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
Bioactivity
Activity Types for Assay ALA3887092
IC50
Parent Molecular Weight | ALogP | Polar Surface Area |
---|---|---|
610.67 | 2.09 | 2.09 |
664.63 | 2.68 | 2.68 |
565.03 | 1.73 | 1.73 |
528.59 | 0.86 | 0.86 |
556.65 | 1.34 | 1.34 |
612.66 | 2.56 | 2.56 |
584.60 | 1.83 | 1.83 |
576.70 | 1.79 | 1.79 |
598.63 | 2.17 | 2.17 |
526.62 | 1.42 | 1.42 |
588.71 | 1.79 | 1.79 |
596.59 | 2.06 | 2.06 |
560.66 | 1.46 | 1.46 |
621.18 | 3.36 | 3.36 |
547.04 | 1.81 | 1.81 |
555.64 | 1.32 | 1.32 |
570.67 | 1.65 | 1.65 |
638.72 | 2.57 | 2.57 |
650.61 | 2.59 | 2.59 |
574.69 | 1.85 | 1.85 |
548.65 | 1.31 | 1.31 |
610.62 | 2.15 | 2.15 |
624.69 | 2.18 | 2.18 |
547.04 | 1.59 | 1.59 |
572.59 | 1.93 | 1.93 |
565.08 | 2.10 | 2.10 |
588.59 | 1.81 | 1.81 |
518.62 | 1.22 | 1.22 |
579.10 | 2.49 | 2.49 |
532.65 | 1.48 | 1.48 |
598.63 | 2.47 | 2.47 |
569.67 | 1.41 | 1.41 |
580.59 | 1.96 | 1.96 |
631.03 | 2.49 | 2.49 |
551.00 | 1.65 | 1.65 |
650.73 | 2.57 | 2.57 |
539.04 | 1.57 | 1.57 |
596.59 | 1.84 | 1.84 |
588.71 | 1.94 | 1.94 |
542.59 | 1.53 | 1.53 |
556.62 | 1.61 | 1.61 |
567.46 | 2.16 | 2.16 |
578.67 | 0.94 | 0.94 |
530.58 | 1.30 | 1.30 |
634.61 | 2.71 | 2.71 |
593.13 | 2.58 | 2.58 |
530.58 | 1.08 | 1.08 |
514.56 | 0.56 | 0.56 |
516.56 | 0.99 | 0.99 |
628.65 | 2.44 | 2.44 |
522.58 | 1.05 | 1.05 |
614.63 | 2.35 | 2.35 |
582.56 | 1.75 | 1.75 |
586.62 | 2.02 | 2.02 |
566.56 | 1.87 | 1.87 |
548.62 | 1.59 | 1.59 |
584.60 | 2.08 | 2.08 |
558.69 | 2.01 | 2.01 |
602.74 | 2.32 | 2.32 |
544.66 | 1.76 | 1.76 |
551.05 | 1.71 | 1.71 |
615.08 | 2.44 | 2.44 |
563.04 | 1.52 | 1.52 |
534.62 | 0.92 | 0.92 |
581.48 | 2.25 | 2.25 |
617.01 | 2.41 | 2.41 |
601.06 | 2.35 | 2.35 |
600.60 | 1.96 | 1.96 |
602.62 | 1.90 | 1.90 |
579.10 | 2.19 | 2.19 |
602.74 | 2.18 | 2.18 |
552.66 | 1.95 | 1.95 |
596.64 | 1.70 | 1.70 |
606.73 | 1.42 | 1.42 |
542.62 | 1.17 | 1.17 |
565.08 | 1.80 | 1.80 |
590.73 | 2.04 | 2.04 |
614.75 | 2.33 | 2.33 |
553.07 | 1.66 | 1.66 |
522.58 | 1.05 | 1.05 |
562.67 | 1.40 | 1.40 |
614.63 | 2.05 | 2.05 |
533.01 | 1.51 | 1.51 |
578.65 | 1.41 | 1.41 |