Reaction Details Report a problem with these data
Target
Protein arginine N-methyltransferase 5
Ligand
BDBM435657
Substrate
n/a
Meas. Tech.
Biochemical Assay
IC50
0.800±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:
BDBM435657
Synonyms:
(2R,3S,4R,5R)-2-(((2-amino-3- bromoquinolin-7-yl)oxy)methyl)-3- methyl-5-(4-methyl-7H-pyrrolo[2,3- d]pyrimidin-7-yl)tetrahydrofuran-3,4-diol | US10570140, Example 55 | US11078205, Example 55 | US11208416, Example 55
Type:
Small organic molecule
Emp. Form.:
C22H22BrN5O4
Mol. Mass.:
500.345
SMILES:
Cc1ncnc2n(ccc12)[C@@H]1O[C@H](COc2ccc3cc(Br)c(N)nc3c2)[C@@](C)(O)[C@H]1O |r|
Structure:
Search PDB for entries with ligand similarity: