Activities

#	Name	Compound Key	Action Type	Relation	Activity Value	Units	Assay ID	Assay Description	Comment	Assay	Assay Organism
1.	ALA5196874	(-)-53; MU1656	Activity		0		ALA5161994		NA		Homo sapiens
2.	ALA3979678	BDBM238766	TGI	=	95	%	ALA4478515			%	Homo sapiens
3.	ALA3979678	BDBM238766	TGI	=	93	%	ALA4478514			%	Homo sapiens
4.	ALA4587596	1	TGI	=	78	%	ALA4478514			%	Homo sapiens
5.	ALA3979678	BDBM238766	TGI	=	65	%	ALA4478513			%	Homo sapiens
6.	ALA3979678	BDBM238766	TGI	=	30	%	ALA4478512			%	Homo sapiens
7.	ALA3979678	BDBM238766	TGI		0		ALA4478511		Dose-dependent effect		Homo sapiens
8.	ALA3979678	BDBM238766	IC50	=	260	nM	ALA4478510	6.58		nM	Homo sapiens
9.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	EC50	=	0.015	uM	ALA4370179	7.82		nM	Homo sapiens
10.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	ED50	=	12	mg kg-1	ALA4370179			mg.kg-1	Homo sapiens
11.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	Activity	=	33	%	ALA4370183			%	Homo sapiens
12.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	TGI	=	100	%	ALA4370182			%	Homo sapiens
13.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	TGI	=	84	%	ALA4370181			%	Homo sapiens
14.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	TGI	=	38	%	ALA4370180			%	Homo sapiens
15.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	TGI		0		ALA4370179		Dose-dependent effect		Homo sapiens
16.	3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	28	IC50	=	0.049	uM	ALA4370174	7.31		nM	Homo sapiens
17.	ALA3979678	BDBM238766	IC50	=	0.26	uM	ALA4370174	6.58		nM	Homo sapiens
18.	Vorinostat (SAHA, MK0683)	SAHA	Activity		0		ALA4315215		Active		Homo sapiens
19.	Vorinostat (SAHA, MK0683)	SAHA	EC50	=	0.94	uM	ALA4315189	6.03		nM	Homo sapiens
20.	ALA4554522	24c	EC50	=	7.6	uM	ALA4315189	5.12		nM	Homo sapiens

1.

ALA5196874

(-)-53; MU1656

Activity

0

ALA5161994

NA

Homo sapiens

2.

ALA3979678

BDBM238766

TGI

=

95

%

ALA4478515

%

Homo sapiens

3.

ALA3979678

BDBM238766

TGI

=

93

%

ALA4478514

%

Homo sapiens

4.

ALA4587596

1

TGI

=

78

%

ALA4478514

%

Homo sapiens

5.

ALA3979678

BDBM238766

TGI

=

65

%

ALA4478513

%

Homo sapiens

6.

ALA3979678

BDBM238766

TGI

=

30

%

ALA4478512

%

Homo sapiens

7.

ALA3979678

BDBM238766

TGI

0

ALA4478511

Dose-dependent effect

Homo sapiens

8.

ALA3979678

BDBM238766

IC50

=

260

nM

ALA4478510

6.58

nM

Homo sapiens

9.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

EC50

=

0.015

uM

ALA4370179

7.82

nM

Homo sapiens

10.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

ED50

=

12

mg kg-1

ALA4370179

mg.kg-1

Homo sapiens

11.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

Activity

=

33

%

ALA4370183

%

Homo sapiens

12.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

TGI

=

100

%

ALA4370182

%

Homo sapiens

13.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

TGI

=

84

%

ALA4370181

%

Homo sapiens

14.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

TGI

=

38

%

ALA4370180

%

Homo sapiens

15.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

TGI

0

ALA4370179

Dose-dependent effect

Homo sapiens

16.

3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6~{R})-6-methyl-4-oxo-5,6-dihydro-1~{H}-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one

28

IC50

=

0.049

uM

ALA4370174

7.31

nM

Homo sapiens

17.

ALA3979678

BDBM238766

IC50

=

0.26

uM

ALA4370174

6.58

nM

Homo sapiens

18.

Vorinostat (SAHA, MK0683)

SAHA

Activity

0

ALA4315215

Active

Homo sapiens

19.

Vorinostat (SAHA, MK0683)

SAHA

EC50

=

0.94

uM

ALA4315189

6.03

nM

Homo sapiens

20.

ALA4554522

24c

EC50

=

7.6

uM

ALA4315189

5.12

nM

Homo sapiens