Target
Protein arginine N-methyltransferase 5
Ligand
BDBM422011
Substrate
n/a
Meas. Tech.
Revised Biochemical Assay
IC50
70.0±n/a nM
Citation
 Bergman, YEFoitzik, RCMorrow, BJCamerino, MAWalker, SRLagiakos, HRFeutrill, JStevenson, GIStupple, PA Tetrahydroisoquinoline derived PRMT5-inhibitors US Patent  US10494376 Publication Date 12/3/2019 
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:
BDBM422011
Synonyms:
US10494376, Example 124
Type:
Small organic molecule
Emp. Form.:
C24H29F3N4O3
Mol. Mass.:
478.5073
SMILES:
O[C@H](CNC(=O)c1ccnc(OC2CCN(CC(F)(F)F)CC2)c1)[C@@H]1Cc2ccccc2CN1
Structure:
Search PDB for entries with ligand similarity: