Reaction Details Report a problem with these data
Target
Protein arginine N-methyltransferase 5
Ligand
BDBM453026
Substrate
n/a
Meas. Tech.
Biochemical Assay
IC50
1.60±n/a nM
Citation
 Luengo, J; Lin, H; Hawkins, M; Shetty, R; Pitis, P; Saborit Villarroya, G Selective inhibitors of protein arginine methyltransferase 5 (PRMT5) US Patent  US11254683 Publication Date 2/22/2022 
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:
BDBM453026
Synonyms:
(2R,3R,4S,5S)-2-(4-amino- 7H-pyrrolo[2,3-d]pyrimidin-7- yl)-5-((R)-6,7- dichloroisochroman-1- yl)tetrahydrofuran-3,4-diol | US10711007, Example 88 | US11214574, Ex# 88 | US11254683, Example 88
Type:
Small organic molecule
Emp. Form.:
C19H18Cl2N4O4
Mol. Mass.:
437.277
SMILES:
Nc1ncnc2n(ccc12)[C@@H]1O[C@@H]([C@@H](O)[C@H]1O)[C@@H]1OCCc2cc(Cl)c(Cl)cc12 |r|
Structure:
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