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2.1.2.2: phosphoribosylglycinamide formyltransferase 1

This is an abbreviated version!
For detailed information about phosphoribosylglycinamide formyltransferase 1, go to the full flat file.

Word Map on EC 2.1.2.2

Reaction

10-formyltetrahydrofolate
+
N1-(5-phospho-D-ribosyl)glycinamide
=
tetrahydrofolate
 +
N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide

Synonyms

2-amino-N-ribosylacetamide 5'-phosphate (glycinamide ribotide) transformylase, 2-amino-N-ribosylacetamide 5'-phosphate transformylase, 5'-phosphoribosylglycinamide transformylase, 5,10-methenyltetrahydrofolate:2-amino-N-ribosylacetamide ribonucleotide transformylase, ADE8, GAR formyltransferase, GAR synthetase, GAR TFase, GAR transformylase, GARFT, GARFTase, GART, GART synthetase, GARTfase, glycinamide ribonucleotide formyl transferase, glycinamide ribonucleotide formyltransferase, glycinamide ribonucleotide transformylase, glycinamide ribotide formyltransferase, N10-formyltetrahydrolate:2-amino-N-ribosylacetamide-5'-phosphate transformylase, phosphoribosylglycinamide formyltransferase, PurN, purN transformylase, trifunctional purine biosynthetic protein adenosine-3

ECTree

     2 Transferases
         2.1 Transferring one-carbon groups
             2.1.2 Hydroxymethyl-, formyl- and related transferases
                2.1.2.2 phosphoribosylglycinamide formyltransferase 1

KI Value

KI Value on EC 2.1.2.2 - phosphoribosylglycinamide formyltransferase 1

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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00021
(S)-2-(((4R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylthio)butyl)benzamido)pentanedioic acid
-
-
0.0014
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl)benzamido)pentanedioic acid
-
-
0.0012
(S)-2-(4((S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl)benzamido)pentanedioic acid
-
-
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
-
-
0.000015
10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
-
0.000015 - 0.00003
10-CF3CO-DDACTHF
0.000014
10-formyl-DDACTHF
0.00058
10-methanesulfonyl-5-DACTHF
-
26°C, pH 7.5
0.00023
10-methanesulfonyl-DDACTHF
-
26°C, pH 7.5
0.00025
10-methylthio-DDACTHF
0.000015 - 0.0019
10-trifluoroacetyl-DDACTHF
0.0067
2,4-diamino-6-(3,4,5-trimethoxyanilino)-methylpyrido[3,2-d]pyrimidine
pH and temperature not specified in the publication
0.02754
2,4-diamino-6-(3,4,5-trimethoxybenzyl)-5,6,7,8-tetrahydro-quinazoline
pH and temperature not specified in the publication
0.000056
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
26°C, pH 7.5
0.0048
4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid
-
26°C, pH 7.5
0.04218
5-((4-carboxy-4-(4-(((2,4-diaminopyrido[3,2-d]pyrimidine-6-yl)methyl)amino)benzamido)butyl)carbamoyl)-isophthalic acid
pH and temperature not specified in the publication
0.0017 - 0.005
DDACTHF
0.0093
LY231514 monoglutamate
-
-
0.000065
LY231514 pentaglutamate
-
-
0.0011
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-hydroxybutyl]phenyl]carbonyl)glutamic acid
-
-
0.00085
N-([4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methoxybutyl]phenyl]carbonyl)glutamic acid
-
-
0.00018
N-([4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]phenyl]carbonyl)glutamic acid
-
-
0.000005 - 0.00005
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]-4-methylthiophen-2-yl)carbonyl]glutamic acid
pH and temperature not specified in the publication
0.000005 - 0.00005
N-[(5-[2-[(6R)-2-amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
pH and temperature not specified in the publication
0.000005 - 0.00005
N-[(5-[2-[(6S)-2-amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimido[5,4-b][1,4]thiazin-6-yl]ethyl]thiophen-2-yl)carbonyl]glutamic acid
pH and temperature not specified in the publication
0.00021
N-[4-[(1R)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
pH and temperature not specified in the publication
0.00018
N-[4-[(1S)-4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(methylsulfanyl)butyl]benzoyl]glutamic acid
pH and temperature not specified in the publication
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
-
-
0.001067
N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
at pH 7.5 and 37°C
0.000017
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
at pH 7.5 and 37°C
0.000007 - 0.000009
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
0.0005
N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid
-
26°C, pH 7.5
0.000068
N-[5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]-L-glutamic acid
-
at pH 7.5 and 37°C
0.000022
N-[5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophene-2-carbonyl]-L-glutamic acid
-
at pH 7.5 and 37°C
0.000067
N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-D-glutamic acid
-
at pH 7.5 and 37°C
0.000099
N-[8-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)octanoyl]-D-glutamic acid
-
at pH 7.5 and 37°C
additional information
additional information
-
4-carbamoyl-2-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid and 4-carbamoyl-4-[4-[4-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-1-(2,2,2-trifluoroacetyl)butyl]benzoylamino]butyric acid show Ki-values above 0.1 mM
-