Activities

#	Name	Compound Key	Action Type	Relation	Activity Value	Units	Assay ID	Assay Description	Comment	Assay
1.	ALA4456642	rac-9c	Activity	=	3.5	%	ALA4429064			%
2.	ALA4456642	rac-9c	Activity		0		ALA4429065		Active
3.	4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide	13g; GNF2133	Efficacy	=	95	%	ALA4604977			%
4.	ALA4640031	13f	Efficacy	=	100	%	ALA4604977			%
5.	4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide	13g; GNF2133	Efficacy	=	110	%	ALA4604976			%
6.	ALA4640031	13f	Efficacy	=	99	%	ALA4604976			%
7.	4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide	13g; GNF2133	EC50	=	0.21	uM	ALA4604975	6.68		nM
8.	ALA4640031	13f	EC50	=	0.12	uM	ALA4604975	6.92		nM
9.	4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide	13g; GNF2133	EC50	=	0.4	uM	ALA4604974	6.40		nM
10.	ALA4640031	13f	EC50	=	0.64	uM	ALA4604974	6.19		nM
11.	(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid	GNF4877	Efficacy	=	263	%	ALA4604966			%
12.	ALA4638292	GNF7156	Efficacy	=	100	%	ALA4604966			%
13.	(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid	GNF4877	Efficacy	=	162	%	ALA4604965			%
14.	ALA4638292	GNF7156	Efficacy	=	100	%	ALA4604965			%
15.	(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid	GNF4877	EC50	=	0.54	uM	ALA4604964	6.27		nM
16.	ALA4638292	GNF7156	EC50	=	0.76	uM	ALA4604964	6.12		nM
17.	(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid	GNF4877	EC50	=	0.19	uM	ALA4604963	6.72		nM
18.	ALA4638292	GNF7156	EC50	=	3.5	uM	ALA4604963	5.46		nM
19.	5-Iodotubercidin	1s	Efficacy	=	56	%	ALA4604960			%
20.	5-Iodotubercidin	1s	EC50	=	0.31	uM	ALA4604959	6.51		nM

1.

ALA4456642

rac-9c

Activity

=

3.5

%

ALA4429064

%

2.

ALA4456642

rac-9c

Activity

0

ALA4429065

Active

3.

4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide

13g; GNF2133

Efficacy

=

95

%

ALA4604977

%

4.

ALA4640031

13f

Efficacy

=

100

%

ALA4604977

%

5.

4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide

13g; GNF2133

Efficacy

=

110

%

ALA4604976

%

6.

ALA4640031

13f

Efficacy

=

99

%

ALA4604976

%

7.

4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide

13g; GNF2133

EC50

=

0.21

uM

ALA4604975

6.68

nM

8.

ALA4640031

13f

EC50

=

0.12

uM

ALA4604975

6.92

nM

9.

4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide

13g; GNF2133

EC50

=

0.4

uM

ALA4604974

6.40

nM

10.

ALA4640031

13f

EC50

=

0.64

uM

ALA4604974

6.19

nM

11.

(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid

GNF4877

Efficacy

=

263

%

ALA4604966

%

12.

ALA4638292

GNF7156

Efficacy

=

100

%

ALA4604966

%

13.

(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid

GNF4877

Efficacy

=

162

%

ALA4604965

%

14.

ALA4638292

GNF7156

Efficacy

=

100

%

ALA4604965

%

15.

(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid

GNF4877

EC50

=

0.54

uM

ALA4604964

6.27

nM

16.

ALA4638292

GNF7156

EC50

=

0.76

uM

ALA4604964

6.12

nM

17.

(3R)-1-[3-[[3-amino-6-(2-fluoro-5-propan-2-yloxyphenyl)pyrazine-2-carbonyl]amino]pyridin-4-yl]piperidine-3-carboxylic acid

GNF4877

EC50

=

0.19

uM

ALA4604963

6.72

nM

18.

ALA4638292

GNF7156

EC50

=

3.5

uM

ALA4604963

5.46

nM

19.

5-Iodotubercidin

1s

Efficacy

=

56

%

ALA4604960

%

20.

5-Iodotubercidin

1s

EC50

=

0.31

uM

ALA4604959

6.51

nM