Reaction Details |
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Target | Trifunctional purine biosynthetic protein adenosine-3 |
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Ligand | BDBM50249875 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_497844 (CHEMBL1003027) |
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IC50 | 32±n/a nM |
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Citation | Deng, Y; Zhou, X; Kugel Desmoulin, S; Wu, J; Cherian, C; Hou, Z; Matherly, LH; Gangjee, A Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry. J Med Chem52:2940-51 (2009) [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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BDBM50249875 |
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n/a |
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Name | BDBM50249875 |
Synonyms: | CHEMBL522455 | N-{4-[2-(2-Amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)-ethyl]benzoyl}-L-glutamic Acid |
Type | Small organic molecule |
Emp. Form. | C20H20N4O6S |
Mol. Mass. | 444.461 |
SMILES | Nc1nc2sc(CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)cc2c(=O)[nH]1 |r| |
Structure |
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