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Target
Protein arginine N-methyltransferase 5
Ligand
BDBM415566
Substrate
n/a
Meas. Tech.
PRMT5 assay
IC50
30.0±n/a nM
Citation
 Tatlock, JH; McAlpine, IJ; Tran-Dube, MB; Rui, EY; Wythes, MJ; Kumpf, RA; McTigue, MA Substituted nucleoside derivatives useful as anticancer agents US Patent  US10428104 Publication Date 10/1/2019 
Target
Name:
Protein arginine N-methyltransferase 5
Synonyms:
72 kDa ICln-binding protein | ANM5_HUMAN | HRMT1L5 | Histone-arginine N-methyltransferase PRMT5 | IBP72 | JBP1 | Jak-binding protein 1 | PRMT5 | PRMT5/MEP50 complex | Protein arginine N-methyltransferase 5 (PRMT5) | Protein arginine methyltransferase 5 (PRMT5) | SKB1 | SKB1 homolog | SKB1Hs | Shk1 kinase-binding protein 1 homolog
Type:
Enzyme
Mol. Mass.:
72679.99
Organism:
Homo sapiens (Human)
Description:
O14744
Residue:
637
Sequence:
MAAMAVGGAGGSRVSSGRDLNCVPEIADTLGAVAKQGFDFLCMPVFHPRFKREFIQEPAKNRPGPQTRSDLLLSGRDWNTLIVGKLSPWIRPDSKVEKIRRNSEAAMLQELNFGAYLGLPAFLLPLNQEDNTNLARVLTNHIHTGHHSSMFWMRVPLVAPEDLRDDIIENAPTTHTEEYSGEEKTWMWWHNFRTLCDYSKRIAVALEIGADLPSNHVIDRWLGEPIKAAILPTSIFLTNKKGFPVLSKMHQRLIFRLLKLEVQFIITGTNHHSEKEFCSYLQYLEYLSQNRPPPNAYELFAKGYEDYLQSPLQPLMDNLESQTYEVFEKDPIKYSQYQQAIYKCLLDRVPEEEKDTNVQVLMVLGAGRGPLVNASLRAAKQADRRIKLYAVEKNPNAVVTLENWQFEEWGSQVTVVSSDMREWVAPEKADIIVSELLGSFADNELSPECLDGAQHFLKDDGVSIPGEYTSFLAPISSSKLYNEVRACREKDRDPEAQFEMPYVVRLHNFHQLSAPQPCFTFSHPNRDPMIDNNRYCTLEFPVEVNTVLHGFAGYFETVLYQDITLSIRPETHSPGMFSWFPILFPIKQPITVREGQTICVRFWRCSNSKKVWYEWAVTAPVCSAIHNPTGRSYTIGL
  
Inhibitor
Name:
BDBM415566
Synonyms:
(2R,3R,4S,5R)-2-(4-(difluoromethyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-((R)-(3,4-difluorophenyl)(hydroxy)methyl)tetrahydrofuran-3,4-diol (UU-3) | US10428104, Example 97
Type:
Small organic molecule
Emp. Form.:
C18H15F4N3O4
Mol. Mass.:
413.323
SMILES:
O[C@@H]([C@H]1O[C@H]([C@H](O)[C@@H]1O)n1ccc2c(ncnc12)C(F)F)c1ccc(F)c(F)c1
Structure:
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