Literature summary for 2.7.10.2 extracted from

Yogo, T.; Nagamiya, H.; Seto, M.; Sasaki, S.; Shih-Chung, H.; Ohba, Y.; Tokunaga, N.; Lee, G.N.; Rhim, C.Y.; Yoon, C.H.; Cho, S.Y.; Skene, R.; Yamamoto, S.; Satou, Y.; Kuno, M.; Miyazaki, T.; Nakagawa, H.; Okabe, A.; Marui, S.; Aso, K.; Yoshida, M.
Structure-based design and synthesis of 3-amino-1,5-dihydro-4H-pyrazolopyridin-4-one derivatives as tyrosine kinase 2 inhibitors (2016), J. Med. Chem., 59, 733-749 .

Inhibitors

Inhibitors	Comment	Organism
3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one	-	Homo sapiens
3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	-	Homo sapiens
3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one	inhibits IL-23-induced IL-22 production in a rat pharmacodynamic assay, as well as inhibits IL-23 signaling in human peripheral blood mononuclear cell. It shows selectivity for IL-23 signaling inhibition against GMCSF, demonstrating the unique cytokine selectivity	Homo sapiens
baricitinib	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O60674	-	-
Homo sapiens	P23458	-	-
Homo sapiens	P29597	-	-
Homo sapiens	P52333	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
peripheral blood mononuclear cell	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine	-	Homo sapiens	ADP + [Signal Transducer and Activation of Transcription (STAT) protein]-L-tyrosine phosphate	-	?

Synonyms

Synonyms	Comment	Organism
Jak1	-	Homo sapiens
JAK2	-	Homo sapiens
Jak3	-	Homo sapiens
Tyk2	-	Homo sapiens
tyrosine kinase 2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.00000055	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000008	-	37°C, pH not specified in the publication	Homo sapiens	baricitinib
0.00000092	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00000098	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
0.00000099	-	37°C, pH not specified in the publication	Homo sapiens	baricitinib
0.0000012	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000015	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000021	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000023	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000028	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000033	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000046	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
0.0000046	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000053	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000055	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000063	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000064	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000069	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000007	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0000087	-	37°C, pH not specified in the publication	Homo sapiens	baricitinib
0.0000097	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000012	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
0.000012	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000013	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000013	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000014	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000015	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000016	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(morpholin-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000016	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000017	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(2-hydroxypropan-2-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000024	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-[1-methyl-5-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-3-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]-pyridin-4-one
0.000025	-	37°C, pH not specified in the publication	Homo sapiens	baricitinib
0.00003	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000032	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000033	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000052	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000067	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-7-[5-(1,1-dioxidothiomorpholin-4-yl)-1-methyl-1H-pyrazol-3-yl]-5-((2S)-3-methylbutan-2-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00007	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2S)-3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000072	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000079	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000085	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000091	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000091	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.000092	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.0001	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00014	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-((2R)-3-methylbutan-2-yl)-7-[5-(morpholin-4-yl)-pyridin-2-yl]-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00018	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-sec-butyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00023	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00026	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00031	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(3-methylbutan-2-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00039	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-isobutyl-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one
0.00083	-	37°C, pH not specified in the publication	Homo sapiens	3-amino-5-(2-methylpentan-3-yl)-7-(1-methyl-1H-pyrazol-3-yl)-1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-one