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Target
Trifunctional purine biosynthetic protein adenosine-3
Ligand
BDBM192710
Substrate
n/a
Meas. Tech.
GAR Transformylase Inhibition Assay
pH
7.5±n/a
IC50
9±1 nM
Comments
extracted
Citation
 Deis, SM; Doshi, A; Hou, Z; Matherly, LH; Gangjee, A; Dann, CE Structural and Enzymatic Analysis of Tumor-Targeted Antifolates That Inhibit Glycinamide Ribonucleotide Formyltransferase. Biochemistry 55:4574-82 (2016) [PubMed]  Article 
Target
Name:
Trifunctional purine biosynthetic protein adenosine-3
Synonyms:
GAR Tfase | GAR transformylase | GART | Glycinamide ribonucleotide formyltransferase (GARFTase) | Glycinamide ribonucleotide transformylase (GAR Tfase) | PGFT | PRGS | PUR2_HUMAN | Thymidylate synthase/GAR transformylase/AICAR transformylase
Type:
Protein
Mol. Mass.:
107768.47
Organism:
Homo sapiens (Human)
Description:
P22102
Residue:
1010
Sequence:
MAARVLIIGSGGREHTLAWKLAQSHHVKQVLVAPGNAGTACSEKISNTAISISDHTALAQFCKEKKIEFVVVGPEAPLAAGIVGNLRSAGVQCFGPTAEAAQLESSKRFAKEFMDRHGIPTAQWKAFTKPEEACSFILSADFPALVVKASGLAAGKGVIVAKSKEEACKAVQEIMQEKAFGAAGETIVIEELLDGEEVSCLCFTDGKTVAPMPPAQDHKRLLEGDGGPNTGGMGAYCPAPQVSNDLLLKIKDTVLQRTVDGMQQEGTPYTGILYAGIMLTKNGPKVLEFNCRFGDPECQVILPLLKSDLYEVIQSTLDGLLCTSLPVWLENHTALTVVMASKGYPGDYTKGVEITGFPEAQALGLEVFHAGTALKNGKVVTHGGRVLAVTAIRENLISALEEAKKGLAAIKFEGAIYRKDVGFRAIAFLQQPRSLTYKESGVDIAAGNMLVKKIQPLAKATSRSGCKVDLGGFAGLFDLKAAGFKDPLLASGTDGVGTKLKIAQLCNKHDTIGQDLVAMCVNDILAQGAEPLFFLDYFSCGKLDLSVTEAVVAGIAKACGKAGCALLGGETAEMPDMYPPGEYDLAGFAVGAMERDQKLPHLERITEGDVVVGIASSGLHSNGFSLVRKIVAKSSLQYSSPAPDGCGDQTLGDLLLTPTRIYSHSLLPVLRSGHVKAFAHITGGGLLENIPRVLPEKLGVDLDAQTWRIPRVFSWLQQEGHLSEEEMARTFNCGVGAVLVVSKEQTEQILRDIQQHKEEAWVIGSVVARAEGSPRVKVKNLIESMQINGSVLKNGSLTNHFSFEKKKARVAVLISGTGSNLQALIDSTREPNSSAQIDIVISNKAAVAGLDKAERAGIPTRVINHKLYKNRVEFDSAIDLVLEEFSIDIVCLAGFMRILSGPFVQKWNGKMLNIHPSLLPSFKGSNAHEQALETGVTVTGCTVHFVAEDVDAGQIILQEAVPVKRGDTVATLSERVKLAEHKIFPAALQLVASGTVQLGENGKICWVKEE
  
Inhibitor
Name:
BDBM192710
Synonyms:
AGF118
Type:
Small organic molecule
Emp. Form.:
C21H27N5O6S
Mol. Mass.:
477.534
SMILES:
CC1SC(CCCCc2cc3c(nc(N)[nH]c3=O)[nH]2)C=C1C(=O)N[C@@H](CCC(O)=O)C(O)=O |r,c:21|
Structure:
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