Activities

#	Name	Compound Key	Action Type	Relation	Activity Value	Units	Assay ID	Assay Description	Comment	Assay	Assay Organism
1.	N-tert-Butyl-α-phenylnitrone	1	Activity	=	26	%	ALA4420260			%	Papio
2.	ALA2165204	3, [11C]R121920	Stability	=	50	%	ALA2350911			%	Papio
3.	ALA2349557	6, [11C]DMP696	Stability	=	50	%	ALA2350911			%	Papio
4.	ALA2165204	3, [11C]R121920	Stability	=	50	%	ALA2350910			%	Papio
5.	ALA2349557	6, [11C]DMP696	Stability	=	50	%	ALA2350910			%	Papio
6.	ALA426317	5	Activity		0		ALA861221		Active		Papio
7.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Emax	=	99	%	ALA865440			%	Papio
8.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	ED50	=	0.06	mg Kg-1	ALA865440			mg.kg-1	Papio
9.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	EC50	=	0.17	uM	ALA865440	6.77		nM	Papio
10.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Inhibition	=	86	%	ALA869589			%	Papio
11.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Inhibition	=	64	%	ALA868413			%	Papio
12.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Inhibition	=	20	%	ALA868412			%	Papio
13.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Inhibition	=	87	%	ALA869583			%	Papio
14.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Inhibition	=	61	%	ALA869582			%	Papio
15.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Inhibition	=	14	%	ALA869581			%	Papio
16.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	MRT	=	232	min	ALA869580			hr	Papio
17.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	Vdss	=	5854	ml	ALA869579			ml	Papio
18.	2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid	9	CL	=	26.5	ml/min	ALA869578			ml/min	Papio
19.	ALA204871	[11C]NMI-EPB	PPB	=	40	%	ALA871174			%	Papio
20.	ALA332322	29	Plasma concentration	=	0.7	uM	ALA629839			uM	Papio

1.

N-tert-Butyl-α-phenylnitrone

1

Activity

=

26

%

ALA4420260

%

Papio

2.

ALA2165204

3, [11C]R121920

Stability

=

50

%

ALA2350911

%

Papio

3.

ALA2349557

6, [11C]DMP696

Stability

=

50

%

ALA2350911

%

Papio

4.

ALA2165204

3, [11C]R121920

Stability

=

50

%

ALA2350910

%

Papio

5.

ALA2349557

6, [11C]DMP696

Stability

=

50

%

ALA2350910

%

Papio

6.

ALA426317

5

Activity

0

ALA861221

Active

Papio

7.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Emax

=

99

%

ALA865440

%

Papio

8.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

ED50

=

0.06

mg Kg-1

ALA865440

mg.kg-1

Papio

9.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

EC50

=

0.17

uM

ALA865440

6.77

nM

Papio

10.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Inhibition

=

86

%

ALA869589

%

Papio

11.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Inhibition

=

64

%

ALA868413

%

Papio

12.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Inhibition

=

20

%

ALA868412

%

Papio

13.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Inhibition

=

87

%

ALA869583

%

Papio

14.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Inhibition

=

61

%

ALA869582

%

Papio

15.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Inhibition

=

14

%

ALA869581

%

Papio

16.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

MRT

=

232

min

ALA869580

hr

Papio

17.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

Vdss

=

5854

ml

ALA869579

ml

Papio

18.

2-[3-(5-carbamimidoyl-2,3-dihydro-1H-1,3-benzodiazol-2-ylidene)-5-{5-[(carbamoylamino)methyl]-2-hydroxyphenyl}-4-oxocyclohexa-1,5-dien-1-yl]butanedioic acid

9

CL

=

26.5

ml/min

ALA869578

ml/min

Papio

19.

ALA204871

[11C]NMI-EPB

PPB

=

40

%

ALA871174

%

Papio

20.

ALA332322

29

Plasma concentration

=

0.7

uM

ALA629839

uM

Papio