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Target
Protein arginine N-methyltransferase 5
Ligand
BDBM435525
Substrate
n/a
Meas. Tech.
Biochemical Assay
IC50
0.500±n/a nM
Citation
 Lin, H; Luengo, J; Shetty, R; Hawkins, M Selective inhibitors of protein arginine methlytransferase 5 (PRMT5) US Patent  US11078205 Publication Date 8/3/2021 
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:
BDBM435525
Synonyms:
(2R,3S,4R,5R)-2-(((2-amino-3- bromoquinolin-7-yl)oxy)methyl)-5-(4- amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)- 3-methyltetrahydrofuran-3,4-diol | US10570140, Example 12 | US11078205, Example 12 | US11208416, Example 12
Type:
Small organic molecule
Emp. Form.:
C21H21BrN6O4
Mol. Mass.:
501.333
SMILES:
C[C@@]1(O)[C@@H](COc2ccc3cc(Br)c(N)nc3c2)O[C@H]([C@@H]1O)n1ccc2c(N)ncnc12 |r|
Structure:
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