Basic Information
ID: ALA3705618
Type: Binding
Description: Homogeneous Time Resolved Fluorescence Assay: 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 μg/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. The reaction is allowed to proceed for two hours after which the plate is read on an Envision plate reader in HTRF mode.
Activity Charts
Bioactivity
Activity Types for Assay ALA3705618
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 534.45 | 6.49 | 6.49 |
| 552.44 | 6.63 | 6.63 |
| 536.47 | 6.56 | 6.56 |
| 534.45 | 6.32 | 6.32 |
| 552.44 | 6.63 | 6.63 |
| 552.44 | 6.63 | 6.63 |
| 552.44 | 6.63 | 6.63 |
| 552.44 | 6.63 | 6.63 |
| 492.46 | 7.11 | 7.11 |
| 538.42 | 6.09 | 6.09 |
| 538.42 | 6.09 | 6.09 |
| 480.57 | 5.60 | 5.60 |
| 482.58 | 5.67 | 5.67 |
| 557.54 | 6.76 | 6.76 |
| 557.54 | 6.76 | 6.76 |
| 541.57 | 6.70 | 6.70 |
| 559.56 | 6.84 | 6.84 |
| 576.02 | 7.35 | 7.35 |
| 525.53 | 6.09 | 6.09 |
| 557.54 | 6.76 | 6.76 |
| 539.55 | 6.62 | 6.62 |
| 559.56 | 6.84 | 6.84 |
| 574.00 | 7.28 | 7.28 |
| 599.65 | 8.41 | 8.41 |
| 528.53 | 5.65 | 5.65 |
| 480.57 | 5.60 | 5.60 |
| 523.43 | 5.52 | 5.52 |
| 525.45 | 5.59 | 5.59 |
| 529.69 | 5.82 | 5.82 |
| 528.53 | 5.65 | 5.65 |
| 523.43 | 5.35 | 5.35 |
| 469.55 | 4.63 | 4.63 |
| 471.56 | 4.70 | 4.70 |
| 530.55 | 5.73 | 5.73 |
| 546.52 | 5.79 | 5.79 |
| 528.53 | 5.65 | 5.65 |
| 546.52 | 5.79 | 5.79 |
| 548.54 | 5.87 | 5.87 |
| 548.54 | 5.87 | 5.87 |
| 543.44 | 5.73 | 5.73 |
| 526.41 | 5.92 | 5.92 |
| 552.44 | 6.46 | 6.46 |
| 552.44 | 6.63 | 6.63 |
| 538.42 | 6.09 | 6.09 |
| 473.55 | 5.64 | 5.64 |
| 554.46 | 6.70 | 6.70 |
| 557.54 | 6.76 | 6.76 |
| 557.54 | 6.76 | 6.76 |
| 487.58 | 6.17 | 6.17 |
| 559.56 | 6.84 | 6.84 |
| 487.58 | 6.17 | 6.17 |
| 489.59 | 6.25 | 6.25 |
| 541.55 | 6.71 | 6.71 |
| 487.58 | 6.00 | 6.00 |
| 543.52 | 6.23 | 6.23 |
| 568.90 | 7.14 | 7.14 |
| 554.87 | 6.61 | 6.61 |
| 568.90 | 7.14 | 7.14 |
| 568.90 | 6.97 | 6.97 |
| 542.86 | 6.44 | 6.44 |
| 524.07 | 7.53 | 7.53 |
| 557.88 | 6.17 | 6.17 |
| 558.56 | 5.66 | 5.66 |
| 544.57 | 6.04 | 6.04 |
| 541.42 | 5.66 | 5.66 |
| 559.41 | 5.80 | 5.80 |
| 564.51 | 5.93 | 5.93 |
| 487.54 | 4.77 | 4.77 |
| 555.60 | 7.01 | 7.01 |
| 497.39 | 4.81 | 4.81 |
| 508.42 | 5.78 | 5.78 |
| 591.99 | 7.42 | 7.42 |
| 520.43 | 5.95 | 5.95 |
| 520.43 | 5.95 | 5.95 |
| 509.40 | 4.98 | 4.98 |
| 508.42 | 5.78 | 5.78 |
