383.43 | 2.77 | 2.77 |
| 384.42 | 2.16 | 2.16 |
| 384.42 | 2.16 | 2.16 |
| 384.42 | 2.16 | 2.16 |
| 423.45 | 2.22 | 2.22 |
| 399.43 | 1.75 | 1.75 |
| 398.44 | 2.71 | 2.71 |
| 434.54 | 3.18 | 3.18 |
| 351.38 | 4.02 | 4.02 |
| 355.37 | 3.40 | 3.40 |
| 355.46 | 5.09 | 5.09 |
| 313.38 | 3.92 | 3.92 |
| 411.43 | 4.48 | 4.48 |
| 456.56 | 5.16 | 5.16 |
| 355.37 | 3.40 | 3.40 |
| 327.40 | 4.31 | 4.31 |
| 349.41 | 4.71 | 4.71 |
| 407.45 | 4.45 | 4.45 |
| 383.38 | 4.00 | 4.00 |
| 366.40 | 3.61 | 3.61 |
| 413.46 | 5.38 | 5.38 |
| 383.45 | 4.44 | 4.44 |
| 365.41 | 4.33 | 4.33 |
| 419.49 | 5.44 | 5.44 |
| 367.38 | 3.72 | 3.72 |
| 367.38 | 3.72 | 3.72 |
| 415.45 | 3.12 | 3.12 |
| 366.40 | 3.61 | 3.61 |
| 367.38 | 3.72 | 3.72 |
| 353.36 | 3.42 | 3.42 |
| 382.40 | 3.31 | 3.31 |
| 382.40 | 3.31 | 3.31 |
| 360.39 | 4.80 | 4.80 |
| 404.37 | 5.34 | 5.34 |
| 393.42 | 4.71 | 4.71 |
| 405.36 | 4.73 | 4.73 |
| 405.36 | 4.73 | 4.73 |
| 405.36 | 4.73 | 4.73 |
| 394.41 | 4.11 | 4.11 |
| 361.38 | 4.19 | 4.19 |
| 361.38 | 4.19 | 4.19 |
| 361.38 | 4.19 | 4.19 |
| 361.38 | 4.19 | 4.19 |
| 361.38 | 4.19 | 4.19 |
| 404.37 | 5.34 | 5.34 |
| 361.38 | 4.19 | 4.19 |
| 413.47 | 4.33 | 4.33 |
| 413.47 | 4.33 | 4.33 |
| 352.37 | 3.30 | 3.30 |
| 471.38 | 6.96 | 6.96 |
| 404.37 | 5.34 | 5.34 |
| 370.81 | 4.97 | 4.97 |
| 447.92 | 4.98 | 4.98 |
| 405.36 | 4.73 | 4.73 |
| 405.36 | 4.73 | 4.73 |
| 427.50 | 4.64 | 4.64 |
| 481.47 | 5.35 | 5.35 |
| 404.37 | 5.34 | 5.34 |
| 366.40 | 4.33 | 4.33 |
| 352.37 | 3.30 | 3.30 |
| 405.36 | 4.73 | 4.73 |
| 438.48 | 4.88 | 4.88 |
| 481.47 | 5.35 | 5.35 |
| 351.38 | 4.02 | 4.02 |
| 379.44 | 4.84 | 4.84 |
| 352.37 | 3.30 | 3.30 |
| 371.80 | 4.37 | 4.37 |
| 392.44 | 3.92 | 3.92 |
| 448.42 | 4.80 | 4.80 |
| 366.40 | 3.61 | 3.61 |
| 377.42 | 4.59 | 4.59 |
| 396.43 | 3.44 | 3.44 |
| 386.82 | 3.95 | 3.95 |
| 413.46 | 5.38 | 5.38 |
| 413.46 | 5.38 | 5.38 |
| 442.50 | 4.89 | 4.89 |
| 379.44 | 4.84 | 4.84 |
| 432.38 | 5.23 | 5.23 |
| 495.56 | 4.65 | 4.65 |
| 395.44 | 3.09 | 3.09 |
| 395.39 | 3.50 | 3.50 |
| 381.37 | 3.41 | 3.41 |
| 379.39 | 4.62 | 4.62 |
| 380.38 | 4.02 | 4.02 |
| 378.41 | 4.02 | 4.02 |
| 423.50 | 3.69 | 3.69 |
| 380.38 | 2.81 | 2.81 |
| 352.37 | 3.30 | 3.30 |
| 273.31 | 3.14 | 3.14 |
| 259.28 | 2.84 | 2.84 |
| 337.36 | 3.71 | 3.71 |
| 352.37 | 3.30 | 3.30 |
| 396.43 | 3.44 | 3.44 |
| 351.38 | 4.02 | 4.02 |
| 352.37 | 3.30 | 3.30 |
| 379.44 | 4.84 | 4.84 |
| 352.37 | 3.30 | 3.30 |
| 365.41 | 4.33 | 4.33 |
| 394.45 | 4.42 | 4.42 |
| 380.38 | 2.81 | 2.81 |
| 367.38 | 3.72 | 3.72 |
| 353.36 | 3.42 | 3.42 |
| 298.32 | 3.01 | 3.01 |
| 284.29 | 2.71 | 2.71 |
| 418.43 | 4.28 | 4.28 |
| 297.33 | 4.04 | 4.04 |
| 283.31 | 3.74 | 3.74 |
| 441.43 | 6.63 | 6.63 |
| 373.43 | 5.61 | 5.61 |
| 272.32 | 3.75 | 3.75 |
| 258.30 | 3.44 | 3.44 |
| 406.46 | 5.10 | 5.10 |
| 392.43 | 5.01 | 5.01 |
| 298.32 | 3.44 | 3.44 |
| 297.33 | 4.04 | 4.04 |
| 314.36 | 3.97 | 3.97 |
| 300.33 | 3.67 | 3.67 |
| 390.46 | 5.54 | 5.54 |
| 415.47 | 5.41 | 5.41 |
| 468.55 | 4.94 | 4.94 |
| 404.49 | 5.85 | 5.85 |
| 415.47 | 6.09 | 6.09 |
| 458.46 | 6.56 | 6.56 |
| 433.48 | 4.64 | 4.64 |
| 433.48 | 5.11 | 5.11 |
| 445.42 | 6.17 | 6.17 |
| 448.49 | 5.17 | 5.17 |
| 297.33 | 4.04 | 4.04 |
| 298.36 | 4.13 | 4.13 |
| 284.33 | 3.83 | 3.83 |
| 261.30 | 2.87 | 2.87 |
| 375.56 | ||
| 339.37 | 3.74 | 3.74 |
| 354.39 | 3.33 | 3.33 |
| 354.39 | 3.33 | 3.33 |
| 369.40 | 3.75 | 3.75 |
| 275.33 | 3.17 | 3.17 |
| 261.30 | 2.87 | 2.87 |
| 375.56 | ||
| 339.37 | 3.74 | 3.74 |
| 354.39 | 3.33 | 3.33 |
| 354.39 | 3.33 | 3.33 |
| 298.12 | 2.64 | 2.64 |
| 287.34 | 3.53 | 3.53 |
| 363.44 | 5.10 | 5.10 |