Basic Information
ID: ALA3705947
Type: Binding
Description: Binding 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 ALA3705947
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 570.49 | 7.33 | 7.33 |
| 570.49 | 7.33 | 7.33 |
| 549.55 | 6.76 | 6.76 |
| 549.55 | 6.76 | 6.76 |
| 549.55 | 6.76 | 6.76 |
| 598.54 | 7.80 | 7.80 |
| 562.44 | 6.77 | 6.77 |
| 501.53 | 6.14 | 6.14 |
| 513.54 | 6.31 | 6.31 |
| 534.44 | 7.17 | 7.17 |
| 546.45 | 7.34 | 7.34 |
| 574.45 | 6.94 | 6.94 |
| 588.48 | 7.47 | 7.47 |
| 588.48 | 7.47 | 7.47 |
| 598.54 | 7.80 | 7.80 |
| 573.65 | 6.93 | 6.93 |
| 575.67 | 7.00 | 7.00 |
| 573.65 | 6.76 | 6.76 |
| 618.53 | 7.49 | 7.49 |
| 572.50 | 7.41 | 7.41 |
| 618.53 | 7.39 | 7.39 |
| 545.64 | 6.41 | 6.41 |
| 544.45 | 6.63 | 6.63 |
| 562.44 | 6.77 | 6.77 |
| 550.48 | 6.69 | 6.69 |
| 570.49 | 7.16 | 7.16 |
| 606.52 | 7.56 | 7.56 |
| 556.46 | 6.80 | 6.80 |
| 544.45 | 6.63 | 6.63 |
| 544.45 | 6.63 | 6.63 |
| 516.60 | 6.44 | 6.44 |
| 491.59 | 6.57 | 6.57 |
| 575.59 | 7.47 | 7.47 |
| 505.62 | 6.88 | 6.88 |
| 559.59 | 7.59 | 7.59 |
| 593.58 | 7.61 | 7.61 |
| 593.58 | 7.61 | 7.61 |
| 505.62 | 6.88 | 6.88 |
| 575.59 | 7.47 | 7.47 |
| 516.60 | 6.44 | 6.44 |
| 575.59 | 7.47 | 7.47 |
| 505.62 | 6.88 | 6.88 |
| 559.59 | 7.59 | 7.59 |
| 516.60 | 6.44 | 6.44 |
| 588.48 | 7.47 | 7.47 |
| 588.48 | 7.47 | 7.47 |
| 588.48 | 7.47 | 7.47 |
| 604.93 | 7.99 | 7.99 |
| 604.93 | 7.99 | 7.99 |
| 559.59 | 7.42 | 7.42 |
| 509.58 | 6.54 | 6.54 |
| 521.62 | 6.41 | 6.41 |
| 575.59 | 7.30 | 7.30 |
| 492.58 | 5.79 | 5.79 |
| 492.58 | 5.79 | 5.79 |
| 526.04 | 7.05 | 7.05 |
| 572.50 | 7.58 | 7.58 |
| 479.58 | 6.17 | 6.17 |
| 483.54 | 6.00 | 6.00 |
| 500.00 | 6.52 | 6.52 |
| 479.58 | 6.17 | 6.17 |
| 500.00 | 6.52 | 6.52 |
| 495.58 | 5.87 | 5.87 |
| 533.55 | 6.88 | 6.88 |
| 558.48 | 7.19 | 7.19 |
| 534.44 | 7.17 | 7.17 |
| 551.54 | 7.02 | 7.02 |
| 517.99 | 6.66 | 6.66 |
| 465.55 | 5.87 | 5.87 |
| 500.00 | 6.52 | 6.52 |
| 598.69 | 7.10 | 7.10 |
| 515.61 | 7.02 | 7.02 |
| 516.60 | 6.41 | 6.41 |
| 522.63 | 6.47 | 6.47 |
| 534.66 | 6.25 | 6.25 |
| 543.65 | 5.27 | 5.27 |
| 507.55 | 5.40 | 5.40 |
| 516.60 | 6.41 | 6.41 |
| 519.61 | 5.75 | 5.75 |
| 502.57 | 6.59 | 6.59 |
| 516.60 | 6.95 | 6.95 |
| 570.49 | 7.16 | 7.16 |
| 516.60 | 6.27 | 6.27 |
| 567.69 | 8.07 | 8.07 |
| 585.68 | 8.21 | 8.21 |
| 581.72 | 8.37 | 8.37 |
| 599.69 | 6.86 | 6.86 |
| 598.70 | 7.47 | 7.47 |
| 603.67 | 8.34 | 8.34 |
| 660.80 | 7.44 | 7.44 |
| 574.71 | 7.52 | 7.52 |
| 571.68 | 6.80 | 6.80 |
| 557.65 | 7.66 | 7.66 |
| 586.69 | 7.67 | 7.67 |
| 558.66 | 7.94 | 7.94 |
| 589.64 | 7.98 | 7.98 |
| 607.63 | 8.12 | 8.12 |
| 574.71 | 7.52 | 7.52 |
| 560.68 | 7.16 | 7.16 |
| 586.69 | 7.67 | 7.67 |
| 560.68 | 7.16 | 7.16 |
| 653.68 | 9.40 | 9.40 |
| 557.65 | 7.66 | 7.66 |
| 598.70 | 7.47 | 7.47 |
