Inhibition Assay: The compounds according to the invention are tested in a range of concentrations (10pM to 10 µM final) in assay buffer (50 mM TRIS, ...

Basic Information

ID: ALA3887092

Type: Binding

Description: Inhibition Assay: The compounds according to the invention are tested in a range of concentrations (10pM to 10 µM final) in assay buffer (50 mM TRIS, 100 mM NaCl, 0.1 % BSA, pH 7,5) with 0.1% maximal final DMSO concentration and deposited in a proportion of 25 µl per well, on 25 µL enzyme (human coagulation factor Xa: Enzyme Research Laboratories HFXa, final concentration 0.003Ul/ml). The reactive were mixed, centrifuged and incubated 10 minutes at 37°C in a 96 well microtiter plate. The enzyme reaction was started with 50 µL substrate (S-2765, Biogenic ref 821413 in a final concentration of 62.5µM final). The time course of the reaction was monitored at 405 nm in a microtiter plate reader (Tecan M200) for 20 minutes at 37°C. The percentage of inhibition of enzymatic activity (expressed as maximum rate of cleavage of the substrate) is calculated with respect to the enzymatic activity in the absence of inhibitor.

Format: BAO_0000357

Organism: Homo sapiens

Target:  Coagulation factor X(ALA244)

Document:  ALA3886162

BindingDB Source:  7241

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
610.672.092.09
664.632.682.68
565.031.731.73
528.590.860.86
556.651.341.34
612.662.562.56
584.601.831.83
576.701.791.79
598.632.172.17
526.621.421.42
588.711.791.79
596.592.062.06
560.661.461.46
621.183.363.36
547.041.811.81
555.641.321.32
570.671.651.65
638.722.572.57
650.612.592.59
574.691.851.85
548.651.311.31
610.622.152.15
624.692.182.18
547.041.591.59
572.591.931.93
565.082.102.10
588.591.811.81
518.621.221.22
579.102.492.49
532.651.481.48
598.632.472.47
569.671.411.41
580.591.961.96
631.032.492.49
551.001.651.65
650.732.572.57
539.041.571.57
596.591.841.84
588.711.941.94
542.591.531.53
556.621.611.61
567.462.162.16
578.670.940.94
530.581.301.30
634.612.712.71
593.132.582.58
530.581.081.08
514.560.560.56
516.560.990.99
628.652.442.44
522.581.051.05
614.632.352.35
582.561.751.75
586.622.022.02
566.561.871.87
548.621.591.59
584.602.082.08
558.692.012.01
602.742.322.32
544.661.761.76
551.051.711.71
615.082.442.44
563.041.521.52
534.620.920.92
581.482.252.25
617.012.412.41
601.062.352.35
600.601.961.96
602.621.901.90
579.102.192.19
602.742.182.18
552.661.951.95
596.641.701.70
606.731.421.42
542.621.171.17
565.081.801.80
590.732.042.04
614.752.332.33
553.071.661.66
522.581.051.05
562.671.401.40
614.632.052.05
533.011.511.51
578.651.411.41