Assay Report Card

Basic Information

ID: ALA3705870

Type: Binding

Description: Fluorometric Plate Assay: To determine the efficacy of various synthesized PAI-1 inhibitor compounds, a fluorometric plate assay was carried out to measure the half maximal inhibitory concentration (IC50) of these compounds on recombinant active human PAI-1 in vitro. An IC50 is a measure of the effectiveness of a compound in inhibiting biological or biochemical function. Stated another way, IC50 represents the concentration of a drug that is required for 50% inhibition in vitro. The IC50 of various compounds was measured using a fluorometric plate assay as set out below, and the results are shown in Table 3.Recombinant active human PAI-1 (Molecular Innovations) (final 1 nM) was incubated for 15 min at 23 C. with increasing concentrations of each compound in 100 mM NaCl, 40 mM HEPES, 0.005% Tween-20, 10% DMSO, pH 7.8. Alternately, the assay has been carried out using low concentrations of DMSO (about 0.1% DMSO or less) in the buffer. In various aspects, the invention does not require a solvent, like DMSO.

Organism: Homo sapiens

Activity Charts

Bioactivity

Activity Types for Assay ALA3705870

IC50

Total(37)

Compound Summary

Parent Molecular Weight	ALogP	Polar Surface Area
364.31	0.08	0.08
378.34	0.47	0.47
940.68	1.69	1.69
940.68	1.69	1.69
940.68	1.69	1.69
404.42	-0.23	-0.23
460.53	1.23	1.23
414.32	2.36	2.36
940.68	1.69	1.69
366.28	0.93	0.93
420.37	2.25	2.25
420.37	2.25	2.25
410.33	0.95	0.95
454.38	0.97	0.97
498.44	0.98	0.98
380.31	1.32	1.32
326.31	1.82	1.82
334.28	1.52	1.52
390.31	1.07	1.07
448.47	1.98	1.98
422.39	2.15	2.15
390.35	0.52	0.52
446.46	1.73	1.73
420.37	2.25	2.25
420.37	2.25	2.25
420.37	2.25	2.25
420.37	2.25	2.25
376.37	-0.32	-0.32
404.42	0.37	0.37
344.37	0.27	0.27
430.46	0.90	0.90
606.49	3.37	3.37
534.48	2.16	2.16
408.36	1.96	1.96
495.44	1.83	1.83
562.53	2.64	2.64
940.68	1.69	1.69