| 636.67 | 8.48 | 8.48 |
| 585.68 | 8.21 | 8.21 |
| 612.73 | 7.86 | 7.86 |
| 611.75 | 7.53 | 7.53 |
| 603.67 | 8.34 | 8.34 |
| 612.73 | 6.92 | 6.92 |
| 567.69 | 8.07 | 8.07 |
| 609.77 | 9.19 | 9.19 |
| 660.80 | 7.44 | 7.44 |
| 666.70 | 8.49 | 8.49 |
| 645.78 | 7.47 | 7.47 |
| 599.69 | 6.86 | 6.86 |
| 571.68 | 6.80 | 6.80 |
| 557.65 | 6.79 | 6.79 |
| 660.80 | 7.44 | 7.44 |
| 585.66 | 6.50 | 6.50 |
| 585.66 | 6.50 | 6.50 |
| 589.64 | 7.98 | 7.98 |
| 589.64 | 7.98 | 7.98 |
| 571.65 | 7.84 | 7.84 |
| 571.65 | 7.84 | 7.84 |
| 599.69 | 7.04 | 7.04 |
| 569.67 | 7.03 | 7.03 |
| 636.67 | 8.65 | 8.65 |
| 660.80 | 7.61 | 7.61 |
| 636.67 | 8.65 | 8.65 |
| 660.80 | 7.61 | 7.61 |
| 635.69 | 9.26 | 9.26 |
| 653.68 | 9.40 | 9.40 |
| 635.69 | 9.26 | 9.26 |
| 557.65 | 6.79 | 6.79 |
| 530.63 | 6.47 | 6.47 |
| 572.67 | 6.94 | 6.94 |
| 610.64 | 7.95 | 7.95 |
| 573.65 | 6.33 | 6.33 |
| 572.67 | 6.94 | 6.94 |
| 572.67 | 6.94 | 6.94 |
| 530.63 | 6.86 | 6.86 |
| 634.76 | 6.90 | 6.90 |
| 555.68 | 7.84 | 7.84 |
| 555.68 | 7.84 | 7.84 |
| 545.64 | 6.27 | 6.27 |
| 620.73 | 6.18 | 6.18 |
| 559.64 | 7.67 | 7.67 |
| 559.64 | 7.67 | 7.67 |
| 559.64 | 7.67 | 7.67 |
| 610.64 | 7.95 | 7.95 |
| 585.66 | 7.23 | 7.23 |
| 566.66 | 7.40 | 7.40 |
| 566.66 | 7.40 | 7.40 |
| 619.74 | 6.94 | 6.94 |
| 542.64 | 6.93 | 6.93 |
| 542.64 | 6.93 | 6.93 |
| 620.73 | 6.18 | 6.18 |
| 530.63 | 6.86 | 6.86 |
| 548.67 | 6.99 | 6.99 |
| 634.76 | 6.90 | 6.90 |
| 619.74 | 6.94 | 6.94 |
| 571.68 | 7.54 | 7.54 |
| 634.76 | 6.90 | 6.90 |
| 620.73 | 6.18 | 6.18 |
| 584.68 | 6.63 | 6.63 |
| 598.70 | 7.49 | 7.49 |
| 634.76 | 6.90 | 6.90 |
| 584.68 | 6.63 | 6.63 |
| 548.67 | 6.99 | 6.99 |
| 545.64 | 6.27 | 6.27 |
| 545.64 | 6.27 | 6.27 |
| 555.68 | 7.84 | 7.84 |
| 610.64 | 7.95 | 7.95 |
| 566.66 | 7.40 | 7.40 |
| 619.74 | 6.94 | 6.94 |
| 545.64 | 6.27 | 6.27 |
| 532.60 | 6.52 | 6.52 |
| 548.67 | 6.99 | 6.99 |
| 548.67 | 6.99 | 6.99 |
| 569.67 | 7.03 | 7.03 |
| 569.67 | 7.03 | 7.03 |
| 574.72 | 7.56 | 7.56 |
| 628.69 | 7.94 | 7.94 |
| 628.69 | 7.94 | 7.94 |
| 614.67 | 7.55 | 7.55 |
| 600.64 | 7.16 | 7.16 |
| 660.71 | 8.49 | 8.49 |
| 660.71 | 8.49 | 8.49 |
| 576.70 | 6.24 | 6.24 |
| 574.73 | 7.39 | 7.39 |
| 560.70 | 7.00 | 7.00 |
| 520.63 | 6.08 | 6.08 |
| 584.67 | 7.10 | 7.10 |
| 550.66 | 5.70 | 5.70 |
| 548.69 | 6.86 | 6.86 |
| 534.66 | 6.47 | 6.47 |
| 531.62 | 6.05 | 6.05 |
| 532.60 | 5.45 | 5.45 |
| 532.60 | 5.45 | 5.45 |
| 576.52 | 7.39 | 7.39 |
| 576.52 | 7.39 | 7.39 |
| 562.49 | 6.86 | 6.86 |
| 576.52 | 7.39 | 7.39 |
| 578.53 | 7.47 | 7.47 |
| 605.72 | 7.10 | 7.10 |
| 575.69 | 7.09 | 7.09 |
| 642.70 | 8.71 | 8.71 |
| 604.73 | 7.70 | 7.70 |
| 575.69 | 7.09 | 7.09 |
| 577.71 | 7.16 | 7.16 |
| 580.75 | 7.62 | 7.62 |
| 570.49 | 7.33 | 7.33 |
| 570.49 | 7.33 | 7.33 |
| 593.58 | 7.61 | 7.61 |