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Literature summary for 2.1.2.2 extracted from

  • DeMartino, J.K.; Hwang, I.; Connelly, S.; Wilson, I.A.; Boger, D.L.
    Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase (2008), J. Med. Chem., 51, 5441-5448.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine glycinamide ribonucleotide transformylase has emerged as a productive target for antineoplastic therapeutic intervention Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
-
Homo sapiens
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
-
Homo sapiens
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
-
Homo sapiens
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
-
Homo sapiens
10-CF3CO-DDACTHF
-
Homo sapiens
10-formyl-DDACTHF
-
Homo sapiens
10-methylthio-DDACTHF
-
Homo sapiens
5,10-dideaza-5,6,7,8-tetrahydrofolic acid
-
Homo sapiens
AG2034
-
Homo sapiens
AG2037
-
Homo sapiens
DDACTHF
-
Homo sapiens
LY309887
-
Homo sapiens
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
-
Homo sapiens
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
-
Homo sapiens
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
-
Homo sapiens
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
CCRF-CEM cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
-
Homo sapiens tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
?

Synonyms

Synonyms Comment Organism
GAR TFase
-
Homo sapiens
glycinamide ribonucleotide transformylase
-
Homo sapiens
phosphoribosylglycinamide formyltransferase
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
folate
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000014
-
10-formyl-DDACTHF
-
Homo sapiens
0.000015
-
10-CF3CO-DDACTHF
-
Homo sapiens
0.00003
-
10-CF3CO-DDACTHF
-
Homo sapiens
0.00006
-
N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
-
Homo sapiens
0.00018
-
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
-
Homo sapiens
0.00021
-
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
-
Homo sapiens
0.00025
-
10-methylthio-DDACTHF
-
Homo sapiens
0.00085
-
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
-
Homo sapiens
0.0011
-
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
-
Homo sapiens
0.0011
-
(S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
-
Homo sapiens
0.0012
-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
-
Homo sapiens
0.0014
-
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
-
Homo sapiens
0.0017
-
DDACTHF
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000016
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens 10-CF3CO-DDACTHF
0.000017
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens 10-CF3CO-DDACTHF
0.00005
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.00006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens 10-CF3CO-DDACTHF
0.00006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.00006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.00007
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.00007
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.00008
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.00008
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.00009
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.0002
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.0002
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.0002
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.0005
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.0005
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.0006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.0006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.0006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.0006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.0006
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.0007
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.0007
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.0008
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.0009
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.0009
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.0024
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.0027
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens DDACTHF
0.0027
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens DDACTHF
0.0036
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens DDACTHF
0.0044
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.005
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.0055
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.0055
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.0057
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.006
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.01
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens DDACTHF
0.01
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.01
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens 10-CF3CO-DDACTHF
0.01
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.01
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.01
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/FPGS- cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens DDACTHF
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens 10-CF3CO-DDACTHF
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens (S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens (S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
0.01
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the presence of hypoxanthine Homo sapiens (S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
0.1
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
0.1
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens DDACTHF
0.1
-
in vitro cytotoxic activity in mutant cell line, CCRF-CEM/MTX cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid
0.1
-
in vitro cytotoxic activity, CCRF-CEM cell, in the absence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid
0.1
-
in vitro cytotoxic activity, CCRF-CEM cell, in the presence of thymidine, in the absence of hypoxanthine Homo sapiens (S)-2-(4-(2-(3-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)propyl)-1,3-dithian-2-yl)benzamido)pentanedioic acid