Assay Report Card

Basic Information

ID: ALA3706092

Type: Binding

Description: Biochemical Assay: Compounds of the present invention were evaluated for potency against PI3-Kα using an in vitro kinase assay. PI3-Kα activity is measured in vitro by determining the level of phosphorylation of the substrate PI(4,5)P2. The formation of product PI(3,4,5)P3 is monitored by binding to the Grip1 PH domain in a ligand displacement fluorescence polarization (FP) assay, in which the TAMRA-labeled PI(3,4,5)P3 complexed with Grip1 PH domain is displaced by PI(3,4,5)P3 formed in the PI3-Kα reaction resulting in a decrease in FP signal.

Organism: Homo sapiens

Activity Charts

Bioactivity

Activity Types for Assay ALA3706092

IC50

Total(174)

Compound Summary

Parent Molecular Weight	ALogP	Polar Surface Area
425.49	2.25	2.25
325.37	2.33	2.33
354.41	2.20	2.20
351.41	2.87	2.87
337.38	2.48	2.48
296.33	1.80	1.80
323.36	2.09	2.09
282.31	1.41	1.41
284.32	1.65	1.65
352.40	1.48	1.48
370.39	1.62	1.62
458.52	2.88	2.88
411.47	1.07	1.07
397.44	1.06	1.06
439.48	1.13	1.13
456.48	1.88	1.88
438.49	1.74	1.74
458.52	2.88	2.88
411.47	1.07	1.07
439.48	1.13	1.13
397.44	1.06	1.06
456.48	1.88	1.88
438.49	1.74	1.74
365.44	3.33	3.33
381.44	2.23	2.23
367.41	2.10	2.10
353.38	1.71	1.71
337.39	1.84	1.84
424.51	2.02	2.02
380.45	3.64	3.64
337.38	2.40	2.40
355.83	3.51	3.51
374.45	3.80	3.80
343.43	2.06	2.06
409.49	2.94	2.94
324.39	2.65	2.65
336.40	2.44	2.44
351.41	2.87	2.87
360.42	3.34	3.34
365.44	3.33	3.33
364.45	3.29	3.29
353.40	3.46	3.46
388.48	4.19	4.19
394.48	4.03	4.03
366.42	3.18	3.18
369.86	3.97	3.97
379.46	3.72	3.72
406.49	4.10	4.10
378.48	4.32	4.32
364.45	3.93	3.93
364.45	4.02	4.02
350.42	3.47	3.47
350.42	3.63	3.63
354.41	1.56	1.56
367.41	1.84	1.84
340.39	1.55	1.55
353.22	1.92	1.92
390.45	2.70	2.70
367.41	1.84	1.84
339.19	1.53	1.53
340.39	1.17	1.17
326.36	1.16	1.16
376.42	2.31	2.31
340.39	1.17	1.17
376.42	2.31	2.31
326.36	1.16	1.16
327.18	1.22	1.22
353.22	1.92	1.92
355.40	1.52	1.52
342.37	2.26	2.26
390.45	2.70	2.70
364.41	2.00	2.00
375.43	2.67	2.67
379.42	2.44	2.44
338.37	1.76	1.76
399.43	2.37	2.37
367.25	2.57	2.57
413.45	3.02	3.02
394.48	2.29	2.29
408.51	2.94	2.94
354.41	2.20	2.20
351.20	2.13	2.13
354.41	1.94	1.94
409.49	3.01	3.01
395.46	2.62	2.62
376.42	2.09	2.09
399.43	2.37	2.37
394.48	2.29	2.29
324.27	1.63	1.63
365.32	2.32	2.32
326.36	1.42	1.42
376.42	2.58	2.58
325.17	1.41	1.41
312.33	1.03	1.03
346.39	2.95	2.95
334.38	2.81	2.81
332.37	2.56	2.56
353.22	1.94	1.94
340.39	1.57	1.57
381.44	2.25	2.25
390.45	2.72	2.72
339.19	1.48	1.48
326.36	1.11	1.11
367.41	1.79	1.79
376.42	2.26	2.26
339.19	1.62	1.62
326.36	1.25	1.25
367.41	1.93	1.93
376.42	2.40	2.40
397.44	1.86	1.86
438.49	2.54	2.54
447.50	3.02	3.02
337.39	1.84	1.84
355.83	3.51	3.51
365.44	3.01	3.01
351.41	2.55	2.55
338.42	2.66	2.66
324.39	2.20	2.20
388.42	3.39	3.39
374.39	2.93	2.93
326.36	0.71	0.71
340.39	1.17	1.17
382.47	2.43	2.43
339.40	2.41	2.41
381.44	2.18	2.18
399.43	2.27	2.27
357.39	2.50	2.50
338.42	2.96	2.96
452.52	2.93	2.93
420.52	2.82	2.82
369.40	3.01	3.01
352.40	2.26	2.26
348.45	4.03	4.03
378.48	3.23	3.23
390.49	3.46	3.46
368.40	1.50	1.50
366.42	2.19	2.19
408.46	2.60	2.60
368.41	3.61	3.61
385.40	2.24	2.24
326.36	1.73	1.73
312.33	1.01	1.01
401.47	3.37	3.37
382.42	1.62	1.62
382.42	1.62	1.62
395.46	2.69	2.69
427.48	3.22	3.22
410.48	2.47	2.47
411.47	1.63	1.63
327.35	1.24	1.24
355.40	1.73	1.73
409.49	2.40	2.40
378.44	2.90	2.90
368.40	2.50	2.50
426.48	1.64	1.64
443.48	2.38	2.38
445.52	3.39	3.39
384.44	1.56	1.56
397.27	1.94	1.94
438.53	2.30	2.30
426.48	1.64	1.64
443.48	2.38	2.38
445.52	3.39	3.39
384.44	1.56	1.56
455.52	1.61	1.61
384.44	1.56	1.56
398.47	1.58	1.58
397.44	1.47	1.47
415.43	1.60	1.60
398.42	0.86	0.86
410.43	0.96	0.96
428.42	1.10	1.10
411.42	0.35	0.35