Reaction Details |
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Target | Trifunctional purine biosynthetic protein adenosine-3 |
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Ligand | BDBM50306576 |
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Substrate/Competitor | n/a |
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Meas. Tech. | GAR Transformylase Inhibition Assay |
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pH | 7.5±n/a |
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IC50 | 22±3 nM |
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Comments | extracted |
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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. Biochemistry55:4574-82 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Trifunctional purine biosynthetic protein adenosine-3 |
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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: | MAARVLIIGSGGREHTLAWKLAQSHHVKQVLVAPGNAGTACSEKISNTAISISDHTALAQ
FCKEKKIEFVVVGPEAPLAAGIVGNLRSAGVQCFGPTAEAAQLESSKRFAKEFMDRHGIP
TAQWKAFTKPEEACSFILSADFPALVVKASGLAAGKGVIVAKSKEEACKAVQEIMQEKAF
GAAGETIVIEELLDGEEVSCLCFTDGKTVAPMPPAQDHKRLLEGDGGPNTGGMGAYCPAP
QVSNDLLLKIKDTVLQRTVDGMQQEGTPYTGILYAGIMLTKNGPKVLEFNCRFGDPECQV
ILPLLKSDLYEVIQSTLDGLLCTSLPVWLENHTALTVVMASKGYPGDYTKGVEITGFPEA
QALGLEVFHAGTALKNGKVVTHGGRVLAVTAIRENLISALEEAKKGLAAIKFEGAIYRKD
VGFRAIAFLQQPRSLTYKESGVDIAAGNMLVKKIQPLAKATSRSGCKVDLGGFAGLFDLK
AAGFKDPLLASGTDGVGTKLKIAQLCNKHDTIGQDLVAMCVNDILAQGAEPLFFLDYFSC
GKLDLSVTEAVVAGIAKACGKAGCALLGGETAEMPDMYPPGEYDLAGFAVGAMERDQKLP
HLERITEGDVVVGIASSGLHSNGFSLVRKIVAKSSLQYSSPAPDGCGDQTLGDLLLTPTR
IYSHSLLPVLRSGHVKAFAHITGGGLLENIPRVLPEKLGVDLDAQTWRIPRVFSWLQQEG
HLSEEEMARTFNCGVGAVLVVSKEQTEQILRDIQQHKEEAWVIGSVVARAEGSPRVKVKN
LIESMQINGSVLKNGSLTNHFSFEKKKARVAVLISGTGSNLQALIDSTREPNSSAQIDIV
ISNKAAVAGLDKAERAGIPTRVINHKLYKNRVEFDSAIDLVLEEFSIDIVCLAGFMRILS
GPFVQKWNGKMLNIHPSLLPSFKGSNAHEQALETGVTVTGCTVHFVAEDVDAGQIILQEA
VPVKRGDTVATLSERVKLAEHKIFPAALQLVASGTVQLGENGKICWVKEE
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BDBM50306576 |
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n/a |
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Name | BDBM50306576 |
Synonyms: | (S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)-butyl]-thiophene-2-carbonyl}-amino)-pentanedioicAcid | AGF71 | CHEMBL590740 |
Type | Small organic molecule |
Emp. Form. | C20H23N5O6S |
Mol. Mass. | 461.492 |
SMILES | Nc1nc2[nH]c(CCCCc3ccc(s3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)cc2c(=O)[nH]1 |r| |
Structure |
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