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Literature summary extracted from

  • Deng, Y.; Wang, Y.; Cherian, C.; Hou, Z.; Buck, S.A.; Matherly, L.H.; Gangjee, A.
    Synthesis and discovery of high affinity folate receptor-specific glycinamide ribonucleotide formyltransferase inhibitors with antitumor activity (2008), J. Med. Chem., 51, 5052-5063.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.2.2 N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
-
 Homo sapiens
2.1.2.2 N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
-
 Mus musculus
2.1.2.2 N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
-
 Homo sapiens
2.1.2.2 N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
-
 Mus musculus
2.1.2.2 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
2.1.2.2 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
-
 Mus musculus
2.1.2.2 N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
 Mus musculus
2.1.2.2 N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
-
 Mus musculus
2.1.2.2 N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
-
 Mus musculus
2.1.2.2 N-{4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl}-L-glutamic acid
-
 Homo sapiens
2.1.2.2 N-{4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl}-L-glutamic acid
-
 Homo sapiens
2.1.2.2 N-{4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl}-L-glutamic acid
-
 Homo sapiens
2.1.2.2 pemetrexed
-
 Homo sapiens
2.1.2.2 pemetrexed
-
 Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
2.1.2.2 Homo sapiens
-
-
-
2.1.2.2 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.2.2 KB cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.2.2 10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
-
 Mus musculus tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
 ?
2.1.2.2 10-formyltetrahydrofolate + N1-(5-phospho-D-ribosyl)glycinamide
-
 Homo sapiens tetrahydrofolate + N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.2.2 GARFTase
-
 Mus musculus
2.1.2.2 GARFTase
-
 Homo sapiens
2.1.2.2 glycinamide ribonucleotide formyltransferase
-
 Mus musculus
2.1.2.2 glycinamide ribonucleotide formyltransferase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.1.2.2 37
-
 in situ GARFT enzyme inhibition assay Homo sapiens
2.1.2.2 37
-
 in vitro GARFT enzyme inhibition assay Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.1.2.2 7.5
-
 in vitro GARFT enzyme inhibition assay Mus musculus

Cofactor

EC Number Cofactor Comment Organism Structure
2.1.2.2 folate
-
 Mus musculus
2.1.2.2 folate
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.2.2 0.0000068
-
 in situ Homo sapiens N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
2.1.2.2 0.0000072
-
 in situ Homo sapiens N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
2.1.2.2 0.0000086
-
 in situ Homo sapiens N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
2.1.2.2 0.000014
-
 in situ 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
2.1.2.2 0.000018
-
 in situ Homo sapiens N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
2.1.2.2 0.00003
-
 in situ Homo sapiens pemetrexed
2.1.2.2 0.00015
-
 in vitro Mus musculus N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
2.1.2.2 0.00078
-
 in vitro Mus musculus 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
2.1.2.2 0.001
-
 in situ Homo sapiens N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid
2.1.2.2 0.00226
-
 in vitro Mus musculus N-[4-[5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)pentyl]benzoyl]-L-glutamic acid
2.1.2.2 0.00244
-
 in vitro Mus musculus N-([4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)ethyl]phenyl]carbonyl)glutamic acid
2.1.2.2 0.00251
-
 in vitro Mus musculus N-[4-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexyl]benzoyl]-L-glutamic acid
2.1.2.2 0.02
-
 in vitro Mus musculus pemetrexed
2.1.2.2 0.02
-
 in vitro Mus musculus N-([4-[(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methyl]phenyl]carbonyl)glutamic acid