| 469.59 | 6.03 | 6.03 |
| 455.56 | 5.50 | 5.50 |
| 514.50 | 5.12 | 5.12 |
| 588.42 | 6.91 | 6.91 |
| 570.43 | 6.77 | 6.77 |
| 479.53 | 5.61 | 5.61 |
| 526.41 | 5.92 | 5.92 |
| 544.40 | 6.06 | 6.06 |
| 562.39 | 6.20 | 6.20 |
| 549.50 | 6.20 | 6.20 |
| 538.42 | 6.09 | 6.09 |
| 520.43 | 5.95 | 5.95 |
| 509.40 | 4.98 | 4.98 |
| 500.57 | 5.81 | 5.81 |
| 554.46 | 6.70 | 6.70 |
| 653.62 | 8.83 | 8.83 |
| 635.63 | 8.69 | 8.69 |
| 617.64 | 8.55 | 8.55 |
| 570.43 | 6.77 | 6.77 |
| 609.60 | 7.98 | 7.98 |
| 591.61 | 7.85 | 7.85 |
| 591.61 | 7.85 | 7.85 |
| 519.65 | 6.88 | 6.88 |
| 555.64 | 9.10 | 9.10 |
| 555.64 | 9.10 | 9.10 |
| 601.67 | 8.49 | 8.49 |
| 565.67 | 6.07 | 6.07 |
| 538.69 | 6.72 | 6.72 |
| 578.64 | 6.71 | 6.71 |
| 564.61 | 6.32 | 6.32 |
| 564.61 | 6.32 | 6.32 |
| 571.58 | 5.49 | 5.49 |
| 545.66 | 5.88 | 5.88 |
| 576.69 | 7.04 | 7.04 |
| 564.61 | 6.32 | 6.32 |
| 610.65 | 7.08 | 7.08 |
| 592.66 | 6.94 | 6.94 |
| 592.66 | 6.94 | 6.94 |
| 574.67 | 6.80 | 6.80 |
| 570.71 | 7.10 | 7.10 |
| 556.68 | 6.85 | 6.85 |
| 572.73 | 7.18 | 7.18 |
| 590.72 | 7.32 | 7.32 |
| 588.58 | 6.30 | 6.30 |
| 586.75 | 7.42 | 7.42 |
| 544.67 | 6.40 | 6.40 |
| 566.62 | 6.24 | 6.24 |
| 608.64 | 7.66 | 7.66 |
| 615.67 | 6.75 | 6.75 |
| 597.68 | 6.61 | 6.61 |
| 534.45 | 6.49 | 6.49 |
| 534.45 | 6.49 | 6.49 |
| 534.45 | 6.49 | 6.49 |
| 599.65 | 8.41 | 8.41 |
| 599.65 | 8.41 | 8.41 |
| 469.55 | 4.63 | 4.63 |
| 552.44 | 6.63 | 6.63 |
| 542.56 | 5.96 | 5.96 |
| 564.51 | 5.93 | 5.93 |
| 564.51 | 5.93 | 5.93 |
| 546.62 | 6.18 | 6.18 |
| 607.43 | 6.42 | 6.42 |
| 580.10 | 6.35 | 6.35 |
| 546.62 | 6.18 | 6.18 |
| 552.44 | 6.63 | 6.63 |
| 527.67 | 5.75 | 5.75 |
| 599.65 | 8.41 | 8.41 |
| 539.55 | 6.62 | 6.62 |
| 563.65 | 5.99 | 5.99 |
| 623.08 | 8.09 | 8.09 |
| 588.42 | 6.91 | 6.91 |
| 562.11 | 6.40 | 6.40 |
| 574.67 | 6.96 | 6.96 |
| 592.66 | 7.10 | 7.10 |
| 538.69 | 6.72 | 6.72 |
| 560.65 | 6.57 | 6.57 |
| 564.61 | 6.32 | 6.32 |
| 553.58 | 6.93 | 6.93 |
| 578.64 | 6.71 | 6.71 |
| 469.59 | 6.03 | 6.03 |
| 546.52 | 5.79 | 5.79 |
| 618.45 | 7.39 | 7.39 |
| 574.67 | 6.96 | 6.96 |
| 588.70 | 7.24 | 7.24 |
| 476.55 | 5.20 | 5.20 |
| 553.58 | 6.93 | 6.93 |
| 580.97 | 6.45 | 6.45 |
| 542.56 | 5.96 | 5.96 |
| 588.63 | 7.44 | 7.44 |
| 574.00 | 7.28 | 7.28 |
| 562.98 | 6.31 | 6.31 |
| 535.60 | 5.21 | 5.21 |
| 521.44 | 5.37 | 5.37 |
| 565.52 | 5.35 | 5.35 |
| 521.44 | 5.37 | 5.37 |