Activities

#	Name	Compound Key	Action Type	Relation	Activity Value	Units	Assay ID	Assay Description	Comment	Assay	Assay Organism
1.	ALA4781562	9	Activity	=	28	%	ALA4727289			%	Homo sapiens
2.	(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-naphthalen-2-yl-2-(3-pyridin-3-ylpropanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]buta	8d	EC50	=	1.7	nM	ALA4727286	8.77		nM	Homo sapiens
3.	(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-naphthalen-2-yl-2-(3-pyridin-3-ylpropanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]buta	8d	Intrinsic activity	=	71	%	ALA4727285			%	Homo sapiens
4.	ALA4798983	8; CPN-223	Intrinsic activity	=	75	%	ALA4727280			%	Homo sapiens
5.	ALA4757331	10	Intrinsic activity	=	67	%	ALA4727280			%	Homo sapiens
6.	ALA4757331	10	Activity	=	30	%	ALA4727278			%	Homo sapiens
7.	ALA4798983	8; CPN-223	Activity	=	59	%	ALA4727278			%	Homo sapiens
8.	(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-naphthalen-2-yl-2-(3-pyridin-3-ylpropanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]buta	8d	Activity	=	61	%	ALA4727278			%	Homo sapiens
9.	ALA4752011	7	Activity	=	88	%	ALA4727276			%	Homo sapiens
10.	ALA4094091	5i	Activity	=	88	%	ALA4727276			%	Homo sapiens
11.	ALA4757331	10	EC50	=	30	nM	ALA4727274	7.52		nM	Homo sapiens
12.	ALA4798983	8; CPN-223	EC50	=	3.2	nM	ALA4727274	8.49		nM	Homo sapiens
13.	ALA4781562	9	Activity		0		ALA4727272		Not Active		Homo sapiens
14.	ALA4759601	4	Activity		0		ALA4727272		Not Active		Homo sapiens
15.	Remibrutinib (LOU064)	25; LOU064	Activity		0		ALA4358639		Not Active		Homo sapiens
16.	Belzutifan	2; PT2977	Activity		0		ALA4312524		Not Active		Homo sapiens
17.	Apinocaltamide	66b; ACT-709478	INH	=	56	%	ALA4181796			%	Homo sapiens
18.	ALA4173224	11	Emax	=	99	%	ALA4149977			%	Homo sapiens
19.	ALA4164987	10	Emax	=	127.7	%	ALA4149977			%	Homo sapiens
20.	ALA4171236	9	Emax	=	64	%	ALA4149977			%	Homo sapiens

1.

ALA4781562

9

Activity

=

28

%

ALA4727289

%

Homo sapiens

2.

(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-naphthalen-2-yl-2-(3-pyridin-3-ylpropanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]buta

8d

EC50

=

1.7

nM

ALA4727286

8.77

nM

Homo sapiens

3.

(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-naphthalen-2-yl-2-(3-pyridin-3-ylpropanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]buta

8d

Intrinsic activity

=

71

%

ALA4727285

%

Homo sapiens

4.

ALA4798983

8; CPN-223

Intrinsic activity

=

75

%

ALA4727280

%

Homo sapiens

5.

ALA4757331

10

Intrinsic activity

=

67

%

ALA4727280

%

Homo sapiens

6.

ALA4757331

10

Activity

=

30

%

ALA4727278

%

Homo sapiens

7.

ALA4798983

8; CPN-223

Activity

=

59

%

ALA4727278

%

Homo sapiens

8.

(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-3-naphthalen-2-yl-2-(3-pyridin-3-ylpropanoylamino)propanoyl]amino]-3-phenylpropanoyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]buta

8d

Activity

=

61

%

ALA4727278

%

Homo sapiens

9.

ALA4752011

7

Activity

=

88

%

ALA4727276

%

Homo sapiens

10.

ALA4094091

5i

Activity

=

88

%

ALA4727276

%

Homo sapiens

11.

ALA4757331

10

EC50

=

30

nM

ALA4727274

7.52

nM

Homo sapiens

12.

ALA4798983

8; CPN-223

EC50

=

3.2

nM

ALA4727274

8.49

nM

Homo sapiens

13.

ALA4781562

9

Activity

0

ALA4727272

Not Active

Homo sapiens

14.

ALA4759601

4

Activity

0

ALA4727272

Not Active

Homo sapiens

15.

Remibrutinib (LOU064)

25; LOU064

Activity

0

ALA4358639

Not Active

Homo sapiens

16.

Belzutifan

2; PT2977

Activity

0

ALA4312524

Not Active

Homo sapiens

17.

Apinocaltamide

66b; ACT-709478

INH

=

56

%

ALA4181796

%

Homo sapiens

18.

ALA4173224

11

Emax

=

99

%

ALA4149977

%

Homo sapiens

19.

ALA4164987

10

Emax

=

127.7

%

ALA4149977

%

Homo sapiens

20.

ALA4171236

9

Emax

=

64

%

ALA4149977

%

Homo sapiens